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1st World Conference on Physico-Chemical Methods in Drug Discovery and Development Gliclazide cocrystals: In vitro and In vivo evaluations Averinnei R.K, Johan N, Shavi G, Armugam K, Nayak U, Pandey S, Udupa N Department of Pharmaceutics Manipal College of Pharmaceutical Sciences Manipal University, Manipal, 576 104, India Abstarct As per the BCS classification gliclazide comes under the category of Class II drugs, the drugs with low solubility and good permeability. So the present study is aimed at the preparation of cocrystals with the various carriers such as succinic acid, glutaric acid, nicotinic acid and tartaric acid with different ratios. Here the cocrystals are prepared by the slow solvent evaporation method and cogrinding method. The fornmulated cocrystals were evaluated for the vaious in vitro studies like micromeritic properties (carr’s index, hausners ratio, angle of repose) drug content, saturation solubility and varoius evaluations using the differential scanning calorimeter, infrared spectroscopy, scanning electron microscopy and powder X-ray diffraction. Optimized cocrystals were evaluated for the preclinical pharmacokinetic and pharmacodynamic studies in the plain and diabetes induced male wistar rats. Finally the optinmized formulations were compressed into tablets using the direct compression method. From the results it was observed that there is no incompatibility between the selected carries and the gliclazide. Compared to the pure drug of gliclazide the micromeritic properties were greatly improved. The saturation solubility of the gliclazide is increased about 2 folds compared to the plain drug. From the reuslts of the solubility it was observed that the slow solvent evaporation method was found to optimum compared to the cogriding method. The in vitro dissolution studies shows that there is faster release of the gliclazide in form of cocrystals compared to that of the plain drug. The DSC, IR, SEM and PXRD studies indicated that there is alteration in the crystal form of the structure and hence it showed improved solubility and dissoluton. The pharmacokinetic studies shows improved systemic exposure of the gliclazide in the form of cocrystals compared to the plain drug. The pharmacodynamic studies shows the percentage reduction of blood glucose levels in the plain animals are 30.56, 34.03, 53.16 and 61.55 for the cocrystals of gliclazide prepared with the tartaric acid, succinic acid, glutaric acid and nicotinic acid respectively at the end of one hour and the normal blood glucose levels were reached at the end of four hours. Similarly the percentage reduction of blood glucose levels in the diabetes induced animals are 17.81, 18.40, 22.53 and 23.17 respectively for the cocrystals prepared with tartaric acid, succinic acid, glutaric acid and nicotinic acid. Based on the in vitro and in vivo evaluations and considering the stability studies it was concluded that nicotinic acid was a suitable carrier for the formulation of the gliclazide cocrystals. Reference: 1. P. Vishweshwar, J.A. McMahon, J.A. Bis, M.J. Zaworotko, Pharmaceutical co-crystals. J Pharm Sci. 95 (2006) 499-516.