结论

据我们所知，这是第一个全面的研究，清楚地显示了类药物化合物的内在表面性质对生物相关介质中溶解度增强的影响，而不是在水介质中。这项研究表明，临界胶束浓度（描述化合物在胶束中自缔合的内在能力）比公认的亲脂性更好地预测FaSSIF中的溶解度增强。我们的研究表明，考虑到化合物在胶束中结合的趋势，药物优化策略将潜在地受益，作为增加肠道吸收的一种方式。

作者信息

通讯作者

*电话：+41616881941。传真：+41616882908。电子邮件：鲁本。阿尔瓦雷斯_ sanchez roche.com.

笔记

作者声明没有相互竞争的经济利益。

致谢

作者要感谢比约恩·瓦格纳、维吉尼·米卡列夫、伊莎贝尔·帕里拉和萨宾·皮塔提供的技术援助，以及弗兰兹·舒勒、萨拉·贝利和乔恩·凯尔·博德纳尔对手稿的修订和宝贵意见。

缩写

FaSSIF，禁食状态模拟肠液；FeSSIF，喂食状态模拟肠液；临界胶束浓度；生物制药分类系统；SE，溶解度增强；logd，辛醇/水分配系数；电离常数

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