Abstract

In this experimental work an extended release matrix tablet of Benidipine Hydrochloride (BH) has been prepared to extend drug release for more than 18 hr which has advantage of continuous 24 hr control of blood pressure (BP) in hypertension patient, showing long-lasting pharmacological activity and increases the patient compliance. Benidipine is a calcium channel blocker that is used for the treatment of mild to moderate hypertension and angina pectoris and BH extended release tablets reduce the side effects associated with multiple dosing used during conventional tablets. Tablets are prepared tablets containing different polymers concentration through direct compression method. The in vitro percentage drug release and drug release mechanism were studied. From the drug release mechanism, the tablets showed the Higuchi square root model and R2 values for batch F2 (R2 =0.998) indicates that the drug released by diffusion mechanism and from Peppas equation n value 0.720 (range 0.89-1) indicates that diffusion–erosion mechanisms resulting from swelling and hydration behavior of Chitosan and along with HPMC K 100 M and Eudragit R S 100 extending drug release. Different pharmacokinetics parameters has been studied from results of in vivo study by using PK solver software which shows that marketed conventional BH tablet reached peak plasma concentration of 830.986 µg/ml after 2 hr of administration, where as selected optimized prepared tablets reached the maximum concentration of 708.83 µg/ml after 1 hr of administration, but it continues to release drug for more than 36 hr when in vivo was carried out in carried out on white New Zealand rabbits. These results proved that drug is released slowly for prolonged period of time and achieving better BP control. So based on this research outcome and results, we may conclude our objective is achieve by extending drug release pattern of BH.

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