'World Meeting on Pharmaceutics, Biopharmaceutics ... · Scientific programme M Tuesday,9May1995...

1st World Meetingon

Pharmaceutics,Biopharmaceutics andPharmaceutical Technology

Budapest, 9 to 11 May 1995

UB/TIB Hannover 89

114 000 417

Scientific programme

M Tuesday, 9 May 1995

Room A

9.00 h Opening ceremony

9.20 h APV Medal

9.30 h Jean Marie Lehn, College de France, Paris

Supramolecular chemistry, Molecular recognition, self-organization and the

molecular information paradigm

10.30 h Break

11.00 h Oral sessions

Room A

Physicochemicalaspects of formulation

and preformulation

12.40 h Lunch break

14.00 h Poster session

Solid oral dosage forms, Nanoparticles, Liposomes,Transmembranal passage.

Posters will be exhibited from 10.30 h to 16.35 h. However authors are

requested to remain by their poster during this special session.


Room A Room B Room C

Physicochemical Microparticles Emulsions and

aspects of formulation suspensionsand preformulation

16.20 h Break


Room A Room B Room C

Cyclodextrins Delivery through mucosae Pellets

17.35 h End of session

RoomB

MicroparticlesRoomCDermal deliverysystems

5


Wednesday, 10 May 1995

Room A

9.00 h Helmut Ringsdorf, Institut fur Chemie, Mainz

What to learn from Mother Nature for drug delivery and biosensors,

Mimicking of biomembrane processes based on functional

supramolecular systems

10.00 h Break

10.20 h

11.20 h Break

Oral sessions

Room A RoomB RoomC

Solid oral dosage forms Cyclodextrins Pellets


Room ASolid oral dosage forms

12.30 h Lunch break

RoomB

Molecular targetingRoomC

Pellets


Delivery through mucosae, Pulmonary delivery, Transdermal delivery,

Pharmacolology, pharmacokinetics and biopharmacy, Emulsions and

suspensions, Stability, Sterilization, Lyophilization.




Room A Room B

Solid oral dosage forms Liposomes

16.20 h Break

RoomCBioadhesion

16.35 h Oral sessionsRoom A Room B

Solid oral dosage forms Liposomes


RoomC

Bioadhesion

6


Thursday, 11 May 1995

Room A

9.15 h Maurice Marie Janot Lecture, Daan J.A. Crommelin,Universiteit UtrechtInternational Jury President: Professor Trevor M. Jones

10.00 h Break

10.20 h Oral sessionsRoom A

Solid oral dosage forms

11.20 h Break

RoomB

NanoparticlesRoomC

Lyophilization


Room A


12.30 h Lunch break

RoomB

NanoparticlesRoomC

Stability


Microspheres, Pellets, Controlled release, Synthesis and analysis,Bioadhesion, Physicochemistry, Cyclodextrins, Miscellaneous




Room A


16.20 h Break

Room B

NanoparticlesRoomC

Pharmacology,pharmacokineticsand biopharmacy


Room A

Pulmonary deliveryRoomB

ProdrugsRoom C

Pharmacology,pharmacokineticsand biopharmacy


7

Tuesday, 9 May 1995

Room A

09.00 h Opening Ceremony

09.20 h APV Medal

09.30 h Jean-Marie Lehn, College de France, Paris

Supramolecular chemistry, Molecular recognition, self-organizationand the molecular information paradigm

10.30 h Break

Room A

Proceedings page

Physicochemical aspects offormulation and preformulationChairmen, Jelka Smid-Korbar and Praveen Tyle

11.00 h Obtaining new generation drugs on the basis of physically stablemetastable modifications of known substances

N. Leonidov 9

11.20 h The presentation of polymorphic systems by energy/temperature diagramsA. Burger and J.-O. Henck 10

11.40 h Drug of low solubility, Physicochemical characterization and dissolutionR. Alle, J. Berail, C. Boull6, A. Caron, C Condamine

and J.C. Gautier 12

12.00 h Interactions between fenoprofen sodium and hydrophilic polymeric excipientsT. Rades and C.C. Muller-Goymann 14

12.20 h Interactions between Carbopol 980 and additional second

macromolecule in aqueous formulations

M. Oechsner and S. Keipert 16

12.40 h Lunch break

Physicochemical aspects offormulation andpreformulationChairmen, Christel Muller-Goymann and Artur Burger

15.00 h Preformulation studies of a novel HIV protease inhibitor, AG1343

M. Longer, I. Zamansky and P. Tyle 18

15.20 h Influence of mechanical and thermal treatments on the

colloidal/chemical structure of a semisolid mixture

B. Otten and C. Fuhrer 20

15.40 h Partitioning and solubility of the psoralens used in therapyassessed through a spectrofluorimetric analysis

A. Said, P. Muret, S. Makki, J.-C. Rouland and J. Millet 22

16.00 h D-alpha tocopheryl polyethylene glycol 1000 succinate (TPGS) as

an absorption enhancerS.H.W. Wu, W. Hopkings and D. Wyatt 24

16.20 BreakProceedings page

CyclodextrinsChairmen, Dominique Duchene and Jose Luis Vila Jato

16.35 h Solution for insolubility problems of base-type drugs,Multi-component cyclodextrin complexation

L. Szente, J. Szejtli, M. Vikmon, J. Szeman, E. Fenyvesi,M. Pasini, E. Redenti and P. Ventura 579

16.55 h Idebenone/8-cyclodextrin inclusion complexes,Characterization and in vitro studies

C.A. Ventura, G. Puglisi, M.A. Vandelli and M.T. Zappala 581

17.15 h Interaction between 8-methoxypsoralen and cyclodextrinsM. Kata, F. Giordano, M. Rillosi, G.P. Bettinetti,A. Gazzaniga and LA. Hadi 583

Tuesday, 9 May 1995

RoomB

MicroparticlesChairmen, James McGinity and Tadeusz W. Hermann

11.00 h PDLLA microspheres containing steroids, Spray-drying and w/o/wemulsification as preparation methods

P. Giunchedi, A. Benvenga, H.O. Alpar and U. Conte 389

11.20 h Preparation of poly (D,L lactide-co-glycolide) microsphereswith narrow size distributions

C. Albayrak, S. Keipert, G. RSBling and R. Schmitz 391

11.40 h Ultrasound-induced degradation of aliphatic polyestersduring microsphere processing, Influence of formulation variables

G. Reich 393

12.00 h Composite swellable polymeric microparticles for improved bioavailabilityF. Carli and P.A. Esposito 395

12.20 h Bone morphogenic protein-2 release from freeze-dried polymer matrices

S. Duggirala and P.P. DeLuca 397

12.40 h Lunch break

MicroparticlesChairmen, Ubaldo Conte and Nicholas Peppas

15.00 h Microencapsulation of tetanus toxoid using poly(lactide-coglycolide)polymers and novel ABA-triblock copolymers for single-shot vaccines

R. Koneberg and T. Kissel 399

15.20 h Malaria antigen in biodegradable PLA/PLGA microspheres,Formulation and quality control aspects

E. Casali, G. Corradin, H.P. Merkle and B. Gander 401

10

Proceedings page15.40 h Enhancement of vaccine efficacy by induction of IgA with ricin toxoid

vaccine incorporated into poly(lactide-co-glycolide) (PLG) microspheresM. Kende, C. Yan,W. Rill, R. Malli, H. Naseem,J. Hewetson and R. Tammariello 403

16.00 h Protracted immunity evoked by ricin toxoid vaccine

incorporated into a new carrier systemC. Yan, W. Rill, J. Hewetson, R. Tammariello,R. Malli and M. Kende 405

16.20 h Break

Delivery through various mucosae

Chairmen, Peter Langguth and Gilles Ponchel

16.35 h In vivo buccal delivery of macromolecular drugsA.J. Hoogstraate, J. Verhoef, A.H.G.J. Schrijvers, A. Pijpers,L.A.M.G. van Leengoed, J.H.M. Verheijden, H.E. JungingerandH.E. Bodde 747

16.55 h Experimental anti-thrombotic effect of a low-molecular weight heparinabsorbed through the nasal mucosa, Role of the enhancing effect

of sodium glycocholateM. Buhannic, C. Bardin, F. Chast, C. Busin, L. Bara,M. Samama and J.-C. Chaumeil 749

17.15 h Characterization of the uterus as a site of drug administration

for systemic effect

A. Hoffman, I. Shaked, A. Nyska, A. Avramoff and G. Golomb 751

Tuesday, 9 May 1995

RoomC

Dermal and transdermal delivery systems

Chairmen, Veronique Preat-Haine and Bernhard C. Lippold

11.00 h Cosmetic efficiency assessment on human skin microtopographyS. Makki, P. Agache, P. Muret and J. Millet 679

11.20 h Microemulsion as a topical drug delivery vehicle for

local anaesthetics of the carbamate typeM. Zabka, M. Benkova and E. Racanska 681

11.40 h Universal hydrophilic drug-containing adhesive matrix

for systemic and topical transdermal drug deliveryA.E. Vasiliev, M.M. Feldstein, M.E. Pudel and N.A. Plate 683

12.00 h In vitro percutaneous permeation of a model zwitterion, baclofen

M. Sznitowska and S. Janicki 685

12.20 h Electroperturbation of the human skin barrier in vitro,

Effects on stratum comeum impedance and lipid fine structure

W.H.M. Craane-van Hinsberg, F. Spies, J. vErhoef and G. Gooris 687

12.40 h Lunch break

11

Emulsions and suspensionsChairmen, Jacqueline Plaizier-Vercammen and Yasemin Yazan

Proceedings

15.00 h HPMC as emulsifier for submicron emulsions

M. Schulz and R. Daniels 637

15.20 h Positively-charged self-emulsifying oily formulation

for improving oral bioavailability of progesteroneT. Gershanik and S. Benita 639

15.40 h Dry emulsions as a potential drug delivery systemG.P. Pedersen, P. Faldt, B. Bergenstahl and H.G. Kristensen 641

16.00 h Adsorption behaviour of a surfactant (oleic acid) on to salbutamol

base and salbutamol sulphate in non-aqueous suspensionP.M. Blackett and G. Buckton 643

16.20 h Break

Pellets

Chairmen, Luc Delattre and Christina Graffner

16.35 h Structure and pharmaceutical properties of pellets,Effect of the granulation liquid

M. Schroder and P. Kleinebudde 341

16.55 h Homogeneous pellets of binary mixtures,Comparison between extruder/ spheronizer and high-shear mixer

P. Kleinebudde and L. Nymo 343

17.15 h Matrix pellets based on the combination of waxes,

starches and maltodextrinsZ. Fang, C. Vervaet and J.P. Remon 345

Tuesday, 9 May 1995

Posters

Exhibited continuously from 10.30 to 16.35, with special session from 14.00 to 15.00 h.

The number indicates the number displayed on the poster panel.

