Formulation and in vitro evaluation of a fast-disintegrating/sustained dual release bucoadhesive bilayer tablet of captopril for treatment of hypertension crises

Abstract

Hypertension crisis is one of the main health problems and its effective treatment is of high importance. For this purpose, fast-disintegrating and sustained release formulations of captopril, as a drug of choice, were prepared using conventional mucoadhesive polymers hydroxypropyl methylcellulose (HPMC), sodium carboxymethyl cellulose (Na-CMC), hydroxypropyl cellulose (HPC), Carbopol 934 (CP934) and sodium alginate (Na-alg). The optimum sustained release formulations were selected based on mean dissolution time (MDT). The swellability and mucoadhesive properties of selected formulations were assessed and compared. A direct relationship between swelling and release rates/adhesiveness of sustained release formulations was observed. The results showed that formulations containing combination of CP934 and cellulose-based polymers had the highest swellability, sustainability and adhesion strength. These formulations prolonged drug release up to 8 h showing good fitness to Korsemeyer-Peppas model. Moreover, the adopted fast-disintegrating tablet could release up to 100% of drug within 3 min in oral pH. Finally, a dual fast-disintegrating/sustained release bucoadhesive bilayer tablet consisting of optimized formulations was prepared releasing 30% of the drug initially within 15 min and the remaining up to 8 h which could be considered as an appropriate formulation for the treatment of hypertension crises.

Keywords

• Bilayer; Captopril; Dual release; Fast-disintegrating; Sustained release; Bucoadhesive