PREPARATION AND CHARACTERIZATION OF GLICLAZIDE SOLID DISPERSION IN BINARY AND TERNARY SYSTEM
Keywords:
Dissolution, Gliclazide, Solid dispersions, Poloxamer 188, HPMC, NilAbstract
Objective: The objective of this research was to improve the dissolution rate of gliclazide by solid dispersion technique with poloxamer 188, HPMC, and Eudragit® E100 as carriers.
Methods: Solid dispersions were prepared by solvent evaporation methods in the binary and ternary system. In binary system gliclazide was mixed with poloxamer188 in the ratio of 1:0.5, 1:0.75, 1:1, 1:1.5 and 1:2, with HPMC in the ratio of 1:0.1, 1:0.125, and 1:0.25, and with Eudragit® E100 in 1:0.25 ratio. In ternary system gliclazide was prepared with poloxamer188 and HPMC in the ratio of 1:2:0.1 and 1:2:0.25, and with poloxamer188 and Eudragit® E100 in the ratio of 1:1:0.25 and 1:2:0.25. Pure gliclazide, solid dispersions, and physical mixtures were characterized by dissolution testing, DSC, FTIR, dan XRD.
Results: At the 15th minute, the highest dissolution rate observed from binary and ternary solid dispersions of gliclazide were from gliclazide-poloxamer188 1:2 dan gliclazide-poloxamer188 and Eudragit® E100 1:2:0,25 which showed 12 and 15 fold increase in dissolution rate compared by pure gliclazide. The decrease of endothermic peak (DSC) and the intensity of the diffraction pattern by XRD of solid dispersions showed the decrease of crystallinity rate. Characterization by FTIR virtually showed no shift of absorption peaks of gliclazide on solid dispersion.
Conclusion: The results of this study indicate that the solid dispersion of gliclazide using poloxamer and Eudragit®E100 in 1:2:0, 25 ratio of weight was the best in enhancing the dissolutions characteristics and bioavailability.
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References
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