Enhanced dissolution and bioavailability of gliclazide using solid dispersion techniques

Shavi, Gopal Venkatesh and Averineni, Ranjith Kumar and Nayak, Usha Yogendra and Armugam, Karthik and Ranjan, Om prakash and Pandey, Sureshwar and Udupa, N and Ginjupalli, Kishore (2010) Enhanced dissolution and bioavailability of gliclazide using solid dispersion techniques. International Journal of Drug Delivery, 2 (1). pp. 49-57. ISSN 1083-7450

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Gliclazide is practically insoluble in water and its bioavailability is limited by dissolution rate. To enhance the dissolution rate and bioavailability the present study was aimed to formulate solid dispersions using different water soluble polymers such as polyethylene glycol 4000 (PEG 4000), polyethylene glycol 6000 (PEG 6000) using fusion method and polyvinyl pyrrolidone K- 30 (PVP K 30) by solvent evaporation method. The interaction of gliclazide with the hydrophilic polymers was studied by Differential Scanning Calorimetry (DSC), Fourier Transformation-Infrared Spectroscopy (FTIR) and X-Ray diffraction analysis. Solid dispersions were characterized for physicochemical properties like drug content, surface morphology and dissolution studies. Various factors like type of polymer and ratio of the drug to polymer on the solubility and dissolution rate of the drug were also evaluated. Pharmacokinetic studies of optimized formulation were compared with pure drug and marketed formulation in wistar rats. The dissolution of the pure drug and solid dispersion prepared with PVP K 30 (1:1) showed 38.3 + 4.5 % and 95 + 5.2 % release respectively within 30 min. Peak plasma concentration of pure drug, solid dispersion (PVP K 30) and marketed formulation was found to be 8.76 + 2.5, 16.04 + 5.5 and 9.24 + 3.6 μg/ml respectively, from these results it was observed that there is two fold increase in peak plasma concentration compared to pure drug. Solid dispersion is an effective technique in increasing solubility, dissolution rate and bioavailability of the poorly soluble drugs.

Item Type: Article
Uncontrolled Keywords: Gliclazide; solubility; solid dispersion; pharmacokinetics; peak plasma concentration; half life
Subjects: Dentistry > MCODS Manipal > Dental Materials
Pharmacy > MCOPS Manipal > Pharmaceutics
Depositing User: KMC Manipal
Date Deposited: 28 Apr 2012 04:28
Last Modified: 23 Oct 2013 04:24
URI: http://eprints.manipal.edu/id/eprint/76351

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