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
Related Articles
- EP ID EP397224
- DOI -
- Views 71
- Downloads 0
A Validated Reversed Phase HPLC Assay for the Determination of Gliclazide in Human Plasma
Abstract:A simple and precise reversed-phase high performance liquid chromatography (HPLC) method for the determination of gliclazide in human plasma was developed and validated. Using glipizide as an internal standard (...
Antisnake Venoms and their Mechanisms of Action: A Review
Abstract:Snakebite is a major socio-medical problem affecting many communities globally, especially African and Asian countries. It is still depending on the usage of antisera as the major source of treatment, which has...
Antibacterial Activity of Methanolic Fruit Extract of RandiadumetorumLamk against Ocular Pathogens
Abstract:Ocular diseases have been documented as the most common health problems universally. Most of the chemicals and synthetic drugs currently in use have marked side effects. Hence, there has been an ideal shift from...
Antinociceptive Properties of Desmodium adscendens in Mice
Abstract: This study evaluated the analgesic property of Desmodium adscendens (DA) in mice using the Hot plate test and the Formalin test. Eighteen (18) mice of 15-25g body weight were used for this study. The mice were...
Synthesis of Possible Anti-Cancer and Anti-Mycobacterial Fluoro Substituted Sulphonamide Benzothiazoles Comprising Potent Thiazolidinone
Abstract: In the present study, a series of N-[6-fluoro-7-substituted-1,3-benzothiazol-2-yl]-4-[2-(3-nitrophenyl)-4-oxo-thiazolidin-3-yl]benzenesulphonamide and N-[6-fluoro-7-substituted-1,3-benzothiazol-2-yl]-4-[2-(4-ni...