Microwave-induced solid dispersion technology to improve bioavailability of glipizide.

Jinu Isaac, Santanu Kaity, Swastika Ganguly, Animesh Ghosh

Department of Pharmaceutical Sciences, Birla Institute of Technology, Ranchi, India.

The Journal of pharmacy and pharmacology 2013 Feb

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The effect of microwave (MW) irradiation and conventional heating (CH) on solid dispersion (SD) of poorly water-soluble glipizide (GPZ) and polyethylene glycol 4000 (PEG 4000) were studied in detail. The chemical stability of GPZ on exposure to MW irradiation and CH was confirmed by high-performance liquid chromatography, Fourier transform infra red spectroscopy, proton nuclear magnetic resonance and mass spectroscopy studies. Comparative bioavailability studies were performed in rabbits using glipizide sustained-release tablets prepared using MW irradiation (MW-SD) or CH (CH-SD), with Glytop 2.5 mg SR as a reference. The MW-assisted melt mixing showed higher efficiency than CH in obtaining a homogeneous mixture having glass transparency. The polymorphic transformation of GPZ in each case was further confirmed by powder X-ray diffraction study. The solubility of GPZ in phosphate buffer pH 6.8 was greater for MW-SD (72.250 ± 0.154 μg/ml) than CH-SD (46 ± 0.201 μg/ml). The MW-SD matrix tablet (2.5 mg) displayed retarded drug release (releasing 99.320 ± 4.992% drug in 12 h). In-vivo pharmacokinetic study in rabbits revealed that the relative bioavailability of GPZ from MW-SD tablets improved greatly (153.73 ± 9.713%). MW-induced SD technology could be a better alternative to CH-SD for the enhanced solubility and bioavailability of GPZ. © 2012 The Authors. JPP © 2012. Royal Pharmaceutical Society.

Citation

Jinu Isaac, Santanu Kaity, Swastika Ganguly, Animesh Ghosh. Microwave-induced solid dispersion technology to improve bioavailability of glipizide. The Journal of pharmacy and pharmacology. 2013 Feb;65(2):219-29