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改善难溶性药物溶解度的口服制剂策略。

Oral formulation strategies to improve solubility of poorly water-soluble drugs.

机构信息

Laboratory of Pharmacotechnology and Biopharmacy, Katholieke Universiteit Leuven, B-3000 Leuven, Belgium.

出版信息

Expert Opin Drug Deliv. 2011 Oct;8(10):1361-78. doi: 10.1517/17425247.2011.606808. Epub 2011 Aug 3.


DOI:10.1517/17425247.2011.606808
PMID:21810062
Abstract

INTRODUCTION: In the past two decades, there has been a spiraling increase in the complexity and specificity of drug-receptor targets. It is possible to design drugs for these diverse targets with advances in combinatorial chemistry and high throughput screening. Unfortunately, but not entirely unexpectedly, these advances have been accompanied by an increase in the structural complexity and a decrease in the solubility of the active pharmaceutical ingredient. Therefore, the importance of formulation strategies to improve the solubility of poorly water-soluble drugs is inevitable, thus making it crucial to understand and explore the recent trends. AREAS COVERED: Drug delivery systems (DDS), such as solid dispersions, soluble complexes, self-emulsifying drug delivery systems (SEDDS), nanocrystals and mesoporous inorganic carriers, are discussed briefly in this review, along with examples of marketed products. This article provides the reader with a concise overview of currently relevant formulation strategies and proposes anticipated future trends. EXPERT OPINION: Today, the pharmaceutical industry has at its disposal a series of reliable and scalable formulation strategies for poorly soluble drugs. However, due to a lack of understanding of the basic physical chemistry behind these strategies, formulation development is still driven by trial and error.

摘要

简介:在过去的二十年中,药物受体靶标的复杂性和特异性呈螺旋式上升。随着组合化学和高通量筛选技术的进步,有可能针对这些不同的靶点设计药物。不幸的是,但也并非完全出乎意料的是,这些进展伴随着活性药物成分的结构复杂性增加和溶解度降低。因此,提高难溶性药物溶解度的制剂策略的重要性是不可避免的,因此了解和探索最新趋势至关重要。

涵盖领域:本文简要讨论了药物传递系统(DDS),如固体分散体、可溶性络合物、自乳化药物传递系统(SEDDS)、纳米晶体和中孔无机载体,以及市售产品的实例。本文为读者提供了当前相关制剂策略的简明概述,并提出了预期的未来趋势。

专家意见:如今,制药行业拥有一系列可靠且可扩展的难溶性药物制剂策略。然而,由于对这些策略背后的基本物理化学缺乏了解,制剂开发仍然是基于反复试验。

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