English

Wenwu Zheng

doi:10.5897/ajpp12.1391

Abstract

The purpose of this study was to develop once-daily sustained-release matrix capsules of nifedipine (F1) using the combination of solid dispersion and drug controlled release techniques. F1 were prepared by the wetting granules methods using hydroxypropyl methyl cellulose (HPMC) as hydrophilic retard drug release agent and ethylcellolulose (EC) ethanol solution based on the polyvinyl pyrrolidone / stearic acid solid dispersion. In vitro drug release kinetic model of F1 was fitted well with the zero-order kinetic equation: Q=0.0736 t+0.0871 (R=0.993) in the range of 0-6 h, the first-order kinetic equation: Ln (1-Q) =-0.0934 t-0.1375 (R=0.999) in the range of 6-24 h, respectively. The relative bioavailability of F1 was studied in rabbits after oral administration using a commercial available controlled release tablet (F2) as a reference. The pharmacokinetic results showed no significant differences in Cmax, MRT and AUC (0-24h). The relative oral bioavailability value from F1 in comparison with F2 was 97.12 %. The results of both in vitro and in vivo studies indicated that once-daily sustained-release matrix capsules of NFD prepared by the optimized formulation exhibited excellent sustained-release effects and high relative oral bioavailability.   Key words: Once-daily sustained-release matrix capsules of nifedipine, solid dispersion, pharmacokinetic behavior.

Highlights

For the treatment of chronic diseases, such as hypertension and angina pectoris, the most suitable administration route is the oral route
Application of solid dispersions composed of hydrophilic carrier in which a lipophilic drug is incorporated is a proven technique to improve the poor water solubility of drug (Huang et al, 2011; Srinarong et al, 2012)
Many studies have been reported that the solid dispersion technique was used to enhance oral bioavailability of poor water soluble drugs (Boghra et al, 2011; Tran et al, 2011)

Summary

Introduction

For the treatment of chronic diseases, such as hypertension and angina pectoris, the most suitable administration route is the oral route. In long-term therapy of the treatment of hypertension, conven- tional formulations of the most antihypertensive drugs need to be administered twice or three times a day, which result in marked blood pressure fluctuations. The formulations of drug sustained (controlled) release delivery systems are preferred for such therapy because of the advantages like reduced frequency of administra- tion and fluctuation in plasma drug concentration, maintenance of stable blood pressure and improvement of patient compliance (Barakat and Almurshedi, 2011; Sousa de Silva et al, 2011). Successful treatment of hypertension in clinical practice means maintenance of blood pressure at a normal physiological level. The oral drug sustained (controlled) release delivery system for the treatment of hypertension is an ideal strategy

Objectives

Methods

Results

Conclusion