Solubilization of rapamycin.
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.
Simamora
P
P
Pharmaceutical Research and Development, Schering-Plough HealthCare Products, Inc., 3030 Jackson Avenue, Memphis, TN 38151, USA. pahala.simamora@spcorp.com
Alvarez
J M
JM
Yalkowsky
S H
SH
D000900:Anti-Bacterial Agents / Q000737:chemistry*; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D002851:Chromatography, High Pressure Liquid; D020123:Sirolimus / Q000737:chemistry*; D012995:Solubility; D012997:Solvents
D000900:Anti-Bacterial Agents; D012997:Solvents; D020123:Sirolimus