Solid Dispersion of an Anti-Diabetic Drug with Block Co-Polymer for Enhancement of Aqueous Solubility, Dissolution and Bioavailability | Chapter 5 | Technological Innovation in Pharmaceutical Research Vol. 8

 Pre-formulation and formulation studies for the creation of solid dispersions with improved oral bioavailability are the focus of this study. Gliclazide (GLC), an oral hypoglycemic medication, has a low solubility in stomach fluid, a slow dissolving rate, and a wide range of bioavailability between individuals. The goal of this work was to use the lyophillisation process to create optimal solid dispersions (SD) of GLC with a hydrophilic carrier, such as poloxamer 407 (PXM), in order to improve the drug's aqueous solubility and therapeutic efficacy. The influence of polymer concentration on GLC solubility was investigated using a phase solubility research with increasing PXM concentrations (0.5 to 10% w/v). Physical mixing and lyophillisation (freeze drying) were used to make SDs of GLC and PXM in 1:1, 1:3, and 1:5w/w ratios, which were then tested for dissolving. On twelve healthy New Zealand rabbits, an in vivo comparison of optimised SD and GLC was undertaken. When compared to physical mixes and pure drug, the dissolution rate of GLC from lyophilized dispersions was significantly higher. In vivo experiments revealed that the pharmacokinetic properties of the optimised SD and pure GLC after oral administration were significantly different (P 0.05). The peak serum concentrations (Cmax) for the lyophilized SD and GLC were determined to be 3.010.42 g/mL and 2.27 0.39 g/mL, respectively, while the time required to attain the peak serum concentration (Tmax) for the optimised SD was much less (2.160.41) than for GLC (4.330.52). In an invivo test, the SD's relative bioavailability was reported to be 158.52 percent. These findings show that using a suitably hydrophilic carrier such as PXM to create SDs using the lyophillisation approach can significantly increase the solubility and in vitro dissolution of a lipophilic medication such as GLC. The proposed approach shows promising results in terms of gliclazide absorption and bioavailability after oral administration, and it can be used for other hydrophobic drug moities.

Author (s) Details

Farzana S. Bandarkar
Department of Pharmaceutics, Faculty of Pharmacy, Kuwait, University, Kuwait.

Ibrahim S. Khattab
Kuwait Saudi Pharmaceutical Industries Company, Kuwait.

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