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Pharmaceutical Methods for Enhancing the Dissolution of Poorly Water-Soluble Drugs.
ASSAY and Drug Development Technologies ( IF 1.8 ) Pub Date : 2023-01-01 , DOI: 10.1089/adt.2022.119
Tahir Mahmood 1 , Rai M Sarfraz 1 , Asmara Ismail 2 , Muhammad Ali 2 , Abdur Rauf Khan 2
Affiliation  

Low water solubility is the main hindrance in the growth of pharmaceutical industry. Approximately 90% of newer molecules under investigation for drugs and 40% of novel drugs have been reported to have low water solubility. The key and thought-provoking task for the formulation scientists is the development of novel techniques to overcome the solubility-related issues of these drugs. The main intention of present review is to depict the conventional and novel strategies to overcome the solubility-related problems of Biopharmaceutical Classification System Class-II drugs. More than 100 articles published in the last 5 years were reviewed to have a look at the strategies used for solubility enhancement. pH modification, salt forms, amorphous forms, surfactant solubilization, cosolvency, solid dispersions, inclusion complexation, polymeric micelles, crystals, size reduction, nanonization, proliposomes, liposomes, solid lipid nanoparticles, microemulsions, and self-emulsifying drug delivery systems are the various techniques to yield better bioavailability of poorly soluble drugs. The selection of solubility enhancement technique is based on the dosage form and physiochemical characteristics of drug molecules.

中文翻译:

提高水溶性差药物溶解度的制药方法。

水溶性低是制药业发展的主要障碍。据报道,大约 90% 正在研究的药物新分子和 40% 的新药具有低水溶性。制剂科学家的关键和发人深省的任务是开发新技术来克服这些药物与溶解度相关的问题。本综述的主要目的是描述克服生物制药分类系统 II 类药物溶解度相关问题的常规和新颖策略。回顾了过去 5 年发表的 100 多篇文章,以了解用于提高溶解度的策略。pH 值改变、盐形式、无定形形式、表面活性剂增溶、共溶剂、固体分散体、包合物络合、聚合物胶束、晶体、尺寸减小、纳米化、前体脂质体、脂质体、固体脂质纳米颗粒、微乳液和自乳化药物递送系统是提高难溶性药物生物利用度的各种技术。增溶技术的选择基于药物分子的剂型和理化特性。
更新日期:2023-03-15
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