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固体制剂中 pH 调节剂对低水溶性的弱酸性或弱碱性药物溶出度的调节机制。

Dissolution-modulating mechanism of pH modifiers in solid dispersion containing weakly acidic or basic drugs with poor water solubility.

机构信息

Kangwon National University, College of Pharmacy, Bioavailability Control Laboratory, Chuncheon, Republic of Korea.

出版信息

Expert Opin Drug Deliv. 2010 May;7(5):647-61. doi: 10.1517/17425241003645910.

Abstract

IMPORTANCE OF THE FIELD

Although the solid dispersion method has been known to increase the dissolution rate of poorly water-soluble drugs by dispersing them in hydrophilic carriers, one obstacle of the solid dispersion method is its limited solubilization capacity, especially for pH-dependent soluble drugs.

AREAS COVERED IN THIS REVIEW

pH-modified solid dispersion, in which pH modifiers are incorporated, may be a useful method for increasing the dissolution rate of weakly acidic or basic drugs. Sufficient research, including the most recent reports, was undertaken in this review.

WHAT THE READER WILL GAIN

How could the inclusion of the pH the pH modifiers in the solid dispersion system change drug structural behaviors, molecular interactions, microenvironmental pH, and/or release rate of pH modifiers, relating with the enhanced dissolution of weakly acidic or weakly basic drugs with poor water solubility? These questions have been investigated to determine the dissolution-modulating mechanism of pH modifiers in solid dispersion containing weakly acidic or basic drugs.

TAKE HOME MESSAGE

It is believed that step-by-step mechanistic approaches could provide the ultimate solution for solubilizing several poorly water-soluble drugs with pH-dependent solubility from a solid dispersion system, as well as provide ideas for developing future dosage systems.

摘要

重要性领域

尽管固体分散体方法通过将其分散在亲水性载体中已经被证明可以提高水溶性差的药物的溶解速率,但是固体分散体方法的一个障碍是其有限的增溶能力,特别是对于 pH 依赖性可溶性药物。

本综述涵盖的领域

pH 改性固体分散体,其中包含 pH 改性剂,可能是增加弱酸性或碱性药物溶解速率的有用方法。在本综述中进行了充分的研究,包括最新的报告。

读者将获得什么

在与增加难溶性弱酸性或弱碱性药物的溶解有关的情况下,将 pH 调节剂包含在固体分散体系统中会如何改变药物的结构行为、分子相互作用、微环境 pH 和/或 pH 调节剂的释放速率?已经研究了这些问题,以确定含弱酸性或弱碱性药物的固体分散体中 pH 调节剂的溶解调节机制。

结论

人们相信,逐步的机制方法可以为从固体分散体系统中溶解几种具有 pH 依赖性溶解度的难溶性药物提供最终解决方案,并为开发未来的剂型系统提供思路。

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