結(jié)論

據(jù)我們所知，這是第一個全面的研究，清楚地顯示了類藥物化合物的內(nèi)在表面性質(zhì)對生物相關(guān)介質(zhì)中溶解度增強的影響，而不是在水介質(zhì)中。這項研究表明，臨界膠束濃度（描述化合物在膠束中自締合的內(nèi)在能力）比公認(rèn)的親脂性更好地預(yù)測FaSSIF中的溶解度增強。我們的研究表明，考慮到化合物在膠束中結(jié)合的趨勢，藥物優(yōu)化策略將潛在地受益，作為增加腸道吸收的一種方式。

作者信息

通訊作者

*電話：+41616881941。傳真：+41616882908。電子郵件：魯本。阿爾瓦雷斯_ sanchez roche.com.

筆記

作者聲明沒有相互競爭的經(jīng)濟利益。

致謝

作者要感謝比約恩·瓦格納、維吉尼·米卡列夫、伊莎貝爾·帕里拉和薩賓·皮塔提供的技術(shù)援助，以及弗蘭茲·舒勒、薩拉·貝利和喬恩·凱爾·博德納爾對手稿的修訂和寶貴意見。

縮寫

FaSSIF，禁食狀態(tài)模擬腸液；FeSSIF，喂食狀態(tài)模擬腸液；臨界膠束濃度；生物制藥分類系統(tǒng)；SE，溶解度增強；logd，辛醇/水分配系數(shù)；電離常數(shù)

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