TRANSMUCOSAL DRUG DELIVERY Using the Mucofilm … · TRANSMUCOSAL DRUG DELIVERY Drug Delivery and...

TRANSMUCOSAL DRUG DELIVERYUsing the Mucofilm® technology to bypass the first pass effect

Drug Delivery and Formulation Summit 2019, March 11 – 13, Berlin

WHO IS tesa Labtec GmbH?

COMPANY AFFILIATION

March 13th, 2019Drug Delivery and Formulation Summit Berlin 2019 - 3 -

tesa is a part of the Beiersdorf Group of Companies

tesa SE is a member of the Beiersdorf Group,

manufacturer of successful international cosmetic brands

including NIVEA, Eucerin, and la prairie

OUR TECHNOLOGIES

• Rapidfilm® Fast dissolving oral dispersible films - No swallowing- No water required- Perfect for children and the elderly

• Transfilm® Transdermal and topical patches

- No first pass effect- Less side effects- Less metabolites

• Mucofilm® Buccal and sublingual films - Fast onset of action- Ease of use- No first pass effect

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Innovative dosage forms

Drug Delivery and Formulation Summit Berlin 2019 March 13th, 2019

ORAL FILMS (RAPIDFILM® AND MUCOFILM®)

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RapidFilm®

Orodispersible film (Ph.Eur., EMA) Soluble film (FDA):

Oral film, thin strip, flash-release wafer, quick-dissolve film, orally dissolving film, rapidly dissolving film

Typical components of our Rapidfilm®

Drug Delivery and Formulation Summit Berlin 2019 March 13th, 2019

TRANSMUCOSAL DRUG DELIVERY

March 13th, 2019Drug Delivery and Formulation Summit Berlin 2019

The Mucofilm® technology

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TRANSMUCOSAL DRUG DELIVERY


The Mucofilm® technology

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WHAT WE CAN DO WITH OUR TECHNOLOGIES…

.

LOCAL TREATMENT

.

USE CASE: LOCAL TREATMENT


Research

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M. Preis et al. / European Journal of Pharmaceutics and Biopharmaceutics 86 (2014) 552–561

Fact sheet

API Lidocaine HCl

Indication Local pain relief

Dosage form Solvent casting, bilayer

system consiting of an

HPC+API inner layer

and an outer backing

layer using different

polymers and polymer

cominations

USE CASE: LOCAL TREATMENT


Research

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H.E. Colley et al. / Biomaterials 178 (2018) 134-146

Fact sheet

API Clobetasol-17-propionate

Indication Oral lichen planus (OLP) and recurrent aphthous

stomatitis (RAS, also termed aphthous ulcers)

Dosage form Electrospun dual-layer mucoadhesive system

comprising of an outer hydrophobic

polycaprolactone (PLC) backing layer and an

inner, mucoadhesive component formed by

electrospinning polyvinylpyrrolidone (PVP) and

Eudragit® RS100, as fibre-forming polymers.

SYSTEMIC RELEASE

.

USE CASE: PARKINSON‘S DISEASE „OFF EPISODES“


Overview

Managing PD Mid-Stride – A Treatment Guide to Parkinson‘s Disease, Parkinson‘s Foundation



Treatment of off episodes with apomorphine

Managing PD Mid-Stride – A Treatment Guide to Parkinson‘s Disease, Parkinson‘s Foundation

Apomorphine, Drugbank.ca

S. Gancher, Pharmacokinetics of apomorphine in Parkinson’s disease,

J. Neural Transm. Suppl. 45 (1995) 137–141.

M.J. Tsai, Y.B. Huang, P.C. Wu, Y.S. Fu, Y.R. Kao, J.Y. Fang, et al., Oral apomorphine delivery

from solid lipid nanoparticles with different monostearate emulsifiers: pharmacokinetic and

behavioral evaluations, J. Pharm. Sci. 100 (2) (2011) 547–557

Characteristics

Half life 33 min

MW 267 Da

Oral BA <2%

logP 3.1

pKa 8.9



Apomorphine – Subcutaneous delivery



Apomorphine – Subcutaneous delivery

Gebauer Company website, 2019

myIV.com, website, 2019

Healthunlocked.com, website, 2019



Apomorphine – buccal transmucosal delivery

Sunovion.com, website, 2019

SPECIAL PATIENT GROUPS

.

