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I Solid Dispersions Based on Peg 4000, Soluplus® and their Hybrids for Enhanced Delivery of Glimepiride

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Description

Download I Solid Dispersions Based on Peg 4000, Soluplus® and their Hybrids for Enhanced Delivery of Glimepiride. Pharmaceutical Sciences students who are writing their projects can get this material to aid their research work.

Abstract

The present study investigates the possibility of enhancing the solubility, and hence the bioavailability of poorly water soluble glimepiride via formation of polyethylene glycol- polyvinyl caprolactam – polyvinyl acetate grafted copolymer (Soluplus)  and  PEG  4000 based solid dispersions by solvent evaporation technique.

Different batches of glimepiride  solid dispersions (SD) were prepared using solvent evaporation method with Soluplus® and PEG 4000 as polymer matrix at different ratios.

The percentage yield, morphology, drug content, micromeritic properties and drug dissolution studies (in different media: SIF pH 7.4 and SGF 1.2) of the dispersions were evaluated. These formulations were characterized for  solid state properties using differential scanning calorimetry (DSC) and fourier transform infrared (FTIR) studies.

The formulations were further evaluated for alloxan-induced antidiabetic and stability studies. The different batches formulated showed excellent morphology, good flow properties, practical yield and drug content.

Solid state characterisation indicated that glimepiride was present in its amorphous form in formulations with Soluplus®and PEG 4000 due to efficient entrapment in the polymer matrix and with no drug-polymer interaction.

Introduction

Dissolution is the process by which molecules or ions, are transferred from a solid state into a solution. The extent to which the dissolution proceeds under a given set of experimental conditions is referred to as the solubility of the solute in the solvent.

The solubility of a substance is a measure of the maximum amount of that substance that can be dissolved in a given amount of solvent to form a stable solution (1).

Solubility of drug entity is an intrinsic factor to its bioavailability and the desired pharmacological activity in the body can only be achieved when the drug molecules are present in the dissolved state at the site of absorption.

Drug dissolution and release are crucial and limiting step for drug bioavailability particularly for drugs with low solubility and high permeability.

Many chemical entities are poorly water soluble drugs, not well-absorbed after administration which can detract from the drugs inherent efficacy. By improving the release profile of these drugsit is possible to enhance their bioavailability and reduce their side effects.

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