Solid oral dosageforms

1 Influencing the neutralization effect of antacids usingpharmaceutical technological methods

R. Zelko, E. Bihari, E. Balogh and I. Riicz 181

2 Methodological approach of the particle size distribution of

two standard powders by image analysis and light scatteringC. Andres, P. Reginault, B. Chaillot and Y. Pourcelot 183

3 Formulation of dispersible tablets containing 50% of

active ingredient prepared by wet granulationM. Rosovsky, B. Huet de Barochez and A. Cuine 185

12

Proceedings page4 Spray-drying as a method to achieve hydrophilization of

sparingly soluble drugsG. Nork, M. Bisrat and H. Nyqvist 187

5 Instrumentation of fluid-bed granulator Niro-Aeromatic Strea-1 ®

for control of critical spray rate and of free humidityT. Abberger, H. Egermann and LA. Raneburger 189

6 Effect of the presence of a lubricant and a binder, respectively,on the compactibility of lactose granulations

G.K. Bolhuis, K. Zuurman and H. Vromans 191

7 Investigation of the mechanical properties of ethylcellulose by the

use of the Fraser-Susuki function and thermal mechanical analysisG. Shlieout, F. Wiese, T. Muller and G. Zessin 193

8 Influence of drying conditions on residual solvent contents in crystalsC. Barthelemy, P. Di Martino and A.-M. Guyot-Hermann 195

9 The effect of moisture content on the volume reduction

behaviour and the compactibility of amorphous lactose

T. Sebhatu, C. Ahlneck and G. Alderborn 197

10 New antiviral compound, Characterization and formulation

of tablet dosage formS. Bogdanova, T. Nikova, D. Sidzhakova and K. Mitikov 199

11 X-ray diffraction to study compression parameters of Compril®A. Mufioz-Ruiz, T. Pay£n, V. Velasco, C. Monedero, A. Justo

and M.R. Jimenez-Castellanos 201

12 The use of gravimetric studies to assess the degreeof crystallinity of predominantly crystalline powders

G. Buckton and P. Darcy 203

13 Investigation of the effect of type and source of microcrystallinecellulose on capsule filling

R. Patel and F. Podczeck 205

14 Influence of the crystallinity of cellulose on its compactibilityand compressibility

H. Gerecke, M. Dittgen, S. Fricke and H. Oelschlager 207

15 Study of flowability and compressibility of microcrystallinecelluloses with different morphological characteristics

P. Szabo-Revesz, K. Pintye-Hodi, P. Kasa Jr and B. Selmeczi 209

16 Behaviour of Vivacel® comprimates during loadingK. Pintye-Hodi, P. Szabo-Revesz, P. Kasa Jr and B. Selmeczi 211

17 Technological comparison of two microcrystalline cellulose brands (c.m.c.)

JJ. Diaz-Esquivel, C.F. Perez-Alvarez, R. Lopez Arellano and

A. Cervantes-Sandoval 213

18 Compactibility curves as a characteristic of technologicalbehaviour of powders

L. Villafuerte Robles 215

13

Proceedings page19 Compactibility of the microcrystalline cellulose 102/calcium

phosphate dihydrate systemL. Villafuerte Robles 217

20 Tabletting properties of pellets of varying porosity consistingof dicalcium phosphate and microcrystalline cellulose

B. Johansson, F. Nicklasson and G. Alderborn 219

21 Evaluation of bonding mechanisms of pharmaceutical materials

by compaction and strength characterization of compacts in liquidA. Adolfsson, H. Olsson and C. Nystrom 221

22 Comparison of the compressional behaviour of four batches of spray-driedlactose with the help of a non-instrumented single-punch machine

E. Joiris, S. Tak Tak and J.-C. Guyot 223

23 Ultrasound-assisted compaction of pharmaceutical materials,

(1) Description and preliminary evaluation of the apparatusM.F. Saettone, B. Giannaccini, D. Monti, I. Cabani,L. Rodriguez, M. Cini, C. Cavallari and O. Caputo 225

24 Ultrasound-assisted compaction of pharmaceutical materials,(2) Preparation of matrices for sustained release of theophylline

L. Rodriguez, M. Cini, N. Passerini, O. Caputo, B. Biannaccini,D. Monti and M.F. Saettone 227

25 Formulation, quality control parameters and release rate for clonidine tabletsD. Lupuleasa, A.M. Dumitrescu, V. Hirjau, M. Pana, I. Popovici,V. Dorneanu, M. Stan, G. Tantaru and N. Bibire 229

26 Drug liberation from tablets containing Vitacel®

M. Vitkova, N. Shalan, J. Rak and M. Chalabala 231

27 Investigation on tablet disintegrating power, Application to a

croscaramellose sodium, Primellose®S. Rizk, C. Barthelemy, C. Duru and A.-M. Guyot-Hermann 233

28 New method for disintegration process analysis in pharmaceutical tabletsL. Maggi, G. Massimo, R. Bettini, P.L. Catellani and P. Colombo 235

29 Dissolution enhancement of an insoluble drug by physical mixturewith a superdisintegrant, Optimization with a simplex lattice design

F. Ferrari, M. Bertoni, M.C. Bonferoni, S. Rossi, C. Caramellaand G.K. Bolhuis 237

30 Effect of crospovidone on the physical properties of acetaminophen tabletsM. Sheikh Salem, G.K. Pillai and A.A. Badwan 239

3.1 The influence of the cross-linking degree on drug dissolution,water uptake and swelling profiles of cross-linked amylose matrices

I.S. Moussa and L.H. Cartilier 241

32 In vitro evaluation of molsidomin release from thermallypregelatinized starch matrices

V. Mihailova, V. Andonova and P. Kazanjieva 243

14

Proceedings page33 Controlled release of theophylline from hydrophilic matrices based

on modified starches, Capsule and tablet availability studiesC. Barthelemy, P. Degen, B. Frimat, A. Delacourte and H. Robert 245

34 Advantage of the use of an experimental design for determining theinfluence of the manufacturing parameters on the release of an

active ingredient from a hydrophilic matrixE. Le Doeuff, J.L. Avan, J. Bougaret and E. Goutay 247

35 Study of pentoxifylline release from matrix tablets based on cellulose ethersF. Vrecer and A. Kramar 249

36 Alginate as hydrophilic matrix for controlled release tabletsmade by direct compression

T. Grenager and J. Karlsen 251

37 Co-transformed matrices for oral controlled releaseR.TJ. Mutambara, J.N. Staniforth and D.J.G. Davies 253

38 Oral sustained release of nifedipine from tablets prepared with polyacrylatesR. Maraqa and S .E. Leucuta 255

39 Use of an acrylic and metacrylic acid derivative as a sustained release

matrix for theophylline hydrate tablets

S.I. Ofoefule and A. Chukwu 257

40 Sustained release effect of a natural polymer in chlorpheniraminemaleate tablet formulations

A. Chukwu, J.I. Mbanisi and S.L Ofoefule 258

41 An assessment of the performance of matrices containinghydroxypropyl methylcellulose, sodium carboxy methylcelluloseand propranolol hydrochloride

J.L. Ford, M.A. Dabbagh, M.H. Rubinstein and J.E. Hogan 259

42 Formulation of sustained release propranolol hydrochloride tablets

using hydroxypropyl methylcellulose matrices

A. Bodea, A. Bakri, C. Jeannin and S.E. Leucuta 261

43 In vitro evaluation of sustained release matrix tablets prepared with

new modified polymeric carbohydratesM.V. Velasco, I. Castellano, A. Muiioz, I. Goni,M. Gurruchaga and M.R. Jimenez-Castellanos 263

44 Dissolution of diflunisal from controlled release tablets

C. Martinez-Oharriz, C. Martin, M.M. Goni,C. Rodriguez-Espinosa and M. Sanchez 265

45 Process variables affecting performance of modified release dosageforms of nifedipine prepared by the solvent evaporation method

J.M. Khanna, H. Sen, V.K. Arora and K.V. Rangaiah 267

46 Pharmaceutical availability of oxazepam from solid dispersion systemsR. Jachozicz 269

15

Proceedings page47 Use of lipid matrices of Gelucire for sustained release

of salbutamolR.M. Hernandez, A. San Vicente, A. Esquisabel, M. Igartua,D. Ilardia and J.L. Pedraz 270

48 Design of diclofenac sodium 100 mg sustained release tablets,In vitro and in vivo studies

E. Sallam, S. Al-Deleq, M. Shubair, S. Zemeili, M. Hasan,N. Najib and T. Arafat 272

49 Pharmaceutical testing of sustained release theophyllineproducts on the Turkish market

O. Coskun, G. Aksoy and I. Agabeyoglu 274

50 A polymeric matrix tablet containing a centralized drug core

exhibiting bimodal release propertiesD.L. Munday 276

51 A delayed delivery system for colonic drug release

M.A. Vandelli, F. Forni and M.T. Bernabei 278

52 Development and scale-up of new film-coated Tisasen A+B

10 and 20 mg tablets

Z.B. Jeko and M. Mit6 280

53 The effect of atomizing air pressure on the aqueous film coatingprocess and on film coat quality

A.M. Twitchell, J.E. Hogan and M.E. Aulton 282

54 Protector effect of some coating agents in fluidized bed,

Comparative study and application to josamycine and paracetamolE. Cauture, P. Prinderre, M. Todorova, P. Piccerelle,R. Boistelle and J. Joachim 284

55 Delayed release system based on retarding low viscosityHPMC coating

A. Gazzaniga, C. Busetti, L. Moro, C. Lombardi

and F. Giordano 286

56 Zero-order release by partial coating ofHPMC matrix tablets with

permeable and semi-permeable films

R. Bettini, G. Massimo, P.L. Catellani, N.A. Peppasand P. Colombo 288

57 Control of drug release by ternary film coatingsP.I. Fekete and I. Antal 290

58 The influence of process parameters on the quality of enteric

polymethacrylate film coatingsB. Brogmann and P. Wolff 292

59 Diffusion/osmotic drug release control by ammonio methacrylate(Eudragit RL/RS) copolymers

P.L Fekete and M. Kiraly 294

16

Nanoparticles Proceedings page

60 Influence of the viscosity of the dispersed phase on the mean diameterof nanoparticles prepared by emulsification/solvent evaporation

S. Desgouilles, D. Bazile, L-L. Grossiord, J.-R. Authelin,M. Veillard and P. Couvreur 475

61 Biopharmaceutical studies of poly (methyl glyoxylate) as a potentialdrug carrier

R. Duclos, C.H. Brachais, B. Mac6, C. Bunel

and A.-M. Orecchioni 477

62 Preparation, characterization, toxicity and efficacy ofamphotericin B-loaded poly(caprolactone) nanoparticles

M.S. Espuelas, J.M. Irache, A.-M. Orecchioni, C. Gamazo

and P. Ygartua 479

63 Stability study of poly (D,L-lactide), poly(D,L-lactide-co-glycolide)and poly(e-caprolactone) nanoparticles

D. Lemoine, C. Francois, V. Berlage, F. Kedzierewicz,P. Maincent, M. Hoffman and V. Preat 481

64 Polyethyl-2-cyanoacrylate nanocapsules, Influence of preparationconditions on the mechanisms of formation

M. Fresta, G. Puglisi, G. Giammona, C.A. Ventura and

G. Cavallaro 483

65 Sterilization of drug-free and tetracaine-loaded solid lipidnanoparticles

C. Schwarz and W. Mehnert 485

66 In vivo photodynamic activity of hexadecafluoro zinc phthalocyaninloaded in PEG-coated nanoparticles

E. Allemann, S. Kudrevich, K. Lewis, R. Gurnyand J.E. van Lier 487

67 Solid lipid nanoparticles, Determination of in vivo toxicityH. Weyhers, S. Ehlers, W. Mehnert, H. Hahn nd R.H. Miiller 489

