ENHANCEMENT OF DISSOLUTIONAND BIOAVAILABILITY OF BCS- CLASS II DRUG BY SOLID DISPERSION METHOD
Abstract
Glibenclamideis a BCS –class II drug it has poor solubility and absorption patterns. The aim of the present study is to improve the solubility and dissolution characteristics of Glibenclamide by preparing solid dispersion using Melting- Solvent method technique and to study the effect of particle size and different dissolution media on drug release property. The carrier used was Soluplus as a solubilizer. The solid dispersions were prepared in drug: carrier ratios 1:1.5, 1:2, 1:3, 1:4, 1:6 and 1:8 by solvent evaporation method. The resultant solid dispersions were evaluated for solubility studies at different pH conditions. From the dissolution analysis it was observed that the drug release from 1:3 formulation was released above 50% within 5min than that of physical mixture of Glibenclamide, soluplus and pure drug. Solid dispersions of 1:1.5 and 1:2 were also shown 50% release but after 30 min. Hence 1:3 formulation was optimized. In 1:3 formulation 250-micron particle size of solid dispersion showed higher release than with other solid dispersion. A Solid-state characterization of solid dispersion has been carried out by DSC, FTIR and results revealed that the solid dispersion containing drug: polymer ratio 1:3 has shown amorphous form with improved solubility and dissolution. Solid dispersions were subjected to accelerated stability studies and were characterized by DSC.
Keywords
Glibenclamide, soluplus, DSC, FTIR