Improvement of Solubility of Repaglinide by Physical Mixing and Melt Solvent Method
Journal Title: Saudi Journal of Medical and Pharmaceutical Sciences - Year 2018, Vol 4, Issue 2
Abstract
Abstract:This study focused on an investigation of solubility and dissolution rate of the drug repaglinide, a practically water-insoluble antidiabetic drug and the purpose of this study was to enhance the dissolution rate by solid dispersion system consisting of drug, excipients and carrier. Solid dispersion formulations were prepared by using the physical mixing and melt Solvent method. Physical mixtures (PMs) of repaglinide and hydrophilic polymer Kollicoat IR, HPMC, Kollidon 90F, Poloxamar 407 and PVK 30 were prepared at 1:1, 1:3 and 1:5 ratios. Melt Solvent method was used to prepare solid dispersion of repaglinide with hydrophilic excipients Kollicoat IR, HPMC, Kollidon 90F, Poloxamar 407 and PVK 30 at 1:1, 1:3 and 1:5 ratios. All formulations were characterized by scanning electron microscopy (SEM)and dissolution tests. Characterization studies revealed that solid dispersion prepared by melt solvent methods showed better dissolution property compared to physical mixing and pure repaglinide due to theconversion into a less crystalline and/or amorphous form. The order of dissolution enhancement was Kollicoat IR > PVK30>Kollidon 90F>Poloxamar 407> HPMC in solid dispersions. In all cases improvement of dissolution was significantly greater in solid dispersions prepared by Melt solvent method than in physical mixtures. The SEM studies influenced that a decreased crystallinity of the solid dispersions revealed that a portion of repaglinide was in an amorphous state. This was because ofKollicoat IR, Kollidon 90F, Poloxamar 407, HPMC and PVK 30 modified the crystallinity that could beconsidered as an important factor in enhancement of the dissolutionrate. Keywords:Melt Solvent method; Repaglinide; hydrophilic excipients; poorly water-soluble drug; dissolution rate.
Authors and Affiliations
Raihan Sarkar
Keywords
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