68 Nanosuspensions, A novel formulation for the intravenous

administration of poorly soluble drugsR.H. Miiller, K. Peters, R. Becker and B. Kruss 491

69 Effect of storage conditions on long-term stability of solid lipidnanoparticles in aqueous dispersion

C. Freitas, J.S. Lucks and R.H. Miiller 493

70 Comparison of drug-loaded and drug-free physiological low-densitylipoproteins and artificial lipid particles

A. Gerke, K. Westesen and M.H.J. Koch 495

71 Complex fats as matrix constituents in lipid nanoparticlesH. Bunjes, K. Westesen and M.H.J. Koch 497

72 Stability studies of the doxorubicin association to new colloidal

carriers made of amphiphilic cyclodextrinsF. Leroy-Lechat, D. Wouessidjewe, D. Duchene and F. Puisieux 499

17

Proceedings page73 Physicochemical characterization of vicilin coacervates

and small-sized particlesI. Ezpeleta, LM. Irache, S. Staimesse and A.-M. Orecchioni 501

74 Legumin nanoparticles, In vitro response of human skin fibroblasts

and immunological behaviour in rats

T. Mirshahi, LM. Irache and A.-M. Orecchioni 503

75 Comparative study on encapsulation of an azole compound within

colloidal drug carrier systemsS. de Chasteigner, H. Fessi, J.-P. Devissaguet and F. Puisieux 505

76 Estimation of hydrodynamic sizes of dextran coated iron oxide

nanoparticles by size exclusion chromatographyM. Kresse, D. Pfefferer, K. Thode, R.H. Miiller and W. Semmler 507

77 Mini-HIC for the determination of the surface hydrophobicityof magnetite dispersions

K. Thode, M. Kresse, D. Pfefferer, W. Semmler and R.H. Muller 509

78 Development of a quantitative PAGE analysis using a multi-channel

radioactivity counter for oligonucleotide drug carrier evaluationI. Aynid, M. Foulquier, E. Fattal, F. Puisieux, P. Couvreur

and C. Vauthier 511

79 Characterization of microspheres loaded with a cholecystokininderivative peptide

MJ. Blanco Prieto, E. Fattal, F. Delie, V. Dauge, B.P. Roquesand P. Couvreur 513

80 Protection against muscular side effects of diclofenac byencapsulation in poly(D,L-lactide) nanocapsules

S. Guterres, H. Fessi, G. Barratt, F. Puisieux and J.-P. Devissaguet 515

81 Poly(D,L-lactide) nanocapsules containing non-steroidal anti¬

inflammatory drugs, Gastro-intestinal tolerance followingintravenous and oral administration

S. Guterres, H. Fessi, G. Barratt, F. Puisieux and J.-P. Devissaguet 517

82 Effects of mononuclear phagocyte system of acute administration of

polymeric nanoparticlesR. Fernandez-Urrusuno, LM. Rodrigues Jr, E. Fattal,P. Bedossa and P. Couvreur 519

83 Induction of macrophage nitric oxide synthase by an immunomodulator

entrapped within polymeric nanocapsulesI. Seyler, G. Barratt, M. Appel, J.-P. Devissaguet and F. Puisieux 521

84 Uptake and localization of fluorescent polystyrene nanoparticlesin the spleen

M. Demoy, J.P. Andreux, C. Weingarten, S. Gibaud and P. Couvreur 523

85 Phagocytic uptake of polymeric particles in vitro, Effect of surface

hydrophobicity and fluorescent labellingD. Riihl, B.-R. Paulke, H.R. Maurer and R.H. Muller 525

18

Proceedings page86 Influence of nanoparticles on the body distribution of

azidothymidin (AZT)R. Lobenberg, L. Araujo and J. Kreuter 527

87 Nanoparticles as a carrier system for an HIV-protease inhibitorA. Bender, H. von Briesen, H. Riibsamen-Waigmannand J. Kreuter 529

88 Influence of polyethylene oxide chains on protein adsorptionon nanoparticles for drug targeting

T. Blunk, M. Luck, B.W. Muller and R.H. Muller 531

89 Drug targeting in leishmaniasis, Factors affecting the fate of

colloidal carriers in Leishmania donovani-infectcd miceLM. Rodriguez Jr, H. Fessi, R. Fernandez-Urrussuno,C. Bories and J.-P. Devissaguet 533

Liposomes

90 Physical stability studies on different liposome preparationsA. Memoli, L.G. Palermiti, V. Travagli and F. Alhaique 551

91 Prediction of physical stability of liposomes by the EPR method

K. Gregorc, J. Kristl, V. Gabrijelcic, M. Sentjurcand J. Smid-Korbar 553

92 Particle size analysis of liposomes in hydrogels by photoncorrelation spectroscopy (PCS)

J. Herbort, J.E. Diederichs and R.H. Muller 555

93 Design and characterization of a liposome dispersion in poloxamer 407

A. Bochot, E. Fattal, J.-L. Grossiord, F. Puisieux and

P. Couvreur 557

94 The use of pressurized aerosols for the topical delivery of

liposomes/phospholipidsA. Sasse, D.Q.M. Craig, K.M.G. Taylor and D. Gregory 559

95 In vivo studies on radio-opaque liposomes containing iopromideS. Erdogan, A.Y. Ozer, M.T. Ercan and A.A. Hincal 561

96 Lipophilic amide derivatives of methotrexate, DSC studies on their

interaction with DPPC liposomes as a membrane model

R. Pignatello, M. Fresta and G. Puglisi 563

97 Drug/phospholipid interaction evidence by fluorescence measurements

A. Doisy, J.-L. Dubois and LC. Brochon 565

98 Liposomes for oral immunization

S. Ouadahi, G. Barratt, I. Genin, C. Andre, T. Tran Xuan,J.-P. Devissaguet, F. Puisieux and M. Paternostre 567

99 Amphotericin B release from liposomes and its action againstfungal and mammalian cells

P. Legrand, M. Cheron, H. Fessi, J.-P. Devissaguet and J. Bolard 569

19

Proceedings page100 Interleukin-2 and dipalmitoyl phosphatidylcholine liposomes,

Evidence for a specific interaction

L. Fleury, M. Ollivon, J.-L. Dubois, F. Puisieux and G. Barratt 571

101 Characterization of liposome uptake by macrophagesM. Macchluf, I. Likhman and S. Cohen 573

102 Establishment of the endocytic capability of platelets and determination

of the feasibility of carrier-mediated drug delivery to plateletsP. Bandyopadhyay, G.H. Rao and Y.E. Rayman 575

Transmembranal passage

103 Raman spectroscopy and differential scanning calorimetry for

characterizing structure and function of the stratum corneum ceramides

M. Wegener, R. Neubert, W. Rettig and S. Wartewig 851

104 Mathematical assessment of different penetration mechanisms

from vehicles with propylene glycolS. Huth, R. Neubert and L. Boltze 853

105 Comparative study of the release of a model compound using two

types of artificial membrane

A.M. Rodriguez Bayon and A.M. Ariza Osorio 854

106 Comparative study of ISDN transport through biological and

artificial membranes

N. Cvetkovic, M. Rosic, M. Nesic, B. Vujovic and T. Nedeljkovic 856

107 NADH, Evaluation of the possibilities for permeation throughbiological membranes

C. Mattern, R. Hacker and H.-H. Borchert 858

108 Bisphosphonates increase tight junction permeability in the

human intestinal epithelial (Caco-2) model

X. Boulenc, C. Roque and Y. Berger 860

109 Paracellular transport and other mechanisms involved in intestinal

peptide absorptionV. Bohner, B. Rothen-Rutishauser, LC. Perriard, C. Ottiger,H. Wunderli-AUenspach, H.P. Merkle and P. Langguth 862

110 Blood/brain barrier in vitro, Rapid evaluation of strategies for

achieving drug targeting to the central nervous systemM.P. Dehouck, B. Dehouck, E. Teissier and R. Cecchelli 864

20


Room A

09.00 h Helmut Ringsdorf, Institut fur Chemie, MainzWhat to learn from Mother Nature for drug delivery and biosensors,Mimicking of biomembrane processes based on functional

supramolecular systems

10.00 h Break

Room A

Solid oral dosage formsChairmen, James L. Ford and Istvan Racz

Proceedings page

10.20 h Flow properties of two pharmaceutical powders, Assessment byJenike's shear test and by air permeability

G. Mortha and C. Jeannin 135

10.40 h Characterization of wetting behaviour of pharmaceutical powdersby contact angle measurement using capillary rise technology

H. Lechner 137

11.00 h Power wettability and agglomeration in the granulation processS. Kiortsis and S. Malamataris 139

11.20h Break

Solid oral dosageformsChairmen, Gerad K. Bolhuis and Stavros Malamataris

11.30 h Differential scanning calorimetry, An alternative for compatibilitystudies of complete mixtures for fabricating tablets

R.M. Cruz-Hernandez and F. Mijangos-Santiago 141

11.50 h A new maltodextrin as filler/binder for direct compressionK.-L Steffens 143

12.10 h Binding performance of pregelatinized starchesC.W. Symecko and C.T. Rhodes 145

12.30 h Lunch break

Solid oral dosage formsChairmen, Paolo Colombo and Jan Karlsen

15.00 h Disintegration efficiency of sodium starch glycolate preparedfrom enset starch

T. Gebre-Mariam and P.C. Schmidt 147

15.20 h Image analysis for the study of water penetration and polymerswelling in cross-linked amylose

I.S. Moussa and L.H. Cartilier 149

21

Proceedings page15.40 h Growth kinetics of granulation in a high-shear mixer

H.G. Kristensen and T. Schaefer 151

16.00 h Compressive elastic modulus and strength isotropy of tabletted

pharmaceutical powdersS. Malamataris, T. Hatjichristos and LE. Rees 153

16.20 h Break

Solid oral dosageformsChairmen, David LG. Davies and Fritz Stanislaus

16.35 h NIR spectroscopy as a tool for in-process control in pharmaceuticalproduction, An example

K.-J. Steffens and K. List 155

16.55 h Instrumented punch for rotary tablet machines

A. Gullatz and K.-L Steffens 157

17.15 h Use ofpercolation theory to interpret the deformation hardness,the tensile strength and the modified Young's modulus of tablets

consisting of Sta-RX 1500®, a-monohydrous lactose, either as

powder or as granulesL. Ineichen and H. Leuenberger 159


RoomB

CyclodextrinsChairmen, Bernd W. Muller and Jozsef Szejtli

10.20 h Characterization and dissolution rate of tolbutamide/6-cyclodextrincomplexes prepared by different methods

F. Veiga, J.J. Teixeira-Dias and A. Sousa 585

10.40 h Preparation and properties of a physiologically active nitric oxide

releasing agentM. Vikmon, J. Szemdn, J. Szejtli and J. Geczy 587

11.00 h Diclofenac/6-cyclodextrin inclusion compounds,Characterization and dissolution studies

B. Cappello, F. Barbato, M.I. La Rotonda and A. Miro 589

11.20 h Break

Molecular targetingChairmen, Joseph R. Robinson and Alan S. Rudolph

11.30 h PK1/PK2 lyophilized formulations, HPMA/doxorubicin conjugateswith potentially improved anti-tumour activity

