合作客戶/
拜耳公司 |
同濟大學 |
聯合大學 |
美國保潔 |
美國強生 |
瑞士羅氏 |
相關新聞Info
推薦新聞Info
-
> 超低界面張力環保型高溫高鹽油藏的驅油表面活性劑配方比例及制備（二）
> 超低界面張力環保型高溫高鹽油藏的驅油表面活性劑配方比例及制備（一）
> 表面張力和接觸角的關系|寶玉石接觸角的測量結果和表面張力計算方法（三）
> 表面張力和接觸角的關系|寶玉石接觸角的測量結果和表面張力計算方法（二）
> 表面張力和接觸角的關系|寶玉石接觸角的測量結果和表面張力計算方法（一）
> 表面張力儀系統測定：溫度范圍內甲基九氟丁醚的液相密度與表面張力
> 一套低溫、高壓懸滴法表面張力實驗測量系統實踐效果（三）
> 一套低溫、高壓懸滴法表面張力實驗測量系統實踐效果（二）
> 一套低溫、高壓懸滴法表面張力實驗測量系統實踐效果（一）
> 不同溫度下純有機物液體表面張力估算方法及關聯方程（二）
Delta-8臨界膠束濃度對于藥物在生物體內的增溶性的重要性研究——結論、致謝！
來源：上海謂載 瀏覽 1994 次 發布時間:2021-12-21
結論
據我們所知，這是第一個全面的研究，清楚地顯示了類藥物化合物的內在表面性質對生物相關介質中溶解度增強的影響，而不是在水介質中。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在能力）比公認的親脂性更好地預測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合的趨勢，藥物優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，禁食狀態模擬腸液；FeSSIF，喂食狀態模擬腸液；臨界膠束濃度；生物制藥分類系統；SE，溶解度增強；logd，辛醇/水分配系數；電離常數
參考資料
(1)Amidon,G.L.;Lennernas,H.;Shah,V.P.;Crison,J.R.A theoretical basis for a biopharmaceutic drug classification:the correlation of in vitro drug product dissolution and in vivo bioavailability.Pharm.Res.1995,12(3),413?20.
(2)Tsume,Y.;Mudie,D.M.;Langguth,P.;Amidon,G.E.;Amidon,G.L.The Biopharmaceutics Classification System:Subclasses for in vivo predictive dissolution(IPD)methodology and IVIVC.Eur.J.Pharm.Sci.2014,57,152?63.
(3)Jones,H.M.;Parrott,N.;Ohlenbusch,G.;Lave,T.Predicting pharmacokinetic food effects using biorelevant solubility media and physiologically based modelling.Clin Pharmacokinetics 2006,45(12),1213?26.
(4)Galia,E.;Nicolaides,E.;Horter,D.;Lobenberg,R.;Reppas,C.;Dressman,J.B.Evaluation of various dissolution media for predicting in vivo performance of class I and II drugs.Pharm.Res.1998,15(5),698?705.
(5)Andrieux,K.;Forte,L.;Lesieur,S.;Paternostre,M.;Ollivon,M.;Grabielle-Madelmont,C.Insertion and partition of sodium taurocholate into egg phosphatidylcholine vesicles.Pharm.Res.2004,21(8),1505?16.
(6)Nawroth,T.;Buch,P.;Buch,K.;Langguth,P.;Schweins,R.Liposome formation from bile salt-lipid micelles in the digestion and drug delivery model FaSSIF(mod)estimated by combined timeresolved neutron and dynamic light scattering.Mol.Pharmaceutics 2011,8(6),2162?72.
(7)Mithani,S.D.;Bakatselou,V.;TenHoor,C.N.;Dressman,J.B.Estimation of the increase in solubility of drugs as a function of bile salt concentration.Pharm.Res.1996,13(1),163?7.
(8)Ottaviani,G.;Gosling,D.J.;Patissier,C.;Rodde,S.;Zhou,L.;Faller,B.What is modulating solubility in simulated intestinal fluids?Eur.J.Pharm.Sci.2010,41(3?4),452?7.
(9)Fagerberg,J.H.;Karlsson,E.;Ulander,J.;Hanisch,G.;Bergstrom,C.A.Computational prediction of drug solubility in fasted simulated and aspirated human intestinal fluid.Pharm.Res.2014,32,578?89.
