ENHANCEMENT OF SOLUBILITY OF AN ORAL HYPOGLYCAEMIC DRUG, GLIMEPERIDE BY THE TECHNIQUE COCRYSTALLISATIONAbstract
Co-crystallization is one of the most reliable alternative approaches to increase the solubility of poorly water-soluble drugs without affecting their physicochemical properties. Pharmaceutical cocrystals are neutral organic compounds connected to the API preferentially by loosely formed bonds as dipole-dipole interaction. Our present study aims at improving the solubility of an effective oral hypoglycemic, Glimepiride, a sulphonylurea class of drug that often lacks water solubility. In the process of enhancing its solubility, four different co-formers were used as Anthranilic acid, Succinic acid, Salicylic acid, Benzoic acid, and Gallic acid in different stoichiometric ratios like 1:2 and 1:3. The technique opted for the making is slow evaporation and prepare the nanoparticle by using Chitosan and gelatin polymeric matrix with aldehydic oxidized Xanthan gum as crosslinking agent. Initial confirmation was made through melting point determination. Later structure elucidation of co-crystals was carried out by several analytical methods, such as FTIR, X-ray Diffraction. In FTIR spectra, a sharp decrease in the intensity of N-H peak of salicylic acid and succinic acid was observed in 1:2 ratio, which in turn indicates the formation of the hydrogen bond. PXRD indicates crystallinity by the formation of a sharp, high intense peak in drug: salicylic acid in 1:2 ratios. The nanoparticle was evaluated on the basis of size determination, DEE, and in-vitro release study, which gives promising results that release for a prolonged period of time. In the future, in-vivo and other physicochemical properties were evaluated.
P. Bose, S. Chandra, A. Das, T. Roy *, S. Paul and L. Mukherjee
Department of Pharmaceutical Technology, JIS University, Kolkata, West Bengal, India.
17 February 2020
13 May 2020
26 May 2020
01 February 2021