A. Cavallo, M. Adami, R. Magrini and G. Colombo 843

11.50 h Enhanced site-specific tumor therapy with monoclonal antibodies

V.P. Torchilin and L.Z. Iakoubov 845

22

Proceedings page12.10 h Polysialylated catalase, In vitro characterization

A.I. Fernandes and G. Gregoriadis 847

12.30 Lunch break

LiposomesChairmen, Rainer H. Muller and Smadar Cohen

15.00 h Importance of zeta potential and hydrophobicity of liposomalpolymyxin B for macrophage uptake and the implications for

lung deliveryS .M. McAllister, H.O. Alpar and M.R.W. Brown 537

15.20 h Site-specific delivery of liposomes to the heart

V.P. Torchilin, J. Narula and B .A. Khaw 539

15.40 h Imrnunoliposomes as carriers of enzymes for site-specificactivation of anti-cancer prodrugs

G. Storm, M.H. Vingerhoeds, H.J. Haisma and D.J.A. Crommelin 541

16.00 h Biological effectiveness of CDP-choline loaded long-circulatingliposomes on in vivo rat ischaemia model

M. Fresta, E. Wehrli and G. Puglisi 543

16.20 h Break

LiposomesChairmen, Daan LA. Crommelin and Ayla Giirsoy

16.35 h Optimized liposomal amikacin for the treatment of disseminated

mycobacterial infections

W.E. Bucke, S. Ehlers, S. Leitzke, LE. Diederichs,H. Hahn and R.H. Muller 545

16.55 h Binding of LPS and phagocytosis of liposome-encapsulatedhaemoglobin attenuates tumor necrosis factor production in

ex vivo murine splenocytes and RAW264.7 cells

A.S. Rudolph, R.O. Cliff, V. Kwasiborski, H. Spielbeg,L. Neville, F. Abdullah and R. Rabinovici 547

17.15 h Activation of rat complement by the red cell substitute,

liposome-encapsulated haemoglobinJ. Szebeni, N.M. Wassef, H. Spielberg, A.S. Rudolphand C.R. Alving 549


Room C

Pellets

Chairmen, Henning G.Kristensen and Tor Waaler

10.20 h Dipyridamole coated pellets prepared by fluidized-bed coatingD.B. Beten, K. Amighi and A.J. Moes 347

23

Proceedings10.40 h The influence of the properties of drug on the preparation of

spherical pellets by extrusion/spheronizationC. Lustig, F. Podczeck and LM. Newton 349

11.00 h The use of a two- and a three-dimensional shape factor to

characterize the sphericity of pelletsF. Podczeck, R. Chopra and LM. Newton 351

11.20 h Lunch break

Pellets

Chairmen, John Newton and Andre Moes

11.30 h Ion exchange resin complex with S(+)-ibuprofen for oral dosageforms with improved dissolution behaviour

K. Cremer, W. Muller and D. Scherer 353

11.50 h The influence of five selected processing and formulation variables

on the release of riboflavin from pellets produced in a rotary processorJ. Vertommen and R. Kinget 355

12.10 h Some technological factors influencing drug release fromB-blocker containing polymer-coated particles

S. Marton, E. Bihari, A. Orban, D. Greskovits and I. R&cz 357

12.30 h Lunch break

Bioadhesion

Chairmen, Pierre Buri and Carla Caramella

15.00 h Oral mucosa enhanced delivery of gonadotropin-releasing hormone,(1) Development of mucoadhesive device

Y.W. Chien, Y. Lee, S. Nakane and K. Yukimatsu 811

15.20 h Oral mucosa enhanced delivery of gonadotropin-releasing hormone,

(2) In vivo evaluations of GnRH-mucoadhesive devices

Y.W. Chien, S. Nakane, Y. Lee, M. Kakumoto and K. Yukimatsu 813

15.40 h Bioadhesive interactions of lectin/latex conjugates with rat

intestinal mucosa

G. Ponchel, J.M. Irache, C. Durrer, F. Puisieux and D. Duchene 815

16.00 h Bioadhesive polyvinyl alcohol) as a carrier for controlled release

of growth factors and proteinsN.A. Peppas, N. Mongia and A.S. Luttrell 817

16.20 h Break

Bioadhesion

Chairmen, Hans E. Junginger and Sorin E. Leucuta

16.35 h Control of acid neutralization and bioadhesion of aluminium and

magnesium containing antacid preparationsI. Antal, J. Plachy, Z. Muskath, M. Gyorffi and I. Racz 819

24

Proceedings page16.55 h Obtention of bioadhesive pellets by extrusion/spheronization

J.L. Vila Jato, J. Blanco-Mendez, F.L Otero-Espinar,S. Anguiano-Igea and J. Amela 821

17.15 h Release and 'washability' properties of mucoadhesive gelsS. Rossi, M.C. Bonferoni, F. Ferrari, M. Bertoniand C. Caramella 823


Posters

Exhibited continuously from 10.00 to 16.35, with special session from 14.00 to 15.00 h.The number indicates the number displayed on the poster panel.

Delivery through various mucosae

111 Bucco-adhesive two-layer tablet for topical delivery of AcitretinP. Minghetti and L. Montanari 753

112 Absorption studies in vivo after nasal administration of propiomazineC. Bjerre, E. Bjork and O. Camber 755

113 Nasal administration of the 5-HTia receptor antagonist(S)-5-fluoro-8-hydroxy-2-(dipropylamino) tetralin

M. Dahlin, C. Bogentoft and E. Bjork 757

114 Formulation and in vitro study of anti-malarial rectal suppositoriesG. Regdon Jr, I. Schirm, B. Selmeczi and G. Regdon 759

115 Recrystallization studies on indomethacin suppositoriesL. Albertin and M. Rillosi 761

Pulmonary delivery

116 Depression of glass transition temperature of amorphous spray-driedsalbutamol sulphate

G. Venthoye, K.M.G. Taylor, J.M. Newton and M.C.R. Johnson 771

117 Nebulization of fluids with different surface tensions

O.N.M. McCallion, K.M.G. Taylor, M. Thomas and A.J. Taylor 773

118 Formulation and characterization of aerosol suspensions for inhalationS. Tzolova, L. Stanoeva, P. Kazandjieva, L. Naumova,F. Michailova and V. Zidarova 775

119 Comparative study of the in vitro availability of aerosol emitted

by various jet nebulizers

M.-P. Flament, P. Leterme, T. Burnouf and A.T. Gayot 777

120 In vitro performance of Jago's dry powder inhaler (Prototype No.9),Glaxo's Diskhaler® and Astra's Turbuhaler® using the

twin impinger BP 93 as the test deviceE. Trachslin, M. Keller and U. Gaibrois 779

25

Proceedings page

121 Effect of various actuators/nozzles on the in vitro depositionpattern of liquid metered dose inhalers powered byhydrofluorocarbons

M. Keller, E. Trachslin and H. Kraus 780

122 Evaluation of effective cut-off diameters of a multi-stage liquid impingerG. Wamke, D. Konig, K.H. Bauer and M. Brandl 782

Ophthalmic delivery

123 Determination of the influence of a series of excipients on the irritation

potential of a local anaesthetic on the murine cornea

P. Kalin, LC. Etter and LM. Mayer 787

124 Rheological and surface tension measurements on commercial

tear substitutes

S. Keipert and M. Oechsner 789

125 Fungicidal activity of benzalkonium chloride in acidic

ophthalmic solutionsG. Chastaing, A. Rozier and B. Plazonnet 791

126 Stability of amphotericin B eye-drops as lipidic emulsionT. Cohen, D. Brossard, H. Sauvageon-Martre, F. Chastand J.-C. Chaumeil 793

127 Enhancementsof the bioavailability of pilocarpine in aqueouseye-drops by means of cyclodextrins

J. Fedder and S. Keipert 795

128 Gelrite® in ophthalmic formulations, Evaluations of rheologicalproperties and in vz'frorelease from pilocarpine/Gelrite® preparations

V. Hartmann and S. Keipert 797

129 Evaluation of niosomes as carriers for ophthalmic drugs,(1) Tests with cyclopentolate

G. Perini, M.F. Saettone, M. Carafa, E. Santucci and F. Alhaique 799

130 Evaluation in vitro/in vivo of colloidal lipospheres containingpilocarpine as ion pair

R. Cavalli, S. Morel, M.R. Gasco, P. Chetoni, M.F. Saettone

and L. Mariotti Bianchi 801

131 Spray-dried microspheres for ocular administration of piroxicam,In vitro/in vivo evaluation

P. Giunchedi, M.F. Saettone, P. Chetoni, L. Fusi and U. Conte 803

132 Ophthalmic mini-tablets for controlled release of timolol

M.F. Saettone, P. Chetoni, L. Mariotti Bianchi, B. Giannaccini,U. Conte and M.E. Sangalli 805

133 Formulation of ocular inserts with reticulated collagenE. Gafitanu, S. Braha, V. Trandafir and O. Coman 807

26

Dermal and transdermal deliveryProceedings page

134 Psoralen percutaneous absorption in respect of their molecular

polarities, An in vitro studyJ. Millet, P. Muret, S. Makki and P. Bassignot 689

135 Permeation kinetics of oestradiol in Transcutol® solution and its

relationship to water absorptionA. Ganem, M. De Carvalho, F. Falson-Rieg and P. Buri 691

136 A study of micronized zinc oxide powders for topical applicationsA. Martini, M.-F. Bobin, A. Revillon and M.-C. Martini 693

137 An investigation into the dielectric and rheological behaviour of

cream bases

G. Vuleta, S. Tamburic and D.Q.M. Craig 695

138 Evaluation of rational contents of pentacaine and heptacaine in hydrogelsK. Gardavska, Z. Vitkova, J. Cizmarik and J. Rak 697

139 Cutaneous gels, Rheological behaviour and FTIR studies

P. Piccerelle, M. Bohor, G. Joachim, LP. Reynier,G. Kalantzis and J. Joachim 699

140 A new transdermal in vitro model for human skin, Comparison of the

transdermal in vitro permeability of excised bovine udder skin with

human skin

K. Ahrens, M. Dittgen, H. Oelschlager and C. Volkel 701

141 Investigation of the influence of polyethylene glycol bases of various

average molecular masses on nitroglycerol release

M. Zivkovic and S. Mihaijlovic 703

142 Dermatological pharmaceutical form based on non-steroid

anti-inflammatory agentA. Nedeva, F. Michailova and L. Maksimova 705

143 Enhancement of piroxicam permeation through rat skin

S. Santoyo, A. Arellano, P. Ygartua and C. Martin 707

144 Enhancing effect of terpenes on the percutaneous absorption of

diclofenac sodium

A. Arellano, S. Santoyo, C. Martin and P. Ygartua 709

145 The optimization of anti-burn ointments containing essential oils

E. Diug, V. Prisacari, V. Rudic, A. Taran, M. BodrugandE. Revenco 711

146 A new formulation approach for the treatment of psoriasisM.K. Youssef, LA. Attia and M.A. Fouda 713

147 In vitro studies on ketoprofen transdermal preparations based on

carrageenanP. Caybasi and T. Tuncel 715

27

Proceedings page

148 Cutaneous distribution of a new anti-androgen from liposomes andsolution in a hairless rat model

E. Bernard, J.-L. Dubois, P. Becourt and J. Wepierre 717

149 Multi-component surfactant systems as potential carriers for non¬

steroidal anti-inflammatory agentsK. Stein and S. Keipert 719

150 Influence of a microemulsion containing diclofenac diethylamine onthe permeability of human stratum corneum

I. Eder and C.C. Muller-Goymann 721

151 Influence of microemulsions on the lipid barrier of human skin

U. SchmalfuB, R. Neubert and W. Wohlrab 723

152 In vitro permeation of B-blockers from microemulsions

F. Pattarino, M.E. Carlotti, M. Trotta and M.R. Gasco 725

153 In vitro permeation of pentacaine from microemulsion and

microemulsion gelM. Zabka, F. Skoviera, V. Koprda and L. Bohacik 727

154 Some results of preclinical and clinical evaluation of topicalpreparations containing glucan

K. Duckova, J. Kucera, L. Kuniak and J. Augustin 729

155 The treatment of Acne vulgaris by phosphatidylcholine-boundlinoleic acid

J. GareiB, M. Ghyczy and H.P. Nissen 731

156 Influence of the adhesive layer on the liberation rate of nitroglycerinfrom TDS matrices

K. Duckova, J. Kucera, D. Haddzimova and H. Hanzclova 732

157 A comparison between newly-developed and existing methods for

determining the in vitro drug release profile of 17-B-oestradiol from a

transdermal delivery systemA. Willi, E. Marti, G. Imanidis and H. Leuenberger 734

