Solubility Advantage of Amorphous Drugs and Pharmaceutical Cocrystals
Solubility Advantage of Amorphous Drugs and Pharmaceutical Cocrystals
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DOI：
10.1021/cg200492w
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发表时间：
2011-07-01
影响因子：
3.8
通讯作者：
Nangia, Ashwini
中科院分区：
文献类型：
--
作者：
Babu, N. Jagadeesh;Nangia, Ashwini
药物开发的当前阶段正在经历一场即将到来的危机，这是由于研发成本增加，新药分子数量减少，一些重磅药物从专利悬崖上跌落以及高比例的先进候选药物表现出水溶性差的综合影响。盐制剂改善药物溶解度的传统方法对于缺乏可电离官能团、具有易于分解/外消旋化的敏感部分和/或酸性/碱性不足以形成盐的分子是不成功的。综述了近十年来几种新型的药物共晶，并分析了共晶的增溶特性。药物共晶的溶出峰值出现在短时间内（
The current phase of drug development is witnessing an oncoming crisis due to the combined effects of increasing R&D costs, decreasing number of new drug molecules being launched, several blockbuster drugs falling off the patent cliff and a high proportion of advanced drug candidates exhibiting poor aqueous solubility. The traditional approach of salt formulation to improve drug solubility is unsuccessful with molecules that lack ionizable functional groups, have sensitive moieties that are prone to decomposition/racemization, and/or are not sufficiently acidic/basic to enable salt formation. Several novel examples of pharmaceutical cocrystals from the past decade are reviewed, and the enhanced solubility profiles of cocrystals are analyzed. The peak dissolution for pharmaceutical cocrystals occurs in a short time (