Formulation and in-vivo evaluation of modified dosage form of Clopidogrel bisulfate

The present study was carried out with an objective to formulate modified dosage form of Clopidogrel bisulfate. Clopidogrel bisulfate is available in the form of oral immediate release tablets. It is modified into both pharmaceutical aqueous injection and oral solid floating tablet formulations.  In-vitro and in- vivo evaluation of both the formulations were evaluated. The aqueous injection comprises solubilizer and aqueous solvent. Floating tablet were formulated in different ratio’s of natural based swelling polymer Swelstar MX-I. The floating tablets were based on effervescent approach using sodium bicarbonate as gas generating agent. The effect of polymers concentration on drug release profile was evaluated. The formulations containing sodium bicarbonate 34 mg per tablet provided desired buoyancy (floating lag time of about 2 minutes and total floating time of >24 hours). The in –vivo study on rabbits to see the effect of bleeding time, clotting time, platelet count and partial thromboplastin time were investigated. The results indicates that the bleeding time of clopidogrel floating tablets exhibited effect upto 12 hrs and the effect was maintained for 24 hours compared to reference product. The IV bolus solution showed maximum bleeding time in 1 hr and than decreased significantly as compared to normal control. No significant change in mean platelt count was observed. The clotting time of treated groups significantly increased in test formulation group as compared to normal group upto12 hours but regains to baseline in 24 hours.