Formulation and Evaluation of Floating-pulsating Drug Delivery System containing Fixed-dose Combination for Chronotherapy of Hypertension

Abstract

This project aims to build a floating, pulsatile hypertension therapy. This work examined the 3-factor, 2-level box-behnken design and optimization technique for the floating pulsatile tablet. The quantity of polyox WSR N12K and polyox WSR205 was chosen to be the independent variable. Drug release, lag time, and swelling index are chosen to function in terms of dependent variables. ANOVA was intended to assess the data statistically, and p-value of 0.05 was regarded to have statistical significance. The tablet containing bisoprolol fumarate (BF) and hydrochlorothiazide (HCTZ) was chosen for preparation. The system comprises of 2 parts: an outer layer comprised of an erodible material with a gas-generating agent and a center core tablet holding the active medicinal component. Super disintegrants and active ingredients are to be used to prepare rapid release core tablets (RRCT). The improved formulation’s release kinetics provided the best fit for the zero-order models. The floating-pulsatile release (FPRT) F13 revealed a lag-time of 4 hours with > 90% of the drug being released at level 0 (65 mg) for polyox (WSR-205) and level +1 (65 mg) for polyox (WSR-N12K). After the burst, drug release is restricted. The tablets floated well and released drug for 6 hours. The concept of floating pulsatile is to be applied to improve retention in a gastric environment of dosage forms that have a lag phase after bursts release.