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COMPOSITIONS {3- [5- (4-CHLOROPHENYL) -1H-PYRROLO [2, 3] PYRIDIN-3-CARBONIL] -2,4-DIPHORORPHENYL} AMIDES OF PROPANE-1-SULPHIC ACID AND THEIR APPLICATION
专利权人:
Ф.ХОФФМАНН-ЛЯ РОШ АГ (CH)
发明人:
ДИОДОНЕ Ральф (DE),ЛАУПЕР Штефан (CH),МАИР Ханс-Юрген (DE),ПУДЕВЕЛЛЬ Иоганнес (CH),ВИРШЕМ Франк (CH)
申请号:
RU2012123958/04
公开号:
RU2012123958A
申请日:
2010.11.08
申请国别(地区):
RU
年份:
2013
代理人:
摘要:
1. A method of obtaining a solid dispersion containing an amorphous form of a compound of formula 1 and HPMCAS, comprising the following steps: (a) dissolving a compound of formula 1 and HPMCAS in the same organic solvent, thereby obtaining one organic phase, (b) continuously adding an organic phase, obtained in stage (a), in the aqueous phase, which is present in the mixing chamber, and the specified mixing chamber is equipped with a mixing device with a high shear and two additional holes that connect the specified mixing a closed-circuit chamber through which said aqueous phase circulates and passes through the mixing chamber, (c) precipitating a mixture comprising an amorphous form of the compound of formula 1 and HPMCAS from the aqueous phase indicated in step (b) with the high-shear mixer turned on and the specified aqueous phase circulates through the mixing chamber and the closed system, thus forming an aqueous suspension of the precipitate, (d) continuous circulation of the aqueous suspension through the mixing chamber until the formation of particles of a certain size and / or until a certain ennogo particle size distribution, while the high shear mixer and after the addition of the organic solution obtained in step (a) into the aqueous phase, (e) isolation of the solid phase from the suspension, (f) washing the selected solid phase 0.01N. HCl and / or water, and (g) destruction and drying of the solid phase. 2. The method according to claim 1, where the organic phase in stage (a) is a 10% to 40% solution of compound 1 and HPMCAS in dimethylacetamide, the ratio of compound 1 to HPMCAS is from about 10:90 (wt.% / Wt.% ) to approximately 60:40 (wt.% / wt.%) and1. Способ получения твердой дисперсии, содержащей аморфную форму соединения формулы 1и HPMCAS, включающий следующие стадии:(a) растворение соединения формулы 1 и HPMCAS в том же самом органическом растворителе, при этом получают одну органическую фазу,(b) непрерывное добавление органической фазы, получ
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