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果胶和壳聚糖游离混合膜的粘膜粘附性和药物渗透性:一项体外和体内研究。

Mucoadhesion and drug permeability of free mixed films of pectin and chitosan: an in vitro and ex vivo study.

作者信息

Hagesaether Ellen, Hiorth Marianne, Sande Sverre Arne

机构信息

Department of Pharmacy, University of Oslo, Oslo, Norway.

出版信息

Eur J Pharm Biopharm. 2009 Feb;71(2):325-31. doi: 10.1016/j.ejpb.2008.09.002. Epub 2008 Sep 12.

Abstract

The objective of this study was to identify the important factors for the drug permeability and mucoadhesion of casted free pectin/chitosan combination films. The factors varied were: the type of pectin (low and high methoxyl pectin) and the ratio pectin:chitosan (25:75, 50:50 and 75:25). The model drug used for measuring drug permeability was paracetamol. A texture analyzer was used for measuring mucoadhesion by using two different setups: (1) in vitro tensile tests measuring the detachment force of films versus a mucin dispersion and (2) ex vivo shear tests measuring the friction forces between pre-hydrated films and fresh porcine small intestine, with the system immersed in phosphate buffer, pH 6.8. The type of pectin used in the combination films did not have a significant effect on the drug permeability. The ex vivo mucoadhesion test revealed significant differences between low and high methoxyl pectin only for the 50:50 pectin:chitosan films. For that type of film, the peak and friction forces were highest for high methoxyl pectin. Both the mucoadhesion and drug permeability generally increased with decreasing amounts of pectin relative to chitosan in the films.

摘要

本研究的目的是确定浇铸的游离果胶/壳聚糖复合膜药物渗透性和黏膜黏附性的重要影响因素。变化的因素包括:果胶类型(低甲氧基果胶和高甲氧基果胶)以及果胶与壳聚糖的比例(25:75、50:50和75:25)。用于测量药物渗透性的模型药物是对乙酰氨基酚。使用质地分析仪通过两种不同设置测量黏膜黏附性:(1)体外拉伸试验,测量膜与黏蛋白分散液之间的分离力;(2)离体剪切试验,测量预水化膜与新鲜猪小肠之间的摩擦力,系统浸入pH 6.8的磷酸盐缓冲液中。复合膜中使用的果胶类型对药物渗透性没有显著影响。离体黏膜黏附试验表明,仅对于50:50果胶:壳聚糖膜,低甲氧基果胶和高甲氧基果胶之间存在显著差异。对于该类型的膜,高甲氧基果胶的峰值力和摩擦力最高。膜中相对于壳聚糖,果胶含量减少时,黏膜黏附性和药物渗透性通常都会增加。

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