158 Influence of ethanol and propylene glycol on iontophoresis efficiencyA. Jadoul, D. Skrzypczak and V. Preat 736

159 Bandages with immobilized indomethacin, Preparation, toxicology,application

A.M. Tsatsakis, E. Kurumali, A. Katahanakis, V. Filatov,V. Riltsev, R. Virnik, M. Selala and M.I. Shtilman 738

160 The effects of elevated and ambient temperature dilutions of fluocinolone

acetonide ointment assessed using the human skin blanching assay

J.M. Haigh and E.W. Smith 740

161 Wound healing effectiveness of rHuGM-CSF from different topicalformulations

E. Memisoglu, F. Oner, I. Basaran and A.A. Hincal 742

28

Proceedings pagePharmacology, pharmacokinetics and biopharmacy

162 Synthesis, physical properties and toxicological studies of

L-pyroglutamic and L-glutamic acid esters of acetaminophen as

potentially useful prodrugsE. Bousquet, S. Tirendi, A. Spadaro, A. Marrazzo and G. Puglisi 883

163 Effect of 'Cerosel' preparation on rat organsF. Ryszka, B. Szulc and B. Dolinska 885

164 The influence of magnesium ascorbate on selected biochemical and

haematological blood indices in rats

F. Ryszka and B. Szulc 887

165 Gelisept, Medicinal gum jellyV. Tamas, D. Stavri and R. Dobos 889

166 Mistletoe extract-induced proliferation and cytokine release in cultures

of lymphocytes from untreated individuals in vitro

G. Stein and P.A. Berg 891

167 Estimation of the apparent volume of distribution of drug in plasmafor a process governed by Michaelis-Menten kinetics

G. Dimitriu, I. Popovici, R. Cuciureanu and G.N. Macovei 893

168 Disposition of quinidine and its distribution in plasma liproproteinsin human with hyperlipidemia

J. Masiakowski, M. Wierzchowiecki, E. Szymanskaand B. Michalowicz 895

169 Antihistaminic activity of flavonoid glycosides of Scutellaria

galericulata from RomaniaV. Stefan, M. Georgescu and N. Teoteoi 897

170 A study in non-patient volunteers to assess technology to achieve

colonic delivery of ibuprofenG.R. Howling, A.B. Jones, N. Washington and M.A. Hayward 899

171 Pharmacokinetics of tolfenamic acid in children after single oral dose

I. Niopas, M. Georgarakis, V. Cidi-Frangandrea,C. Chrisanthopoulos and E. Liara 901

172 Investigations on some pharmacokinetic properties of metronidazole

bound on polymeric supportE. Teslariu, M. Nechifor, V. Domeanu, A. Carpov, A. Spac,C. Filip and A. Negru 903

173 Dog pharmacokinetics of zidovudine and a zidovudine chemical

delivery systemM. Brewster, W. Anderson, E. Pop, N. Bodor and A. Webb 905

174 Glucagon-induced changes of adenylate cyclase activity in rat

reticulocytesM.R. Petronijevic and M.M. Kostic 907

29

Proceedings page175 Methyl iodide-induced neurotoxicity in primary neuronal culture,

A useful pharmacological test model

E. Lapis and E. K£rpati 909

176 Minoxidil and protein synthesis in isolated cardiac myocytesM. Strzalkowska 911

177 Some aspects of planning per os pharmaceutical preparationsP. Miskolczi, D. Greskovits, J. Greskovits, I. Klebovich

and A. David 913

178 Bioequivalence study of two tablet formulations of omeprazoleN.M. Najib, G.K. Pillai, M. Sheikh Salem, M.M. Hassan,F. Ghanem, E. Sallam, M.S. Shubair and S. Al-Delq 915

179 Bioavailability of ketotifen from a Pozitan® tablet and inhalation aerosolJ. Masiakowski, E. Szymanska and S. Dyderski 917

180 Bioavailability of clonidine as an oral pharmaceutical formI. Popovici, R. Cuciureanu, D. Lupuleasa, G. Dimitriu,A. Hriscu, L. Agoroaie and E.A. Popovici 919

181 HPLC analysis for the determination of miconazole in human plasmausing solid-phase extraction

M. Kobylinska, K. Kobylinska and B. Sobik 921

182 Pharmacokinetic study of orally-administered ketoconazole and its

multi-component complex on rabbitsA. Gerloczy, J. Szem&n, K. Csabai, M. Vikmon, J. Szejtli,P. Ventura and M. Pasini 923

183 The influence of dimensions on the gastric emptying of tablets infasted and fed volunteers

C.L. Mitchell, LM. Newton, D.F. Evans, M.B. Short and A. Bye 925

184 Evaluation of the correlation between in vitro and in vivo release ofsulfamethazine from a long-acting ovine bolus

B. Evrard and L. Delattre 927

185 Prolongation of drug absorption from hard gelatin capsules usingdifferent viscosity grades of sodium alginate as diluent

P. Veski, I. Lepist, H. Jurjenson and M. Marvola 929

186 Influence of cellulose ethers on the effect of local anaesthetic drug,Heptacaine

Z. Vitkova, K. Gardavska, J. Cizmarik and J. Rak 931

Emulsions and suspensions

187 Some physicochemical properties of micelle benzalkonium chloride

(BAC) adduct on phase limit in selected eye-dropsE. Zawadzka and M.M. Zgoda 645

188 Application of experimental methodology to emulsion formulationD. Notte, M.-F. Bobin and M.-C. Martini 647

30

ion r> i r xtProceedings page

189 Relevance of pH values to phospholipid stabilized fat emulsionsT.K. Bock and B.W. Muller 649

190 Effect of oil content on the properties of emulsions containingHPMCas polymeric emulsifier

S. Rimpler and R. Daniels 651

191 Emulsifying properties of Gelrite®/Veegum® combinationsM.U. Adikwu 653

192 Investigation of the emulsifying properties of Pemulen TR-1 ®, an

acryl acid alkyl methacrylate colpolymerM. Brisaert, H. De Broyer and J.A. Plaizier-Vercammen 654

193 The influence of water/oil phase ratio on the rheological behaviourof microemulsions

M. Primorac, M. Stupar, D. Vasiljevic and J. Milic-Askrabic 656

194 Rheological properties of a semisolid w/o emulsion system withsilicone emulsifiers

L Milic, G. Vuleta, D. Vasiljevic and M. Primorac 658

195 Analytical approach to determine the effect of azo dyes on the

physical stability of sterically stabilized o/w emulsionsB. Eckstein, J.E. Diederichs, J.J. Burger, E.A. Slootand R.G. Muller 660

196 Physical characterization and stability of microemulsions that

enhance intestinal uptakeA. Owen, A. Sarkahian, S. Sturgis, A. Tustian, P. Dentlingerand S. Yiv 662

197 Kinetics of oxidation of keratinic cystine in a w/o microemulsion

M.P. Savelli, C. Solans, P. Erra, G. Cave" and M. Clausse 664

198 Incorporation of the L-ascorbic acid and the N-acetyl L-cystein in

the inner aqueous phase of a w/o/w multiple emulsion,

Stability, characterization and ageing studies

N.S. Tokgoz, A.E. Fructus, P. Prognon, M. Seiller and

J.-L. Grossiord 666

199 In vivo evaluation of a new amphotericin B emulsion

E.S. Tabosa do Egito, M. Appel, H. Fessi, G. Barratt,F. Puisieux and J.-P. Devissaguet 668

200 In-line filtration of a parenteral emulsion using three filters,

Comparison and assessment

M. Faber, G. Mortha, L. Foroni, C. Jeannin and J. Calop 670

201 The influence of hormone/metal gram/molar relationship on selected

properties of peptide/GnRH analogue suspensionsB. Dolinska and F. Ryszka 672

202 Formulation of some nematocides as suspensionsY. Yazan, I. Isikdag and U. Ucucu 674

31

Proceedings pageStability

203 Stability of sulphadimidine in veterinary pharmaceutical specialitiesJ. Bernabeu, M.E. Gil, V. Ruz, O. Pedaez and A.L Torres 941

204 Photo-instability and degradation kinetics of medazepamY. Topaloglu and G. Yener 943

205 Kinetic study of Romener® in aqueous solution, using third-

derivative ultraviolet spectrometryM. Surmeian, G. Ciohodaru and S. Cilianu 945

206 Possibilities for the application of regression analysis and analysisof variance, (2) Stability determination of pharmaceuticalpreparations, Diclofenac sodium injections

M.B. Arambasic and D. Majkic 947

207 Study of the influence of auxiliary substances on the stability of

new anti-arrhythmic drugH+BZ. Vitkovd, K. Gardavska\ J. Cizmarik and J. Rak 949

208 Influence of metal ions, chelator and anti-oxidants on tiagabinestability in solutions

H. Weibel and H.M. Nielsen 951

209 Stability of ranitidine hydrochloride in aqueous solutionsM.K. Youssef, LA. Attia, S. El Gizawy, M.A. Foudaand G. El Maghraby 953

210 Purity and stability assessment of a semi-solid poly(ortho ester)used in drug delivery systems

M. Zignani, A. Merkli, J. Heller, C. Tabatabay and R. Gurny 955

211 Investigation of the'

anti-oxygen' action of acexamic acid on vegetal oils

R. Cuciureanu, I. Dumistracel, I. Popovici and G. Dimitriu 957

Sterilization and aseptic products

212 Stability of gamma-irradiated diltiazem

E. Ciranni Signoretti, L. Valvo, S. Alimonti and C. Lucia 961

213 Developments in pharmaceutical closure technologyW. Van de Poel 963

214 Validation of filter sterilization in autoclaves

J. Voorspoels, J.P. Remon and G. Vandenbossche 965

215 New clean area designed for the manufacturing of asepticpharmaceuticals integrated into an existing R&D facility

R. Anders 967

216 Viresolve, a membrane-based system for the removal of viral

contaminants from biopharmaceuticalsM. Kalyanpur 968

217 Applications, controlling and open questions in sterile filtrationG. Stampf 970

32

. Proceedings page218 Drug delivery systems, Pre-fillable disposable syringesH. Worder 972

