Najih, Yuli Ainun and Setyawan, Dwi and Radjaram, Achmad (2014) KINETICS STUDY COCRYSTALS KETOCONAZOLE-SUCCINIC ACID PREPARED WITH SLURRY METHOD BASED ON POWDER X-RAY DIFFRACTION (PXRD). In: International Conference on Pharmaceutics & Pharmaceutical Sciences.

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Abstract

The compounds with low solubility drugs can be a problem in the development of drugs for the pharmaceutical industry. Group of drugs that are included in the Biopharmaceutical Classification System (BCS) class II drugs can be a challenge for the preparations of pharmaceutical development because of low solubility drugs as well as the rate of dissolution. In this case to increase the solubility of drugs besides salts, pharmaceutical cocrystals opened a new dimension to search for solid forms such as solubility, dissolution rate, stability, and shelf life of active pharmaceutical ingredients (APIs) without affecting their inherent pharmacological properties1. Pharmaceutical co crystals are materials or crystalline materials consisting of at least two different components (multicomponent crystals or mixed crystals)2-3. Co crystal could be prepared by several methods, such as solvent evaporation, slurry, melt, and grinding. Co crystals formed between ketoconazole (KTZ) as an active pharmaceutical and succinic acid (SA) as a co crystal former (co-former)4 was increased dissolution rate of pure ketoconazole in equimolar ratio (1:1)1. Physical characterization of co crystal was performed by physical mixture of binary system with molar ratio using different thermal analyzer (DTA) data from KTZ and SA. Besides that, physicochemical characterizations of cocrystal were performed by using PXRD and infrared spectroscopy (IR). Active solid materials in the manufacture of pharmaceutical preparation suffered in various thermic or machanical proccessed such as grinding, milling, granulations (wet and dry granulations), tabletasi, and storage at various temperature, so the materials can occure transformation polymorph or hidrat/ solvat5. Kinetic study of cocrystal KTZ-SA prepared with slurry method at various solvent concentrations a follows 2%, 3%, 4%, 5% and 6% (w/w). Therefore, the aim of the present study was determined the kinetics of co crystals KTZ-SA prepared with slurry method by using Powder X-ray Diffraction (PXRD) data such as the research of co crystalline phase transformation of binary mixture of trimethoprim (TMP) and sulfamethoxazol (SMZ) by slurry technique5.

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