Solubilization of flavopiridol by pH control combined with cosolvents, surfactants, or complexants
Solubilization of flavopiridol by pH control combined with cosolvents, surfactants, or complexants
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DOI：
10.1021/js990097r
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发表时间：
1999-09-01
影响因子：
3.8
通讯作者：
Yalkowsky, SH
中科院分区：
文献类型：
--
作者：
Li, P;Tabibi, SE;Yalkowsky, SH
本研究探讨了离子化和unionized物种的flavopiridol在溶解络合，胶束化，共溶作用的作用。pH控制与表面活性剂（聚山梨酯20和聚山梨酯80）、助溶剂（乙醇和丙二醇）以及不带电荷的阴离子络合剂[羟丙基β-环糊精（HP β CD）和磺丁基醚β-环糊精（SBE β CD）]联合使用，以溶解夫拉匹多。这些组合技术不仅增加了未离子化的夫拉吡啶醇的溶解度，而且增加了离子化药物的溶解度。本研究证实，以前开发的方程有效地表征的作用的pH值，pK（a），无论是络合常数，胶束分配系数，或共溶剂增溶能力，在确定药物的总水溶解度。
This study investigates the roles of both ionized and unionized species of flavopiridol in solubilization by complexation, micellization, and cosolvency. Control of pH was used in combination with surfactants (polysorbate 20 and polysorbate 80), cosolvents (ethanol and propylene glycol), as well as uncharged and anionic complexing agents [hydroxypropyl beta-cyclodextrin (HP beta CD) and sulfobutyl ether beta-cyclodextrin (SBE beta CD)] to solubilize flavopiridol. These combined techniques increase not only the solubility of the un-ionized flavopiridol but also the solubility of the ionized drug. This study confirms that previously developed equations effectively characterize the roles of pH, pK(a), and either complexation constant, micelle partition coefficient, or cosolvent solubilizing power in determining drug total aqueous solubility.