Lyophilization (freeze-drying)

219 The use of maltodextrins as lyoprotectants in the lyophilizationof a model protein, LDH

S. Corveleyn and LP. Remon 983

220 Dependence of quality of freeze-dried diazepam/mannitol on some

manufacturing conditionsK.-H. Fromming, M. Bergmann and W. Mehnert 985

Synthesis and analysis

221 Synthesis of new l-l3-(4-phenylpiperazinyl-l)propyll-imidazolidone derivatives

T. Kulinski and T. Tkaczynski 103

222 Synthesis of new l-aryl-2-imino-3-arylsulfonyl-imidazolidinederivatives

M. Rzadkowska and T. Tkaczynski 105

223 Synthesis of new derivatives of 3,8-diphenyl-7,8-di-hydro-6H-imidazo[2,1 -cj-1,2,4-triazin-4-one

K. Sztanke and T. Tkaczynski 107

224 Synthesis and some selected properties of new polyethylenepolyamine/epichlorohydrin copolymers

M.M. Zgoda, K. Rogiewicz and R. Glinka 109

225 Preformulation study of naltrexone, Analytical and thermalcharacterization

J. Alvarez-Fuentes, I. Caraballo, A. Boza, M.A. Holgado andM. Fernandez-Arevalo 111

226 Binding of amino acids and peptides to cyclodextrins, A comparativeelectrospray ionization mass spectrometric and molecular modellingstudy

L. Prokai and R. Ramanathan 113

227 TLC study of nimodipine and degradation productsLL. Lastres, E.M. Garcia, M.P. Ballesteros and P. Frutos 115

228 Ginger extracts, Characterization by analytical determination of

their compositionC. Mattern, P. Eichler, F. Gaedcke and R. Hacker 117

229 A colorimetric method for the assay of pyrimethamine and its dosageforms by charge transfer complexation with chloranilic acid

M/U.Adikwu 119

230 A colorimetric method for the assay of quinine in pharmaceuticalformulations using chloranilic acid as the titrant in non-aqueous medium

M.U. Adikwu 120

33

Proceedings page231 Capillary electrophoresis for the chiral separation of salbutamol

A. Esquisabel, P.F. Goyenaga, A. San Vicente, M.B. Calvo

and J.L. Pedraz 121

232 Rapid spectrophotometric determination of aluminium using colour

complex formation with eriochrome cyanineC. Amezcua, A. Ganem and D. Quintanar 123

Miscellaneous

233 Recent developments in compendial dissolution standards

B.B. Hubert and L.T. Grady 989

234 Mathematical statistical revision of 'uniformity of mass requirementsof single-dose preparations' of different Pharmacopoeias

T.A. Nagy 990

235 Determination of free iodine as a function of dilution in two

different povidone/iodine formulations

D.A. Marroyen, G.R. Bultinck, LM. Haenen and

J.A. Plaizier-Vercammen 992

236 Consequences of the presence of pesticides in medicinal plantsM. Voitcu, V. Nastase, R. Cuciureanu and M. Leanca 994

237 The influence of some excipients on the characteristics of herbal troches

D. Sekulovic, V. Sekesan andL. Tasic 996

238 Isolation, purification and characteruzation of an extracellular

endoglucanase of Aspergillus ochraceusG. Dediu, F. Israel-Roming, M. Milescu and C.G. Tanase 998

239 Aesthetics in scienceK. Lancos, M. Balint and I. Peter 1000

34


Room A

09.15 h Maurice-Marie Janot Lecture, Daan J.A. Crommelin, Universiteit UtrechtInternational Jury President: Professor Trevor M. Jones

10.00 h Break

Room A

Solid oral dosage formsChairmen, Marco Fabrizio Saettone and Klaus-Jiirgen Steffens

Proceedings page

10.20 h Effect of moisture on tensile strength of tablets based on

microcrystalline cellulose and polyvinyl pyrrolidoneL. Stubberud, H.G. Arwidsson and C. Graffner 161

10.40 h Compaction data bank, (1) Batch-to-batch, plant-to-plant, and

manufacture-to-manufacture consistency of microcrystalline cellulose

and dicalcium phosphateM. Celik and E. Okutgen 163

11.00 h The effect of compaction speed on capping of tablets compressed from

viscoelastic pharmaceutical materials, A quantitative approachK. Van der Voort Maarschalk, H. Vromans, G.K. Bolhuis

and C.F. Lerk 165

11.20h Break

Solid oral dosage formsChairmen, John E. Rees and Metin Celik

11.30 h Investigations into the moisture barrier properties of polyvinylalcohol(PVA) tablet film coatings

M.P. Jordan, M.G. Easterbrook and LE. Hogan 167

11.30 h Comparative study on xanthan gum and hydroxypropyl methylcellulose(HPMC) for sustained release formulation

M.M. Talukdar and R. Kinget 169

12.10 h A novel technique to study the physical properties of beads and film-

coated soft gelatin capsulesL. Felton, C. Wang, G. Zhang, N.H. Shah, M.H. Infeld,A.W. Malick and LW. McGinity 171

12.30 h Lunch break

Solid oral dosage formsChairmen, Renaat Kinget and Gyorgy Stampf

15.00 h The effects of viscosity grade of sodium carboxy methylcelluloseon drug release from matrix tablets 173

15.20 h In vivo performance of quick/slow Geomatrix® technologyL. Maggi, S. Morgenthaler, R. Zimmer, T. Shepard and U. Conte 175

35

Proceedings page15.40 h Polymer particle erosion, A new release mechanism of

hydrocolloid embeddingsB.C. Lippold and W.D. Lindner 177

16.00 h Bioavailability of testosterone using a bioadhesive tablet with

penetration enhancers in dogsJ. Voorspoels, W. De Sy and J.P. Remon 179

16.20 Break

Pulmonary deliveryChairmen, Robert Gurny and Gyorgy Szasz

16.35 h Particle size determination of metered dose inhalers by laser

diffraction, cascade impaction and liquid impingementP.M. Holzner and B.W. Muller 765

16.55 h Effect of drug/carrier ratio on the mixing and dispersion of drypowder inhalations of nedocromil sodium

D.Y.T. Wong, P. Wright and M.E. Aulton 767

17.15 h Delivery performances of three dry powder inhalers

G. Ponchel and A. Blattmann 769


RoomB

NanoparticlesChairmen, Francis Puisieux and J6rg Kreuter

10.20 h Drug incorporation and delivery of prednisolone-loaded solid

lipid nanoparticlesA. zur Muhlen and W. Mehnert 455

10.40 h Comparison of tripalmitate nanoparticles prepared by melt

homogenization and solvent emulsificationB. Siekmann and K. Westesen 457

11.00 h Recrystallization tendency and polymorphic transitions in

triglyceride nanoparticlesH. Bunjes, K. Westesen and M.H.J. Koch 459

11.20 Break

NanoparticlesChairmen, Patrick Couvreur and A. Atilla Hincal

11.30 h Encapsulation of oligonucleotides in Stealth Me.PEG-PLA50

nanoparticles by complexation with structured oligopeptidesC. Emile, D. Bazile, F. Herman, C. Helene and M. Veillard 461

11.50 h Potential of solid lipid nanoparticles (SLN) for controlled drug deliveryR.H. Muller and W. Mehnert 463

36

Proceedings page

12.10 h Influence of different physicochemical conditions on the release of

indium oxine from nanocapsulesP. Maincent, F. Kedzierewicz, P. Thouvenot, I. Monot and

M. Hoffman 465

12.30 Lunch break

NanoparticlesChairmen, Michel Veillard and Kirsten Westesen

15.00 h Microparticulate drug carriers, Control of biodistribution by surface

modification with hydrophilic polymersV.P. Torchilin and V.S. Trubetskoy 467

15.20 h Polymethacrylic delivery system with NSAID propertiesP.A. Liso, M. Rebuelta, L San Roman, A. Gallardo and A.M. Villar 469

15.40 h Modification of the body distribution of polymethacrylate nanoparticlesby coating with different concentrations of non-ionic surfactants

J. Kreuter and L. Araujo 471

16.00 h Mechanism of action of polyalkylcyanoacrylate doxorubicin-loaded

nanoparticles in the reversion of resistance of P388/ADR

C. Dubernet, F. Nemati, A. Colin de Verdiere, M.-F. Poupon,F. Puisieux and P. Couvreur 473

16.20 h Break

ProdrugsChairmen, Vladimir P. Torchilin and Michael E. Aulton

16.35 h Water-soluble prodrugs and congeners of dexanabinol

E. Pop, M.E. Brewster, Z.Z. Liu, F. Soti, S. Rachwal, A. Dinculescu,

V. Nadler, Y. Barenholz, R. Mechoulam and A. Biegon 127

16.55 h Supramolecular organization and thermal analysis of a prodrug of

timolol, Palmitoyl timolol malonate

B. Pech, Y. Bouligand, J.-E. Proust and J.-P. Benoit 129

17.15 h Biocatalysed N-terminal deprotection of a dipeptide ester

I. Lupescu, D.M. Petrea and G. Radulescu 131


RoomC

Lyophilization (freeze-drying)Chairmen, Patrick P. DeLuca and Szabolcs Nyiredy

10.20 h Use of statistical experimental design in optimizinginterleukin-2 (RU 49637) freeze-drying

J.-J. Le Fur, B. Voncken, M. Eyraud, N. Gayraud,B. Maneglier and P. Becourt 977

10.40 h Crystal ice size as a critical parameter in freezing of a dispersed system

Y. Bensouda and A. Laatiris 979

37

Proceedings page

11.00 h Freeze-drying plants with modern refrigerants including liquid nitrogenH. Willemer 981

11.20 h Break

StabilityChairmen, Karl-Heinz FrQmming and Svetla Bogdanova

11.30 h Investigation on the chemical stability of erythromycin in lotions

using an optimization systemM. Brisaert, M. Heylen and LA. Plaizier-Vercammen 935

11.50 h Optimization of TLC methods for densitometric determination and

separation of artemisin, arteether and artemether and their isomers

M. Gabriels and LA. Plaizier-Vercammen 937

12.10 h Stability of co-trimoxazole preparations for injectablesF. Giordano, G.P. Bettinetti, A. Gazzaniga, R. Cursano,M. Rillosi and A. La Manna 939

12.30 h Lunch break

Pharmacology, pharmacokinetics and biopharmacyChairmen, Emil Pop and Meir Bialer

15.00 Comparative studies on cellular effects of insulin and vanadate on

cultivated rat hepatocytesR. Albulescu, M. Albulescu, M. Apetroae and D. Gruita 869

15.20 h Effects of aminophylline on ADP-induced biphasic humanplatelet aggregation

M.M. Kostic, M.R. Petronijevic, D.L. Brkovic, M. Avramovic,A. Stajn and R.V. Zikic 871

15.40 h Synergisms between lectins and vesicles of Viscum album L.,(2) Direct cytotoxic effects

R. Scheer, H.H. Fiebig and A. Scheffler 873

16.00 h Some biopharmaceutical aspects of benzyl-iso-quinoline derivatives

S. Marton, P. Szentmiklosi and I. Ricz 875

16.20 Break

Pharmacology, pharmacokinetics and biopharmacyChairmen, Clive G. Wilson and Sylvia Marton

16.35 h Determination of transport rates for ISDN, theophylline and

propranolol across the rabbit colon epitheliumM.A. Rosic, M. Nesic, N. Cvetkovic and G.L. Rosic 877

16.55 h Least-squares deconvolution results in improved estimation ofthe mean input time as a measure of bioavailability

M. Bagli, R. Stiverkriip, M.L. Rao and H. Bode 879

17.15 h Criteria to assess in vivo performance of sustained release products,Application to diltiazem sustained release formulations

M. Bialer 881

38


Posters

Exhibited continuously from 10.00 to 16.35, with special session from 14.00 to 15.00 h.The number indicates the number displayed on the poster panel.

