Formulation & Development of Oral Controlled Release Suspension

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04 Oct 2009 Controlled Release Suspension 2

IntroductionIntroduction

Novel DDS focused on Peroral SR & CR dosage form as Tab. & Caps.

Solid Dosage forms : Difficult -: Pediatric & Geriatric patient: Dysphagic patients.

Suspension : Drug is insoluble in water Liquid Oral Suspension :

: Flexible dosing: Amenable to dose titration.

04 Oct 2009 3Controlled Release Suspension

• Resin :polymeric and ionic properties release the drugs more uniformly.

Resin-So3Na + Drug-HCl

• Complexation : NaCl + Resin-So3 .Drug-H

Resin-So3 .Drug-H + NaCl

• Drug Release : Drug-HCl + ResinSo3.Na

• Microencapsulation to Resinate: by Emulsion solvent Evaporation


Dextromethorphan: Non-Narcotic Antitussive, Sparingly soluble in water, Dose:10-30mg every 4-8 hrs Amine nature: combined with Cationic ER, t1/2 = 3.2-3.6 hr


Justification:

1.Novelty: 1.Novelty: The project aimed at To prepare CR Antitussive Suspension for

Pediatrics, Use of IER for Extended Release, Development of stable suspension.

2.Usefulness: 2.Usefulness: Dose titration is possible, Flexibility in dosing, Reduction in dosing frequency Minimum side effects.


3.Practicability:3.Practicability:

In house facility – * Formulation * Evaluation

Evaluation of Resinates Dissolution study of Suspension

04 Oct 2009 Controlled Release Suspension 7

Plan Of Work:Plan Of Work:


Continued….


Work ProgressWork Progress

Procurement Of Raw material1. Drug2.Excipients

Literature Survey Complexation Process: Batch Process Dissolution Study Of Suspension: Literature


Problem foreseen & Probable SolutionSr. No. Problem foreseen Probable Solution

1. Selection of resin Depending on nature of drug

2. Solubility of Drug candidate at diff. pH

Use of diff. pH

3. Effect of pH on Complexation Formation

Using diff. pH as solvent media

4. Decomplexation study -In Buffer pH7.2-In 0.4M Hcl

5. Coating to resinate Optimization of coating formula

6. Evaluation Of Suspending Agent

By Sedimentation pattern

7. Release property of suspension

From literature


Pending Work:Pending Work: Characterization of Raw material Purification of Resin Drug-Resin Complexation Analytical method development Experimental Design Coating to resinate Release study of coated resinate Formulation of suspension Release study of optimized suspension Stability study Data Compilation


Expected OutcomeExpected Outcome Antitussive CR suspension for pediatric use Reduction in total amount of drug used Reduction in dosing frequency Patient compliance Reduction in Total Cost Of Pharmacotherapy


ReferenReferencesces

1. T.Pongjanyakul et al “ Characterisation & in vitro release of

dextromethorphan resinate”, power Technology,2. Sambhaji Pisal & et al “Drug release properties of polyethylene-glycol-

treated ciprofloxacin-Indion 234 complexes”, AAPS PharmSciTech ,Vol. 5 Number 4, Dec 2004,10.1208/pt050464.

3. www.rohmhass.com/ionexhange/Pharmaceuticals/stabilization.html4. Singh; Onkar N. & et al “Sustained release ophthalmic, otic and nasal

suspension”United States Patent: 7,001,615. February 21, 2006.

5. Jani, Rajni et al “Sustained-release compositions containing cation exchange resins and polycarboxylic polymers”- Patent EP0429732, 16 March1994.

6. Bhalekar MR, & et al “Preparation and in vitro evaluation of sustained release drug delivery system for verapamil HCL”, Indian Journal of Pharm Sci. Year : 2007,Volume : 69, Issue 3, Page: 418-422.

7. Rajan Bawa et al, “Sustained release formulation containing ion exchange resin”US patent-4931279. 5 June 1990.

8. Halder A, et al, “Sustained release of propranolol hydrochloride based on ion-exchange resin entrapped within polystyrene microcapsules” Journal of Microcapsules. 2006 Dec;23(8):899-911. PMID: 17390631.


7. Mrs. Ashwini R. Madgulkar’s “Ion Exchange Resins in Formulation An Update”. Pharmainfonet.com, Vol 5, Issue 1, 25 Feb 2007.

8. H.S.Hall coating Place INC. “ Sustained release from Coated Ion Exchange Resin ”,Presented at the 6th International Symposium on Controlled Release of Bioactive Materials, New Orleans, August, 1979.

9. HF Liu, & et al “Study of the formulation parameters affecting the preparation of microencapsulated ion-exchange resins containing Vanalafaxine hydrochloride” Indian Journal Of Pharmaceutical Sciences. Year : 2007,Volume:69, Issue:4, Page : 550-555.

10. Seong Hoon Jeong, & et al, “Development of sustained release fast-disintegrating tablets using various polymer-coated ion-exchange resin complexes” , International Journal of PharmaceuticsVolume 353, Issues 1-2, 2 April 2008, Pages 195-204.

11. Betty Wan & et al, “Antitussive drug delivery by Ion exchange Resin”, US patent: 6001392, Dec14, 1999.

12. Raghunathan Y, Amsel L, Hinsvark O, Bryant W “Sustained-release drug delivery system I: Coated ion-exchange resin system for phenylpropanolamine and other drugs” International Journal of Science, 1981 Apr, Volume:70 Issue:4 pg:379-84. PMID: 7229946


ReferenReferencesces

Formulation & Development of Oral Controlled Release Suspension

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