The objective of this study was to improve therapeutic activity of gliclazide by improving its aqueous solubility through preparation of inclusion complex between gliclazide and β-cyclodextrin. Gliclazide β-cyclodextrin solid complex was prepared with equimolar ratio of both gliclazide and β-cyclodextrin in presence or absence of water soluble polymers (PVP-K15 and HPMC) using co-evaporation, spray drying and freeze drying techniques. The prepared solid complexes were characterized by DSC, IR, XRD and dissolution testing in comparison with the pure gliclazide powder. The solid complexes prepared by spray drying, freeze drying and co-evaporation in presence of hydrophilic polymers showed a prompt drug release compared to pure gliclazide (P < 0.05). The spry dried complex in presence of PVP-K15 showed the highest drug release after 5 and 90 min and significantly increased the % dissolution efficiency (P < 0.05) compared to the pure drug. Moreover, in vivo assessment of the hypoglycemic activity of this complex in comparison with a commercial drug product was studied in diabetic rats. Statistical analysis of the pharmacodynamic parameters including maximum % reduction in blood glucose level (BGL) and area under % reduction in BGL versus time curve (AUC0-24) data obtained for gliclazide -cyclodextrin complex showed significantly (P<0.05) higher values compared to the commercial drug product. These results suggest that spry dried gliclazide -cyclodextrin complex in presence of PVP-K15 is useful for improving the hypoglycemic effect of gliclazide in diabetic rats.
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