(10)Persson,L.C.;Porter,C.J.;Charman,W.N.;Bergstrom,C.A.Computational prediction of drug solubility in lipid based formulation excipients.Pharm.Res.2013,30(12),3225?37.
(11)Casartelli,A.;Bonato,M.;Cristofori,P.;Crivellente,F.;Dal Negro,G.;Masotto,I.;Mutinelli,C.;Valko,K.;Bonfante,V.A cellbased approach for the early assessment of the phospholipidogenic potential in pharmaceutical research and drug development.Cell Biol.Toxicol 2003,19(3),161?76.
(12)Fischer,H.;Atzpodien,E.A.;Csato,M.;Doessegger,L.;Lenz,B.;Schmitt,G.;Singer,T.In silico assay for assessing phospholipidosis potential of small druglike molecules:training,validation,and refinement using several data sets.J.Med.Chem.2012,55(1),126?39.
(13)Seelig,A.;Gottschlich,R.;Devant,R.M.A method to determine the ability of drugs to diffuse through the blood-brain barrier.Proc.Natl.Acad.Sci.U.S.A.1994,91(1),68?72.
(14)Peresypkin,A.;Kwei,G.;Ellison,M.;Lynn,K.;Zhang,D.;Rhodes,T.;Remenar,J.Supramolecular behavior of the amphiphilic drug(2R)-2-ethylchromane-2-carboxylic acid arginine salt(a novel PPARalpha/gamma dual agonist).Pharm.Res.2005,22(9),1438?44.
(15)Kloefer,B.;van Hoogevest,P.;Moloney,R.;Kuentz,M.;Leigh,M.L.S.;Dressman,J.Study of a standardized taurocholate-lecithin powder for preparing the biorelevant media FeSSIF and FaSSIF.Dissolution Technol.2010,17(3),6?13.
(16)Milletti,F.;Storchi,L.;Sforna,G.;Cruciani,G.New and original pKa prediction method using grid molecular interaction fields.J.Chem.Inf.Model.2007,47(6),2172?81.
(17)Mannhold,R.;Poda,G.I.;Ostermann,C.;Tetko,I.V.Calculation of molecular lipophilicity:State-of-the-art and comparison of log P methods on more than 96,000 compounds.J.Pharm.Sci.2009,98(3),861?93.
(18)Pagliara,A.;Carrupt,P.A.;Caron,G.;Gaillard,P.;Testa,B.Lipophilicity profiles of ampholytes.Chem.Rev.1997,97(8),3385?3400.
(19)Vertzoni,M.;Fotaki,N.;Kostewicz,E.;Stippler,E.;Leuner,C.;Nicolaides,E.;Dressman,J.;Reppas,C.Dissolution media simulating the intralumenal composition of the small intestine:physiological issues and practical aspects.J.Pharm.Pharmacol.2004,56(4),453?62.
(20)Kerns,E.H.;Di,L.;Carter,G.T.In vitro solubility assays in drug discovery.Curr.Drug Metab.2008,9(9),879?85.
(21)Lehto,P.;Kortejarvi,H.;Liimatainen,A.;Ojala,K.;Kangas,H.;Hirvonen,J.;Tanninen,V.P.;Peltonen,L.Use of conventional surfactant media as surrogates for FaSSIF in simulating in vivo dissolution of BCS class II drugs.Eur.J.Pharm.Biopharm.2011,78(3),531?8.
(22)Fagerberg,J.H.;Tsinman,O.;Sun,N.;Tsinman,K.;Avdeef,A.;Bergstrom,C.A.Dissolution rate and apparent solubility of poorly soluble drugs in biorelevant dissolution media.Mol.Pharmaceutics 2010,7(5),1419?30.
(23)Box,K.J.;Comer,J.E.Using measured pKa,LogP and solubility to investigate supersaturation and predict BCS class.Curr.Drug Metab.2008,9(9),869?78.
(24)Avdeef,A.Absorption and Drug Development:Solubility,Permeability,and Charge State,2nd ed.;John Wiley&Sons:Hoboken,NJ,2012;Vol.xli,p 698.