Rani Meena, Surana Rahul, Sankar Chelladurai, Mishra Brahmeshwar
Department of Pharmaceutics, Institute of Technology, Banaras Hindu University, Varanasi-221005 (U.P.), India.
Acta Pharm. 2003 Dec;53(4):263-73.
Based on the principles of an elementary osmotic pump (OP), OP tablets were designed and evaluated with the aim to deliver diclofenac sodium (DS) in a controlled manner. In vitro evaluation was done in various release media and kinetics was evaluated using the regression coefficient analysis. Effects of orifice size, coating membrane type, coating thickness, static and stirred conditions and pH variation were studied. In vivo evaluation was performed on six healthy human volunteers and various pharmacokinetic parameters (c(max), t(max), AUC(0-24), MRT) and relative bioavailability were calculated. The results were compared with the performance of two commercial tablets of DS. The drug release from OP tablets was dependent on the type and thickness of the coating membrane, but was independent of the orifice size and static and stirred conditions of the release medium. The OP tablets provided a prolonged and controlled DS release compared to commercial sustained-release and conventional tablets of DS.
基于基本渗透泵（OP）原理，设计并评估了OP片剂，旨在以可控方式递送双氯芬酸钠（DS）。在各种释放介质中进行体外评估，并使用回归系数分析评估动力学。研究了孔口大小、包衣膜类型、包衣厚度、静态和搅拌条件以及pH变化的影响。对六名健康人类志愿者进行体内评估，并计算各种药代动力学参数（c(max)、t(max)、AUC(0-24)、MRT）和相对生物利用度。将结果与两种DS市售片剂的性能进行比较。OP片剂的药物释放取决于包衣膜的类型和厚度，但与孔口大小以及释放介质的静态和搅拌条件无关。与DS的市售缓释片和普通片相比，OP片剂提供了延长且可控的DS释放。
