Abstract

This study examines the sustained release behavior of both water-soluble (acetaminophen, caffeine, theophylline and salicylic acid) and water-insoluble (indomethacin) drugs from Leucaena leucocephala seed Gum isolated from Leucaena leucocephala kernel powder. It further investigates the effect of incorporation of diluents like microcrystalline cellulose and lactose on release of caffeine and partial cross-linking of the gum (polysaccharide) on release of acetaminophen. Applying exponential equation, the mechanism of release of soluble drugs was found to be anomalous. The insoluble drug showed near case II or zero-order release mechanism. The rate of release was in the decreasing order of caffeine, acetaminophen, theophylline, salicylic acid and indomethacin. An increase in release kinetics of drug was observed on blending with diluents. However, the rate of release varied with type and amount of blend in the matrix. The mechanism of release due to effect of diluents was found to be anomalous. The rate of release of drug decreased on partial cross-linking and the mechanism of release was found to be super case II.

Highlights

  • Hydrophilic matrices are an interesting option when developing an oral sustained-release formulation

  • Leucaena leucocephala seed polysaccharide (LLSP) is used as ingredient in food material, in pharmaceuticals has not been evaluated as hydrophilic drug delivery system

  • [13] This led to its Jeevanandham, et al.: J Young Pharm. 2010;2(1): 15-20 application as excipient in hydrophilic drug delivery system. [11,12] Since LLSP is an important excipient, the present study was undertaken to elucidate release kinetics of both water-soluble and water-insoluble drugs from this matrix

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Summary

Introduction

Hydrophilic matrices are an interesting option when developing an oral sustained-release formulation They can be used for controlled release of both water-soluble and water-insoluble drugs. LLSP is a galactoxyloglucan isolated from seed kernel of Leucaena leucocephala It possesses properties such as high viscosity, broad pH tolerance, and adhesivity.[9] This led to its application as stabilizer, thickener, gelling agent and binder in food and pharmaceutical industries. The commonly adopted model for understanding such behavior from hydrophilic matrices is simple exponential equation.[14] This model facilitates the understanding of mode of release like: Whether the release is due to only diffusion or only erosion, or due to both diffusion and erosion This model has been used for this study

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