Solubilization of rapamycin

Solubilization of rapamycin
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DOI:
10.1016/s0378-5173(00)00617-7
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发表时间:
2001-02-01
影响因子:
5.8
通讯作者:
Yalkowsky, SH
Yalkowsky, SH
中科院分区:
医学2区
文献类型:
--
作者:
Simamora, P;Alvarez, JM;Yalkowsky, SH

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提出了通过促进水溶作用来溶解雷帕霉素(一种水溶性较差的研究性免疫抑制药物)。部分与水混溶的芳香族溶质(例如苯甲醇、苯甲酸酯或苯甲酸)可以通过与水混溶的共溶剂(例如乙醇和丙二醇)溶解。一旦溶解,部分可混溶的芳香族溶质就变成增溶剂。该技术使雷帕霉素的水溶性显着增加(> 1000 倍)。 (C) 2001 Elsevier Science B.V. 保留所有权利。
The solubilization of rapamycin, a poorly water soluble investigational immunosuppressive drug, by facilitated hydrotropy is presented. Partially water-miscible aromatic solutes (such as benzyl alcohol, benzoate, or benzoic acid) can be solubilized by water-miscible cosolvents, such as ethanol and propylene glycol. Once solubilized, the partially miscible aromatic solute becomes a solubilizing agent. This technique yielded a dramatic(> 1000-fold) increase in the aqueous solubility of rapamycin. (C) 2001 Elsevier Science B.V. All rights reserved.