Microspheres

240 Stability evaluation of PDLLA microspheres loaded with

anti-inflammatory drugF. Castelli, B. Conti, M. Fresta, U. Conte and G. Puglisi 407

241 Influence of the preparation method on residual solvents in

biodegradable microspheresC. Bitz and E. Doelker 409

242 Preparation and in vitro release of thymopentin PLGA microspheresB. Conti, A.M. Panico, C.A. Ventura, P. Giunchedi,V. Cardile and G. Puglisi 411

243 In vitro and in vivo evaluation of nifedipine-loaded PLGA microspheresP. Sansdrap, J. Fontaine and A.J. Moes 413

244 Biodegradable PLGA implants for in vivo sustained delivery of

carboplatin and etoposide to the brainT.L. Whateley, P.A. Fallon, L. Robertson and R. Rampling 415

245 New system for the microencapsulation of water-soluble drugsM.-A. Asin, E. Ferret, P. Tarin, R. Arola and A. Perez 417

246 Analysis of microspheres of poly(lactic/glycoiic acid) containingsalcatonin

P. Tarin, R. Arola, M.-A. Asm, E. Ferret and A. Perez 419

247 In vitro ciprofloxacin release from poly(lactide-co-glycolide)microspheres

M.C. Nacucchio, M. Pena, F. Lairion, P. Di Rocco and B. Martinez 421

248 Factors influencing the release of albumin from biodegradablemicroparticulate systems

LL. Pedraz, M. Igartua, A.G. Goicoechea and R.M, Hernandez 423

249 In vitro evaluation of albumin-loaded poly(D,L-lactide-c<?-glycolide)microspheres

M. Igartua, A. Esquisabel, R.M. Hernandez, A.R. Gascon,A.G. Goicoechea and LL. Pedraz 425

250 NSAJD-loaded polylactic acid microspheres, Preparation andin vitro characterization

D.J. Armstrong, P.N.C. Elliott, J.L. Ford, B. Guiziou,G.P. McCarthy and C. Rostron 427

251 Spray-dried biodegradable microparticles containing antigen as

oral vaccineM.-A. Benoit, B. Baras and J. Gillard 429

39

Proceedings page252 Potential of polyester microparticles for the sustained release of

oral vaccine

M.-A. Benoit, B.C. Youan and J. Gillard 431

253 In vitro/in vivo evaluation of diclofenac sodium/alginate beads

containing aqueous polymer dispersionsA. Giirsoy, M. Tiirkoglu, L. Eroglu, S. Aygin and I. Okar 433

254 Gelatin microspheres as carriers for anticancer drug doxorubicin,In vitro studies

M. Achim and S.E. Leucuta 435

255 Preparation of Eudragit RS 100 microspheres in different pH media,

(1) Morphology, surface and internal microsphere structure

M.K. Youssef, W. Korsatko, I. Attia, V. Ribitsch and O.Y. Mady 437

256 Eudragit microparticles prepared by spray-drying, Effect of

microparticle structure on diltiazem release

T. Kristmundsdottir, O.S. Gudmundsson and K. Ingvarsdottir 439

257 Liquid controlled-release formulations of microencapsulatedterbutalene/resin complexes

D. Torres, M. Curia, L. Boado and LL. Vila Jato 441

258 The effect of viscosity on the micromeritic properties of ethylcellulose-walled theophylline microspheres

G. Zessin and A. Dashevsky 443

259 An improved solvent evaporation method for manufacturingethylcellulose microspheres using phospholipids, Influence of

experimental parameters on particle size and release rate profilesG. Evers and T. Kissel 445

260 Investigation of residual methylene chloride in microparticlesproduced by means of the ASES process

F. Ruchatz, J. Thies and B.W. Muller 447

261 Hyaluronidase injectable microparticles for extravasation and

extravasation injury treatment

T. Modena, F. Pavanetto, I. Genta, M.E. Tira, P. Sini,B. Conti and A. Gazzaniga 449

262 Microencapsulated thiophosphonic acid ester (TPE), A new, highlyeffective insecticide formulation with a low environmental impact

S. Schult, R. L6hr and K. Mrusek 451

Pellets

263 Production of microgranules for multiparticulate dosage forms

O. W0rts 359

264 Influence of the nature of the excipients on the feasibility and the

release characteristics of granules made by a thermoplasticpelletization method

C. Peerboom and L. Delattre 361

40

Proceedings page265 Process study and optimization of pellet manufacture by rotary

granulationP. Delmas, F. Andre, G.A. Lewis, L Montel and D. Wouessidjewe 363

266 Influence of the impeller design, the method of screen perforation and the

perforation geometry on pellet quality made by extrusion/spheronizationC. Vervaet and LP. Remon 365

267 Properties of extruded pellets made from binary mixturesL. Nymo, M. Schroder, P. Schultz, B.W. Muller, T. Waalerand P. Kleinebudde 367

268 Preparation of neutral and ketoprofen pellets byextrusion/spheronization technology

J. Sirca, J. Kerc, S. Srcic and B. Kofler 369

269 Evaluation of beta-cyclodextrin as a pelletization agentA. Gazzaniga, M.E. Sangalli, M. Rillosi, G. Bruni, C. Vecchio

and F. Giordano 371

270 Effect of water solubility of drugs on the extrasio/spheronization processJ.A.C. Elbers, L.H.J. Bouwman and E.M.G. van Bommel 373

271 Comparison of two extruders by means of experimental designsE. Le Doeuff, M. Vanhoeve, A.T. Gayot and P. Becourt 375

272 Spherical preparations of bead cellulose, polyethylene glycol and

griseofulvin for controlled releaseB. Wolf, I. Finke and W. Schmitz 377

273 Beads of cross-linked carboxymethylcellulose, Effect of the viscositygrade and concentration of the polymer

V. Iannuccelli, G. Coppi and R. Cameroni 379

274 Coating of pellets, Comparison between aqueous dispersion andalcoholic solution of ethylcellulose

C. Mathieu, B. Huet de Barochez and A. Cuine 381

275 The effect of dispersion concentration and curing temperature on drugrelease of pellets coated with Eudragit NE 30 D

T.C. Wagner and S. Keitel 383

276 Influence of the pellet coating on drug release from ketoprofenslow-release capsules

M. Dittgen, A. Bauer, C. Timpe and H. Osterwald 385

Controlled release

277 Development of fluid compositions for the critical test of dissolution

sensitivity of oral extended release systemsR. Aloul, K. Gjellan, M. Sjolund, M. Sarkela and C. Graffner 299

278 Diffusion coefficients of ketoprofen sodium in ternary systems with

hydroxypropylcelluloseG.E. Hildebrand and C.C. Muller-Goymann 301

41

Proceedings page

279 Effective surface in inert matrix systems, Reactive dimension

M.J. Fernandez-Hervas, M.T. Vela, M.J. Arias and A.M. Rabasco 303

280 Control of the erosion rate of semi-solid poly(ortho ester), Case studyof 5-fluorouracil and mitomycin C

M.B. Sintzel, A. Merkli, J. Heller, C. Tabatabay and R. Gurny 305

281 Equilibrium swelling behaviour of pH-sensitive anionic vinylalcohol copolymers

N.M. Ranjha and E. Doelker 307

282 Non-ionizable, pH-sensitive hydrogels for controlled release, Swellingbehaviour of poly(ethoxy-triethyleneglycol monomethacrylate) films

B. Vasquez, I. Goni, M. Gurruchaga and J. San Roman 309

283 Release study of acebutolol immobilized on y-irradiated PEO-based

hydrogelsN. Lambov, S. Tsankov and E. Minkov 311

284 Preparation and characterization of hydrogel delivery system,

Application to gentamicin and methotrexate

C. Bregni, E. Beyssac, S. Aiache and L-M. Aiache 313

285 Hydrogel implant controlled delivery system for methotrexate

obtained by ionized radiation

E. Beyssac, C. Bregni and J.-M. Aiache 315

286 Floating minitablets for the sustained release of low-solubility drugsN. Rouge, P. Buri, E. Doelker and E.T. Cole 317

287 Polysaccharides and controlled drug release, Gellan for the

formulation of gel capsulesE. Murtas, M. Carafa, T. Coviello and F. Alhaique 319

288 Simultaneous in vitro controlled release of levodopa and carbidopa from

biocompatible polymeric core-in-cup implantsM.P. Danckwerts and J.G. van der Watt 321

289 Use of methyl polymethacrylate (PMMA) as a drug supportS. El Meski, E. Beyssac and J.-M. Aiache 323

290 Preparation of gelatin sponges as sustained release drug carriers

K. Oungbho and B.W. Muller 325

291 Chitosan cross-linked films as vehicles for controlled drug deliveryC. Remunan-Lopez, M.J. Alonso and R. Bodmeier 327

292 In vitro bacterial degradability of inulinHP incorporated in

Eudragit RS films

L. Vervoort and R. Kinget 329

293 Development of a new controlled-release dosage form, Influence of

coating thickness and gamma sterilization on release kinetics

J.-M. Aiache, S. El Meski, E. Beyssac and G. Serpin 331

42

Proceedings page294 pH- and vehicle-dependence of salbutamol release rate through

a polypropylene control membrane

R. Imboden, G. Imanidis and H. Leuenberger 333

295 Proposal of antimoulding delivery device for the stability improvementof cosmetic formulations

A. Gazzaniga, M.E. Sangalli, F. Giordano, U. Conte,A. Semenzato and A. Bettero 335

296 Evaluation of the release of drug from medicated chewing-gumL. Gyldenvang and M.R. Rassing 337

Bioadhesion

297 Use of scintigraphy to measure bioadhesion in an isolated porcineperitoneal sheet model

Y.P. Zhu, C.G. Wilson, I. Hayter and LD. Smart 825

298 Interaction analyses between purified vaginal mucus and Carbopol 934Pby differential scanning calorimetry and scanning electron microscope

S. Galindo, D. Quintanar and E. Aguilera 827

299 Bioadhesive polymers as platforms for oral Barrett's oesophagustreatment, Formulation and evaluation of various water-solublebioadhesive polymers

P. Iooss, A. Gouyette, A.M. Le Ray, T. Patrice and C. Merle 829

300 Bioadhesive tablets of sodium diclofenacA. Popovici and E. Petrescu 831

301 Aminophylline bioadhesive tablets obtained by wet granulationC. Prudat, P. Arnaud and L-C. Chaumeil 833

302 Effect of technological variables on swelling behaviour of

gelatin/poly(acrylic acid) microspheresS .E. Leucuta, G. Ponchel and D. Duchene 835

303 Influence of a number of technological variables on the propertiesof bioadhesive microspheres loaded with oxprenolol

M. Preda and S.E. Leucuta 837

304 A novel mucoadhesive buccal drug delivery systemS. Burgalassi, L. Panichi, M.F. Saettone, J. Jacobsenand M.R. Rassing 839

