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研究pH介质溶解、聚合物的聚合度和溶胀度对基于壳聚糖/藻酸盐混合物的基质中地尔硫卓释放机制的影响。

Study of the influence of the pH media dissolution, degree of polymerization, and degree of swelling of the polymers on the mechanism of release of diltiazem from matrices based on mixtures of chitosan/alginate.

作者信息

Tapia C, Costa E, Moris M, Sapag-Hagar J, Valenzuela F, Basualto C

机构信息

Laboratory of Unit Operations, Faculty of Chemical and Pharmaceutical Sciences, University of Chile, Santiago.

出版信息

Drug Dev Ind Pharm. 2002;28(2):217-24. doi: 10.1081/ddc-120002455.

Abstract

The dissolution profiles of formulations based on mixtures of chitosan/alginate depend on the pH. It is possible to distinguish two processes: (a) a fast kinetic drug release up to 180 min, where the pH value changes from 1.17 to 2.21 and the drug released is controlled by the degree of polymerization and the quantity of chitosan in the formulation; (b) a low kinetic drug release between 210 and 480 min, where the pH value changes from 5.52 to 8.72 and the drug release from the matrix is controlled by the interpolymeric complex. In all formulations the order of release, according to Peppas's model in the range of fast kinetic drug release, was between 0.5 and 1.0. The mechanism of release was non-fickian diffusion, which corresponds to a coupling mechanism of diffusion and relaxation of the polymer.

摘要

基于壳聚糖/藻酸盐混合物的制剂的溶出曲线取决于pH值。可以区分两个过程:(a) 在长达180分钟的快速动力学药物释放过程中,pH值从1.17变为2.21,释放的药物受制剂中壳聚糖的聚合度和数量控制;(b) 在210至480分钟之间的低动力学药物释放过程中,pH值从5.52变为8.72,药物从基质中的释放受聚合物间络合物控制。在所有制剂中,根据Peppas模型,在快速动力学药物释放范围内的释放顺序在0.5至1.0之间。释放机制为非菲克扩散,这对应于聚合物的扩散和松弛的耦合机制。

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