Solubilization of rapamycin

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• 作者：Simamora ; Pahala ; Alvarez ; Joan M. ; Yalkowsky ; Samuel H.
• 关键词：Solubilization ; Rapamycin ; Solubility ; Cosolvent ; Hydrotrope ; Hydrotropy
• 刊名：International Journal of Pharmaceutics
• 出版年：2001
• 出版时间：February 1, 2001
• 年：2001
• 卷：213
• 期：1-2
• 页码：25-29
• 全文大小：67.9 K

文摘

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.