Development and Optimization of Gastro Retentive Formulations of Hydralazine Hydrochloride

Abstract

Hydralazine is a direct-acting smooth muscle relaxant used to treat hypertension by acting as a vasodilator primarily in arteries and arterioles. The half-life of Hydralazine HCl is very short, 2- 3 hours and frequency of dosing is 3-4 times a day. Hence, the patients need to take frequent dosing and missing of dose may lead to chronical symptoms. To avoid frequent administrations, the long acting floating oral dosage forms can be given which can keep on delivering the drug at controlled rate for a specified period of time. Hence to improve patient co-operation, the sustained release oral floating dosage form may be useful option which once given to patient can continuously deliver the drug at controlled rate without the need of taking tablets many times a day. This would improve patient compliance and would improve the treatment / therapy. Different polymers like HPMC K15M, Carbopol 940 and Sodium bicarbonate (Na2CO3) at different concentration 5%, 10%, 15% were used in order to study and get desired results. Several physical and chemical characterizations were done in order to evaluate. In this research four different dosage forms viz. floating effervescent tablets, mucho adhesive tablets, conventional tablets and in-situ gel were prepared in order to understand the best dosage carrier. To optimize the research work Box-Behnken design was used and results were interpreted from contour plots and comparing to this trial batches with optimized batches in order to achieve desire result and reproducibility. All the batches prepared were carefully evaluated and noted. newline%CCPR (Drug Release) were carried on different intervals upto 24 hours. newline