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Solubility Enhancement of Canagliflozin by Binary and Ternary Solid Dispersion Technique
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| Author:
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SHRADHA TIWARI, SHAILESH J WADHER, SURENDRA G.GATTANI
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| Abstract:
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Canagliflozin (CNF) is the newest sodium/glucose cotransporters 2 (SGLT2) inhibitor used for management of type 2 diabetes mellitus having poor aqueous solubility. As very few tablet formulations are available in the market, this study aimed to develop an alternative, cost-effective formulation of CNF with enhanced solubility and dissolution profile. For this purpose, binary (F1-F8) and ternary (F9-F15) solid dispersions of CNF were formulated using polymers such as Soluplus, ß-cyclodextrin, Hydroxypropyl ß-cyclodextrin, Kolliphor P188 and Affinisol in varying ratios. From saturation solubility study and dissolution study, ternary dispersions F9 (CNF/Soluplus/Kolliphor P188 1:1:1) and F10 (CNF/Soluplus/Affinisol 1:1:1) showed 9.04 and 6.62 fold solubility enhancement and drug release of 100.5% and 100.16% respectively. Thus, F9 and F10 were selected for tablet formulation (namely C1 and C2 respectively) and further analysis. In the comparative dissolution study of C1, C2 and marketed formulation (Invokana), the dissolution profile of C1 was found to be comparable with Invokana having per cent drug release of 100.279% and 100.867% respectively. Thus, with the evidence of improved solubility and dissolution profile of C1, it can be concluded that ternary dispersion of CNF/Soluplus/Kolliphor P188 in 1:1:1 ratio can achieve similar dissolution as that of the marketed formulation. CNF pure drug and optimised ternary formulations were characterized by X-ray powder diffraction, thermal analysis and infrared spectroscopy.Thus, binary and ternary amorphous solid dispersions can be a potential alternative for CNF to improve solubility and dissolution profile.
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| Keyword:
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Canagliflozin, Binary and ternary solid dispersion, SGLT 2 inhibitor, solubility
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| EOI:
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| DOI:
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https://doi.org/10.31838/ijpr/2020.12.03.103
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| Download:
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