DUAL RELEASE CHRONOTHERAPEUTIC SYSTEM OF POORLY WATER SOLUBLE ANTIHYPERTENSIVE DRUG CARVEDILOL: DESIGN, DEVELOPMENT AND IN VITRO CHARACTERIZATION

Abstract

The current research investigation’s goal was to design a core-in-cup type pulsatile system of an antihypertensive drug (carvedilol phosphate) to reduce the evening and early-morning symptoms of hypertension. An inclusion complex of this drug was prepared with hydroxyl propyl beta cyclodextrin to increase carvedilol solubility. Using direct compression method, various batches of core tablets were formulated using Croscarmellose sodium as a superdisintegrant. Core tablets of the optimized formulation were press coated with backing layer and release-retarding plug layer. An in vitro release research was performed after evaluating the physicochemical characteristics of the core in cup design tablets. Based on the lag time of 8 h between the first and second pulse releases, a batch containing sodium alginate (100 mg) and hydroxypropyl methylcellulose K4M (100 mg) was chosen as the optimum batch. Thus, the dual-release core-in-cup pulsatile tablets may be utilized for managing the hypertension symptoms appearing in chronological order.