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黄原胶和羟丙基甲基纤维素在控释药物递送方面的流变学特性

Rheological characterization of xanthan gum and hydroxypropylmethyl cellulose with respect to controlled-release drug delivery.

作者信息

Talukdar M M, Vinckier I, Moldenaers P, Kinget R

机构信息

Laboratory of Galenical and Clinical Pharmacy, Katholieke Universiteit Leuven, Belgium.

出版信息

J Pharm Sci. 1996 May;85(5):537-40. doi: 10.1021/js950476u.

Abstract

It has been observed previously that xanthan gum (XG) and hydroxypropylmethyl cellulose (HPMC) show different drug release behavior. In order to clarify these findings, the rheological properties of both polymers have been determined by oscillatory as well as by steady shear measurements. Aqueous solutions of 4 and 7% (w/w) polymer have been used to simulate the outer surface of a hydrated tablet. The dynamic moduli, i.e., storage modulus (G') and loss modulus (G") of the two polymers have been determined in pure water and USP phosphate buffer pH 7.4 at different dilutions. In this concentration range XG solution exhibits "gel-like" behavior, while HPMC behaves as a typical polymer solution. These findings are quite consistent with the reported higher ability of XG matrices to retard drug release than HPMC matrices for controlled-release formulation. The effects of differences in drug solubility and acidity, as well as the addition of lactose, and of the ionic strength of the medium on the rheological properties of XG and HPMC solutions have been studied in detail. Among these parameters, only the salt concentration exerts an enhancing effect on both moduli of XG, while no detectable influence on HPMC solution could be observed.

摘要

先前已观察到,黄原胶(XG)和羟丙基甲基纤维素(HPMC)表现出不同的药物释放行为。为了阐明这些发现,通过振荡测量和稳态剪切测量来测定这两种聚合物的流变性质。使用4%和7%(w/w)聚合物的水溶液来模拟水合片剂的外表面。在纯水和USP磷酸盐缓冲液pH 7.4中不同稀释度下测定了这两种聚合物的动态模量,即储能模量(G')和损耗模量(G'')。在此浓度范围内,XG溶液表现出“凝胶状”行为,而HPMC表现为典型的聚合物溶液。这些发现与报道的在控释制剂中XG基质比HPMC基质具有更高的药物释放延迟能力相当一致。已详细研究了药物溶解度和酸度差异、乳糖添加以及介质离子强度对XG和HPMC溶液流变性质的影响。在这些参数中,只有盐浓度对XG的两种模量都有增强作用,而未观察到对HPMC溶液有可检测到的影响。

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