药物溶解度:重要性和增强技术。

Ketan T Savjani, Anuradha K Gajjar, Jignasa K Savjani
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引用次数: 745

摘要

溶解度,溶质在溶剂中溶解形成均质体系的现象,是药物在体循环中达到所需浓度以达到期望(预期)药理反应的重要参数之一。低水溶性是新化学实体配方开发和通用开发中遇到的主要问题。制药工业开发的nce(新化学实体)40%以上几乎不溶于水。溶解度是配方科学家面临的主要挑战。任何被吸收的药物必须在吸收部位以溶液的形式存在。提高难溶性药物溶解度的方法有多种,包括对药物进行物理和化学改性以及其他方法,如减小粒径、晶体工程、盐的形成、固体分散、使用表面活性剂、络合等。溶解度改善方法的选择取决于药物的性质、吸收部位和所需的剂型特征。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

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Drug solubility: importance and enhancement techniques.

Solubility, the phenomenon of dissolution of solute in solvent to give a homogenous system, is one of the important parameters to achieve desired concentration of drug in systemic circulation for desired (anticipated) pharmacological response. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities as well as for the generic development. More than 40% NCEs (new chemical entities) developed in pharmaceutical industry are practically insoluble in water. Solubility is a major challenge for formulation scientist. Any drug to be absorbed must be present in the form of solution at the site of absorption. Various techniques are used for the enhancement of the solubility of poorly soluble drugs which include physical and chemical modifications of drug and other methods like particle size reduction, crystal engineering, salt formation, solid dispersion, use of surfactant, complexation, and so forth. Selection of solubility improving method depends on drug property, site of absorption, and required dosage form characteristics.

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