一种新型的时间和pH依赖性结肠靶向给药系统的设计、开发与优化。

Design, development and optimization of a novel time and pH-dependent colon targeted drug delivery system.

作者信息

Patel Mayur M, Shah Tejal J, Amin Avani F, Shah Nitesh N

机构信息

Department of Pharmaceutics and Pharmaceutical Technology, Institute of Pharmacy, Nirma University of Science and Technology, Gujarat, India.

出版信息

Pharm Dev Technol. 2009;14(1):62-9. doi: 10.1080/10837450802409412.

DOI:10.1080/10837450802409412

PMID:18802844

Abstract

The aim of present study was to develop a time- and pH-dependent system for delivering mesalamine to the colon. The system consists of the core tablet of mesalamine which is compression coated with hydroxypropyl methylcellulose (HPMC K4M) (time-dependent factor). This is then coated with pH-dependent polymer Eudragit L100. The simplex lattice design was adopted to optimize the independent variables i.e. amount of HPMC (X1), dextrose (X2) and polyvinyl pyrollidone (PVP) (X3) and to study their effect on the dependent variables i.e. lag time and time for 50% drug dissolution (t50). The results of the linear interactive model and graphical representation revealed that as the amount of HPMC increases, the lag time and t50 value also increases and as the amount of dextrose and PVP were increased the lag time and t50 value decreases.

摘要

本研究的目的是开发一种能将美沙拉嗪递送至结肠的时间和pH依赖性系统。该系统由美沙拉嗪核心片剂组成，该片剂用羟丙基甲基纤维素（HPMC K4M）进行压制包衣（时间依赖性因素）。然后再用pH依赖性聚合物尤特奇L100进行包衣。采用单纯形格子设计来优化自变量，即羟丙基甲基纤维素的用量（X1）、葡萄糖（X2）和聚乙烯吡咯烷酮（PVP）（X3），并研究它们对因变量，即滞后时间和50%药物溶解时间（t50）的影响。线性交互模型和图形表示的结果显示，随着羟丙基甲基纤维素用量的增加，滞后时间和t50值也增加，而随着葡萄糖和聚乙烯吡咯烷酮用量的增加，滞后时间和t50值减小。