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[以美达西泮为例探讨重溶性弱碱性药物在骨架片中的释药控制]

[The control of drug release of heavy-soluble, weak basic drugs in matrix tablets using the example of medazepam].

作者信息

Zessin G, Fahr F, Mank R

出版信息

Pharmazie. 1986 Jan;41(1):39-42.

PMID:2870512
Abstract

According to ideas about the diffusion layer in the process of dissolving solids the release of medazepam as a model substance for heavy-soluble, weak alkaline substances is modified by incorporation of solid acids of different solubility and dissociation rate into the matrix. The determination of the solubility and a "virtual" pH-value within the matrix tablets leads to the evaluation of the liberation. A relatively continuous release of medazepam following different pH-values in the medium was obtained by microencapsulation of the citrus acid incorporated. Using the ideas of the diffusion layer to explain the conditions within the matrix it becomes possible to control and influence the drug release from the matrix tablet.

摘要

根据关于固体溶解过程中扩散层的观点,通过将不同溶解度和解离速率的固体酸掺入基质中,来改变作为重溶性、弱碱性物质模型的美达西泮的释放。测定基质片剂内的溶解度和“虚拟”pH值可对释放情况进行评估。通过对掺入柠檬酸的微囊化处理,在介质中不同pH值条件下实现了美达西泮相对持续的释放。利用扩散层的观点来解释基质内的情况,就能够控制和影响基质片剂中药物的释放。

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