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拜耳公司 |
同濟(jì)大學(xué) |
聯(lián)合大學(xué) |
美國(guó)保潔 |
美國(guó)強(qiáng)生 |
瑞士羅氏 |
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Delta-8臨界膠束濃度對(duì)于藥物在生物體內(nèi)的增溶性的重要性研究——結(jié)論、致謝!
來源:上海謂載 瀏覽 1285 次 發(fā)布時(shí)間:2021-12-21
結(jié)論
據(jù)我們所知,這是第一個(gè)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(duì)生物相關(guān)介質(zhì)中溶解度增強(qiáng)的影響,而不是在水介質(zhì)中。這項(xiàng)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(cè)FaSSIF中的溶解度增強(qiáng)。我們的研究表明,考慮到化合物在膠束中結(jié)合的趨勢(shì),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(jìng)爭(zhēng)的經(jīng)濟(jì)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(duì)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(qiáng);logd,辛醇/水分配系數(shù);電離常數(shù)
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