Formulation and Optimization of Drug-Resin Complex Loaded Mucoadhesive Chitosan Beads of Repaglinide Using Factorial Design

Ashwini R M,Mangesh R B,Devaki C U,Nilkanth S P,Rahul R P

doi:10.5923/j.ajmms.20120204.01

Abstract

<b> </b>Some ion exchange resins like Cholestyramine (Duolite AP-143), provide extended gastric retention and have the ability to coat the gastric mucosa uniformly. The use of such mucoadhesive ion exchange resins is another attractive approach in the development of targeted formulations for the GIT. In pesent work, a mucoadhesive gastroretentive system for Repaglinide was developed and optimized using Duolite AP-143 resin by RSM. Studies were carried out to develop and optimize oral mucoadhesive beads for Repaglinide using ion exchange resin and chitosan. Resinates prepared were studied for the effect of pH and drug resin ratio on drug loading. Resin and resinates were evaluated for mucoadhesive property using falling liquid film method. Resin and resinates showed sufficient mucoadhesion strength when compared with other mucoadhesive polymers and other ion exchange resins. Dissolution study of Repaglinide resinate showed that Duolite AP-143 was able to sustain the release of drug. The study suggests that the mucoadhesive beads of Repaglinide provide sustained release over 8 h and also shows sufficient mucoadhesive strength with rabbit gastric mucosa.

Highlights

The control of gastrointestinal transit of orally administered dosage forms using gastroretentive drug delivery systems (GRDDS) can improve the bioavailability of drugs that exhibit site-specific absorption
Resinate of repaglinide was prepared with cholestyramine using the batch method
It was observed that as the concentration of chitosan was increased the % cumulative release of repaglinide decreased. These results indicate that the release behavior of drug is dependent on the viscosity of chitosan solution

Summary

Introduction

The control of gastrointestinal transit of orally administered dosage forms using gastroretentive drug delivery systems (GRDDS) can improve the bioavailability of drugs that exhibit site-specific absorption. Oral bioavailability of certain drugs can be limited by the residence time of the pharmaceutical formulations in the upper gastrointestinal tract. The ability to maintain an oral delivery system at the absorption site for an extended period of time has great appeal for treatment of both local conditions as well as for sustained systemic absorption. Various approaches have been pursued to increase the retention of an oral dosage form in the stomach, including swelling and expanding systems Cargill et al, 1988), high-density systems Davis et al, 1986) and floating systems 1998), modified- shape systems (L.J. Caldwell et al, 1988 and R.I. Cargill et al, 1988), high-density systems (S.S. Davis et al, 1986) and floating systems

Methods

Results

Conclusion