科研之友
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摘要
The present study involves the exploration of the cocrystallization technique for the amelioration of the biopharmaceutical parameters of gliclazide (GL), a poorly water soluble antidiabetic agent, using GRAS status coformers: succinic acid (GL-SA) and malic acid (GL-MA). Cocrystals were prepared by liquid-assisted grinding and characterized by thermoanalytical and vibrational spectroscopic techniques. The crystal structure was determined from PXRD data using BIOVIA Materials Studio software and further assessed for its solubility, intrinsic dissolution and in vivo profile. An almost 2-fold improvement was observed in the solubility and intrinsic dissolution. Pharmacodynamic and pharmacokinetic studies evidenced a remarkable reduction in glucose level and higher C-max in comparison to GL, respectively. The new solid entities thus formed have the potential to be developed as a new formulation of GL and can be commercialized.
- 出版日期2016
