ENHANCEMENT OF DISSOLUTION OF CLOPIDOGREL MINI-TABLETS IN INTESTINAL FLUIDS WITH THE AID OF IN-SITU ACIDIFYING AGENT

The main objective of the present study is to enhance the dissolution of clopidogrel bisulphate in intestinal fluids by formulating into mini-tablets with in-situ acidifying agent mini-tablets. The solubility data reveals, Clopidogrel bisulphate is freely soluble in pH 2.0 and the solubility decreases with increase in pH. Whereas, with weak acid, the solubility of clopidogrel is increased at pH 5.0 blank fed state simulated intestinal fluid and & pH 6.5 blank fasted state simulated intestinal fluid. Hence, tartaric acid is selected in the core tablet to enhance the dissolution of clopidogrel tablets at intestinal fluid pH 5.0 & pH 6.5. Formulation was evaluated with different levels of tartaric acid in core tablet. Formulation with 50mg/unit of tartaric acid showed the extent of dissolution of 100% in pH 5.0 blank fed state simulated intestinal fluid and 96% in pH 6.5 blank fasted state simulated intestinal fluid.  To control the impact of humidity on degradation, a moisture protective layer is coated on core tablet with non-aqueous solvent, using conventional coating pan. The coated mini tablets are encapsulated in a hard gelatin capsule shell. The filled capsules are evaluated for description, assay, dissolution, water by KF