Physicochemistry

305 Reorganization of collagen in the presence of structured (activated) waters

I. Manzatu, V. Trandafir and R. Christof 26

306 Interaction of perfloxacin and ciprofloxacin with antacids

Z. Kokot, H. Bojarowicz, B. Kupcewicz and I. Prawdzik 28

307 Relative lipophilicities of some 1,4-dihydropyridine calcium antagonistsS. Srcic, J. Kerc, M. Pukl, V. Kmetec and O. Planinsek 30

43

Proceedings page

308 Dissolution behaviour of sulphonamides into sodium dodecyl sulphatemicelles, A thermodynamic approach

S. Mall, G. Buckton and D.A. Rawlins 32

309 Comprehensive computer-assisted calculations for pKa, logP and logDvalues of drugs, and their applications to pharmaceutics

A. Papp, F. Csizmadia, F. Darvas and A. DaVid 34

310 Hydration of drug molecules, Cavity inclusion of water in crystals of

loperamide hydrochloride tetrahydrateJ.J. Gerber, M.R. Caira and A.P. Lotter 36

311 Crystal engineering, Solvent effects on glibenclamide crystalsproduced with different crystallization rates

D. Cordes and B.W. Muller 38

312 Phase changes of theophylline crystal forms under different moisture

conditions

U.J. Griesser and A. Burger 40

313 Polymorphism of paracetamolP. Di Martino, A.-M. Guyot-Hermann, P. Conflant, M. Drache,J.-P. Beaufays, J.-P. Huvenne and J.-C. Guyot 42

314 Comparison of physicochemical properties of the polymorphicmodifications and pseudopolymorphic forms of non-steroidal

anti-inflammatory drug substances

A. Burger and J.-O. Henck 44

315 On the solubility of polymorphic modifications of the racemates,

Enantiomers of some 2-arylpropionic acids

A. Burger and K.T. Koller 46

316 Investigations on the melting behaviour, thermotropic mesomorphismand solubility of fenoprofen calcium

T. Rades, Y. Padmadisastra and C.C. Muller-Goymann 48

317 Preparation and characterization of a very stable crystal modification

of H2 antagonist cimetidine

A. Bauer-Brandl 50

318 Determination of thermal properties and film formation characteristics

of different acrylic aqueous dispersions used for film coatingK. Arnighi and A.J. Moes 52

319 Preformulation aspects of hirudin, pH-dependent coprecipitationof hirudin and zinc

U. Gietz, T. Arvinte and H.P. Merkle 54

320 Phase diagram of the carbamazepine/PEG 6000 system and dissolution

rates of eutectic mixture samplesN. Zerrouk, S. Toscani, J. Dugue, R. Ceolin and C. Chemtob 56

321 Preparation, characterization and dissolution performance of

flunnarizine from solid dispersions with PEG 6000

LM. Gines, M.J. Arias, LI. Perez-Martinez, LR. Moyano,M.J. Perez-Barrales, M.D. Veiga, M.T. Faucci and A.M. Rabasco 58

44

Proceedings page322 Solid dispersion systems with nifedipine

S. Michailova, I. Nikolov, A. Pavlova and P. Kazanjieva 60

323 Drug/polymer interactions in coprecipitates with controlled releaseof verapamil hydrochloride

K. Goracinova, A. Simov, L. Klisarova, E. Fredro-Kumbaradzi

and L. Petrusevska-Tozi 62

324 Drug/excipient interaction study of 6-lactame antibiotic usingdifferent techniques

M.A. Hassan, J. Kaloustian, H. Ransis, K.A. Khaled,T.H. El-Faham, S. Shawky-Tous and J. Joachim 64

325 Compatibility study of amonafide hydrochloride with hydrophobicexcipients

M.M. Obregon, M.E. Gil, V. Ruz, J. Bernabeu and M.A. Camacho 66

326 Use of micro DSC III (Setaram) in the study of drug/excipientcompatibility

M. Balint, E. Gondar, I. Peter and S. Sebesi-Siito 68

327 Thermal analysis in pharmaceutical systems using oscillatingdifferential scanning calorimetry (ODSC)

M. Wulff and M. Alden 70

328 Characterization of water uptake by hydrocolloids usingdifferential scanning calorimetry

G. Bhaskar, LL. Ford and D.A. Hollingsbee 72

329 The use of isothermal microcalorimetry in the study of the amorphouscontent of a hydrophobic powder

H. Ahmed, G. Buckton and D. Rawlins 74

330 DSC study of the phase behaviour of an aqueous dextran/mannitol system

during the freezing step of the freeze-drying processJ. Bamba, P. Tchoreloff, G. Cave, F. Puisieux and G. Couarraze 76

331 HLB determination method, Comparison applied to a range of

3-Z-R-1,2-O-isopropylidene-a-D-glucofuranose derivatives

R. Bikanga, P. Gode, D. Postel, G. Ronco, G.-N. Cave,M. Seiller and P. Villa 78

332 Use of the elastic modulus to determine phase transitions of Lutrol F127

gels, Influence of molecular weight and volume fraction of PEG and

PPG on phase transition temperaturesM.E. Voeffray, LM. Mayer and J.-C. Etter 80

333 New gelification method for vegetal oils and rheological study of

oleogels as a function of temperatureP. Gauthier, S. Aiache, E. Beyssac and J.-M. Aiache 82

334 Comparative rheological study of aqueous preparations based on

thickening or gelling agentsC. Montaulieu, P. Michaud, M. Sengelin, E. Leverd and

J. Bougaret 84

45

Proceedings page335 Rheological properties of drug/phospholipid monolayers

A. Doisy, J.-E. Proust, J.C. Chauvin and J.-L. Dubois 86

336 Evaluation of mucin viscoelastic behaviour

J. Kocevar-Nared, J. Kristl and J. Smid-Korbar 88

337 A novel method of dissolution curve processingP. Kaclfk, T. Fazekas, M. Vitkova" and M. Chalabala 90

338 Testing the applicability of the cube root law to the dissolution of

ibuprofen using a particle counterL. Pereira de Almeida, S. Simoes, A. Sousa and M. Figueiredo 92

339 The effect of particle size and shape on the surface specificdissolution rate of suspended, practically insoluble drugs

M. Mosharraf and C. Nystrom 94

340 Influence of particle size variation of a poorly water-soluble

compound on the dissolution behaviour of tablets

A. Bausch, C. Qiao and R. Alex 96

341 Structure/property relationship in the case of PLGA 50/50 copolymersG. Reich 98

Cyclodextrins

342 Microwave drying of a-cyclodextrinG.P. Bettinetti, F. Giordano, M. Rillosi and P. Mura 591

343 Effects of hydrotropic agents on the formation of indomethacin/

B-cyclodextrin inclusion compoundsE. Pioger, D. Wouessidjewe, D. Duchene and S. Bogdanova 593

344 Phase solubility and 13C NMR analysis of the interaction of ketoprofenand ibuprofen with B-cyclodextrins

P. Mura, A. Manderioli, G.P. Bettinetti and G. Bramanti 595

345 Interactions of sulindac with B- and y-cyclodextrinsM.A. Peiia, C. Tros de Ylarduya, C. Martinez-Oharriz,M.M. Goni, C. Martin and M. Sanchez 597

346 Fluorescence study of naproxen/8-cyclodextrin interaction in solution

M. Sanchez, I. Velaz, C. Martin and M.C. Martinez-Oharriz 599

347 Structural characterization of glibenclamide sodium salt inclusion

complex with B-cyclodextrinE. Redenti, M. Pasini, L. Carima, M. Zanol, A. Bacchi,M. Vikmon, J. Szejtli and P. Ventura 601

348 Study of salbutamol/B-cyclodextrin and ethylated B-cyclodextrincomplexes, Determination of stability constant by capillaryelectrophoresis

V. Lemesle-Lamache, M. Taverna, D. Ferrier, D. Duchene

and D. Wouessidjewe 603

46

Proceedings page349 Complexation of the bacteriostat, triclosan, with 7-cyclodextrin

P.M. Ashall, B.M. Kieman and N.R. Russell 605

350 Interaction of triamterene with hydroxypropyl B-cyclodextrin in

ground mixtures, Improvement in the dissolution propertiesM.J. Arias, LM. Gin6s, J.R. Moyano, P.J. Sanchez-Soto,A. Ruiz-Conde, C. Novak and A.M. Rabasco 607

351 Preparation and evaluation of indomethacin/cyclodextrininclusion complexes

D. Lupuleasa, M. Pana, S. Sever, D. Neagu and P. Cracium 609

352 Study of the inclusion complexation of glisentide with B-cyclodextrinJ.R. Moyano, LM. Gines, M.L Arias, LI. Perez-martinez,M.J. Perez-Barrales, M.J. Fernandez-Hervas and A.M. Rabasco 611

353 Inclusion compound of acetazolamide with different cyclodextrinsin liquid and solid state

M.J. P6rez-Barrales, F. Diaz-Estevez, LM. Gines, J.R. Moyano,M.J. Arias and A.M. Rabasco 613

354 Investigation on 2,4-D/DIMEB complexation in aqueous solution

and solid state

LL Perez-Martinez, LM. Gines, M.J. Arias, P.J. Sanchez-Soto,A. Ruiz-Conde, E. Morillo and C. Novak 615

355 Increasing the solubility characteristics of fenofibrate with cyclodextrinZ. Aigner, I. Bencz and M. Kata 617

356 Increasing the solubility and photostability of nifedipine with cyclodextrinsA. Gyeresi, B. Tok6s, G. Regdon and M. Kata 619

357 The influence of 6-cyclodextrin on solubility, stability and inclusion

complexation of a new non-acidic non-steroidal anti-inflammatorydrug (NSA1D) in aqueous solutions

A.M. Le Ray, P. Richomme, J.M.H. Robert and C. Merle 621

358 Improvement in the dissolution properties of ketoconazole throughcomplexation with B- and 2-hydroxypropyl B-cyclodextrin

M.T. Esclusa-Diaz, M. Guimaraens-M6ndez, M. Gayo-Otero,M.B. Perez-Marcos, J.L. Vila Jato and J.J. Torres-Labandeira 623

359 Dissolution studies of mequitazine in several dissolution media

with sodium lauryl sulphate, Tween 20 and B-cyclodextrinM.D. Veiga and F. Ahsan 625

360 Improved oral bioavailability of carbamazepine through the use of

chemically-modified cyclodextrinsM. Brewster, W. Anderson, E. Pop, R. Sawchuk, B. Cheungand A. Webb 627

361 The influence of the method for the preparation of essential oil/

B-cyclodextrin complexes on the stability of selected oil componentsL. Tasic, V. Sekesan, D. Sekulovic and M. Ristic 629

47

Proceedings page362 Photochemical stability of the inclusion complexes formed by

1,4-dihydropyridine derivatives with B-cyclodextrinJ. Mielcarek and J. Pawlaczyk 631

363 A DSC study on the interaction of natural and modified B-cyclodextrinswith liposomes

C.A. Ventura, M. fresta and G. Puglisi 633

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'World Meeting on Pharmaceutics, Biopharmaceutics ... · Scientific programme M Tuesday,9May1995...

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Transcript of 'World Meeting on Pharmaceutics, Biopharmaceutics ... · Scientific programme M Tuesday,9May1995...