Abstract
Objective: The present study aimed at designing of floating matrix tablet of clopidogrel bisulphate by design of experiments.Methods: The tablets were prepared by direct compression technique using hydroxypropyl methylcellulose K15 (HPMC) as a matrix polymer and sodium bicarbonate as a gas generating agent. In order to optimize the concentration of HPMC (X1) and sodium bicarbonate (X2), a 32 full factorial design was employed. The tablet formulations were evaluated for floating lag time (Y1), floating or buoyancy time (Y2), percent water uptake, and differential scanning calorimetry (DSC) and in vitro drug release (Y3).Results: The formulation variables, HPMC concentration, and sodium bicarbonate concentration exerted a significant effect on floating behavior and drug release characteristics of the tablet. The optimized formulation, with 15% sodium bicarbonate concentration and 30 % HPMC concentration resulted in 5±2.6 sec of floating lag time, 22.0±0.6 h of floating time and 42.0±0.99% of clopidogrel bisulphate release in 8 h of dissolution study. The drug release mechanism was identified as nonfickian. The water uptake studies revealed that with an increase in HPMC concentration, there was an increase in swelling index of tablet whereas higher sodium bicarbonate concentration supported the faster erosion of matrix tablets. DSC study revealed no interaction of drug and polymers. The lower percentage error between predicted and observed responses of the optimized formulation validated the design.Conclusion: The study demonstrated successful designing of floating clopidogrel bisulphate tablet with factorial design.
Highlights
Platelet aggregation has a major role in the clotting process and thrombosis [1]
The coronary events may lead to cardiovascular diseases (CVD), brain ischemia, peripheral arterial disease and other hemorrhagic disorders [3] and are the major causes of mortality and morbidity
In India, almost 24.8% of all deaths are due to Coronary artery disease (CAD) and CVD, and 52% of deaths occur before the age of 70
Summary
Platelet aggregation has a major role in the clotting process and thrombosis [1]. Platelet hyper-reactivity in atherosclerosis and inflammatory disorders may result in serious conditions like acute coronary syndromes, increasing incidences of thrombosis and vascular occlusion [2]. The coronary events may lead to cardiovascular diseases (CVD), brain ischemia, peripheral arterial disease and other hemorrhagic disorders [3] and are the major causes of mortality and morbidity. In India, almost 24.8% of all deaths are due to CAD and CVD, and 52% of deaths occur before the age of 70. This has resulted in high social and economic burden [5]
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