A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 9/00 (2006.01) A01N 31/08 (2006.01) A01N 57/00 (2006.01) A61K 31/05 (2006.01) A61K 31/661 (2006.01) A61K 47/02 (2006.01) A61K 47/12 (2006.01) A61K 47/18 (2006.01) A61K 47/20 (2006.01) A61K 47/22 (2006.01) A61K 47/26 (2006.01)
Patent
CA 2470500
The present invention is directed to aqueous based formulations of water- soluble prodrugs of propofol. The formulations comprise in aqueous medium an effective amount of the water-soluble prodrug of propofol and an effective amount of an antioxidant. In one embodiment, the formulation also contains a tonicity modifier. The formulations are particularly useful as intravenous injections. The formulations preferably are buffered to a pH suitable for minimizing degradation of the prodrug during storage. Advantageously, the formulations can be prepared without the use of harmful co-solvents or surfactants, and are stable at room temperature over extended periods of time.
La présente invention concerne des formulations aqueuses de prodrogues de propofol solubles dans l'eau. Ces formulations contiennent un agent aqueux, une quantité efficace de prodrogue de propofol soluble dans l'eau et une quantité efficace d'un antioxydant. Dans un mode de réalisation, la formulation contient également un modificateur de tonicité. Les formulations sont particulièrement utiles en injections intraveineuses. Ces formulations sont, de préférence, tamponnées à un pH permettant de réduire la dégradation du prodrogue pendant le stockage. Ces formulations peuvent avantageusement être préparées sans co-solvants ni tensioactifs nocifs et sont stables à température ambiante pendant de longues durées.
Rhodes Christopher A.
Rogers Tracey L.
Williamson Jeffrey A.
Eisai Inc.
Guilford Pharmaceuticals Inc.
Smart & Biggar
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