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Parenteral preparations of gemcitabine derivatives
专利权人:
КЛАВИС ФАРМА АСА (NO)
发明人:
АХРАБИ Сайех (NO),МИРЕН Финн (NO),ЭРИКСЕН Уле Хенрик (NO)
申请号:
RU2012125350/04
公开号:
RU2012125350A
申请日:
2010.11.15
申请国别(地区):
RU
年份:
2013
代理人:
摘要:
1. A pharmaceutical composition that contains a gemcitabine derivative of the formula I: wherein R and R are hydrogen and R is a C or C saturated and monounsaturated acyl group, or a pharmaceutically acceptable salt thereof, as an active component; wherein the active component is formulated into a preparation containing : a) a solubilizing phospholipid selected from the group consisting of phosphatidylcholine, phosphatidylglycerol, phosphatidylethanolamine, phosphatidylinositol, phosphatidylserine, phosphatidic acid, lysophospholipids, sphingomy lin and cardiolipin in any form, including saline or desalted, hydrogenated or partially hydrogenated natural, semisynthetic or synthetic; b) joint solubilizer selected from the group consisting of charged phospholipids; c) an isotonic agent; where the molar ratio of active component to phospholipid is in the range from 1: 6.6 to 1: 1 and the preparation has an average D particle size in the range of 2.5-30 nm. 2. The pharmaceutical composition of claim 1, wherein the active component is gemcitabine-5'-elaidic acid ester. The pharmaceutical composition according to claim 1, where the solubilizing phospholipid contains natural phospholipids originating from chicken eggs containing a zwitterionic phospholipid that is neutral at a pH in the range of 6-8.4. The pharmaceutical composition according to claim 1, wherein the solubilizing phospholipid contains purified phosphatidylcholine derived from chicken eggs. The pharmaceutical composition of claim 1, wherein the co-solubilizer is chicken egg phosphatidylglycerol. Pharmaceutical composition1. Фармацевтическая композиция, которая содержит производное гемцитабина формулы I:где Rи Rпредставляют собой водород и Rпредставляет собой С- или C-насыщенную и мононенасыщенную ацильную группу, или его фармацевтически приемлемую соль в качестве активного компонента;где активный компонент приготовлен в виде препарата, содержащего:a) солюбилизирующий фосфолипид, выбранный из группы, включающе
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