USE CASE: ACCEPTABILITY OF FILMS FOR TREATING NEONATES AND INFANTS


Clinical trial using placebo films developed and manufactured by tesa Labtec

Prospective, single-centre, open,

randomised, single dose, age-stratified two-

way cross-over design with three age sub-

groups

150 patients aged 2 days – 12 months

To investigate the acceptability,

swallowability and palatability of placebo

ODF (2 x 3 cm) in comparison to glucose

syrup 15 % in children aged 2 days to 12

months Klingmann et al. 2018, EuPFI




Klingmann et al. 2018, EuPFI




ODF

• Everything swallowed

• Chewed / partially swallowed

• Spat out

• Inhaled / coughed

• Refused to take / termination

of examination by parents

Syrup

• Everything swallowed

• Partially swallowed

• Spat out

• Inhaled / coughed

• Refused to take / termination

of examination by parents

➢ Criterion 1 = Swallowability

➢ Criterion 1 + 2 = Acceptability




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ODF > syrup over all age groups

Difference 14.7 % (95 % CI 7.91-21.43), p < 0.0001

0

20

40

60

80

100

ODF Syrup

Acceptability over all age groups




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ODF > syrup ODF > syrup ODF = syrup

p = 0.002 p < 0.001 p = 0.5

0

10

20

30

40

50

60

70

80

90

100

ODF Syrup

Acceptability AG 1 (2 – 28 d)

0

10

20

30

40

50

60

70

80

90

100

ODF Syrup

AcceptabilityAG 2 (29 d – 5 m)

0

10

20

30

40

50

60

70

80

90

100

ODF Syrup

AcceptabilityAG 3 (6 – 12 m)




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ODF > syrup

Difference 21.3 %

(95 % CI 11.11-31.55),

p < 0.0001

0

10

20

30

40

50

60

70

80

90

100

ODF Syrup

Swallowabilityover all AGs

Palatability

Assessments are in favour of

the ODF because the rates of

“unpleasant” judgments were

clearly smaller for ODF than

for syrup.




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Safety

• Galenic formulations well tolerated

• None of the children choked on ODF

• 2 children choked on syrup (age group 2 and 3), both events

without clinical relevance

• But: the number of patients and duration of application do not

provide sufficient data for reliable judgement on safety!




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Conclusion:

• Acceptability of ODF significantly superior to syrup over all age

groups, particularly prominent in age group 2

• ODFs are therefore suitable alternatives to liquid paediatric

formulations for young children as of preterm neonates

THANK YOUtesa Labtec GmbH

Dr. Sebastian Braun

Head of Science and Technology

Raiffeisenstr. 4

40764 Langenfeld

Germany

Phone: +49 2173 9735 0

E-Mail: [email protected]

Internet: www.tesa-labtec.com

tesa® products prove their impressive quality day in, day out in demanding conditions and are regularly subjected to strict controls. All technical information and data above mentioned are provided to the best of our knowledge on the basis of our practical

experience. They shall be considered as average values and are not appropriate for a specification. Therefore tesa SE can make no warranties, express or implied, including, but not limited to any implied warranty of merchantability or fitness for a particular

purpose. The user is responsible for determining whether the tesa® product is fit for a particular purpose and suitable for the user’s method of application. If you are in any doubt, our technical support staff will be glad to support you.

TRANSMUCOSAL DRUG DELIVERY Using the Mucofilm … · TRANSMUCOSAL DRUG DELIVERY Drug Delivery and...

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