A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
167/159, 167/228
A61K 47/00 (2006.01) A61K 31/44 (2006.01) A61K 31/475 (2006.01)
Patent
CA 1159367
Abstract of the Disclosure The present invention relates to a solvent suitable for use in preparing injectable solutions of eburnamenine and dihydroeburnamenine deri- vatives of formula I Image (I) wherein X ~ Y stands for Image or Image wherein Z represents hydroxy or cyano and R is hydrogen an alkoxycarbonyl group having 2 to 6 carbon atoms optionally substituted by one or more halogen atoms or hydroxyl groups or an aralkyloxycarbonyl group. The solvent comprises a pharmaceutically acceptable buffer mixture or an organic acid of pKa = 3-5 cap able of adjusting the pH of the solution to 2.5 to 5.0 preferably 3.0 to 3.5 in case of compounds of the general formula I wherein X~Y represents Image or Image wherein Z represents hydroxy or cyano and R stands for hydrogen, an alkoxy carbonyl group having 2 to 6 carbon atoms optionally substituted by one or more halogen atoms or hydroxy groups or an aralkyloxycarbonyl group provided that if Z stands for hydroxy, then R may not simultaneously stand for hydrogen and to 7.5 to 9.5, preferably to 8.0 to 8.5 in case of compounds of the general formula 1, wherein X~Y represents Image wherein Z represents hydroxy and R stands for hydrogen, one or more stabilizing agents selected from aliphatic alcohols containing one or more hydroxy groups and/or water miscible ethers thereof, 30-70% by weight water, optionally preservatives, anaesthetics and/or antioxidants known per se.
363725
Gazdag Maria
Nagy Geza T.
Szepesi Gabor
Fetherstonhaugh & Co.
Richter Gedeon Vegyeszeti Gyar Rt
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