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SOLID DOSED FORMULATIONS OF POT
专利权人:
МЕРК ШАРП ЭНД ДОМЭ КОРП. (US)
发明人:
МАДЖУР Маджид (US),ЧЖАН Дань (US),МОМЕНТ Аарон Дж. (US)
申请号:
RU2011103170/15
公开号:
RU2011103170A
申请日:
2009.06.29
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
1. A solid metered pharmaceutical preparation containing! (1) N - [(3R, 6S) -6- (2,3-difluorophenyl) -2-oxo-1- (2,2,2-trifluoroethyl) azepan-3-yl] -4- (2-oxo -2,3-dihydro-1H-imidazo [4,5-b] pyridin-1-yl) potassium piperidin-1-carboxamide or its hydrate, or ethanolate, or its amorphous form; ! (2) arginine; and! (3) a pharmaceutically acceptable surfactant. ! 2. The solid dosage pharmaceutical preparation according to claim 1, wherein arginine is present in an amount of at least about 10% by weight of the preparation. ! 3. The solid dosage pharmaceutical preparation according to claim 1, containing from about 100 mg to about 500 mg of N - [(3R, 6S) -6- (2,3-difluorophenyl) -2-oxo-1- (2,2, Potassium 2-trifluoroethyl) azepan-3-yl] -4- (2-oxo-2,3-dihydro-1H-imidazo [4,5-b] pyridin-1-yl) piperidin-1-carboxamide. ! 4. The solid dosage pharmaceutical preparation according to claim 1, containing from about 35 to about 55 wt.% N - [(3R, 6S) -6- (2,3-difluorophenyl) -2-oxo-1- (2,2 , 2-trifluoroethyl) azepan-3-yl] -4- (2-oxo-2,3-dihydro-1H-imidazo [4,5-b] pyridin-1-yl) potassium piperidin-1-carboxamide. ! 5. The solid dosage pharmaceutical preparation according to claim 1, wherein the pharmaceutically acceptable surfactant is a nonionic surfactant. ! 6. The solid dosage pharmaceutical preparation according to claim 5, wherein the pharmaceutically acceptable surfactant is a polyoxypropylene block copolymer. ! 7. The solid dosage pharmaceutical preparation according to claim 1, wherein the pharmaceutically acceptable surfactant is present in an amount up to about 10% by weight of the preparation. ! 8. The solid dosage pharmaceutical preparation according to any one of claims 1 to 7, containing form I of the ethanolate N - [(3R, 6S) -6- (2,3-difluorophenyl) -2-oxo-1- (2,2,2 -t1. Твердый дозированный фармацевтический препарат, содержащий ! (1) N-[(3R,6S)-6-(2,3-дифторфенил)-2-оксо-1-(2,2,2-трифторэтил)азепан-3-ил]-4-(2-оксо-2,3-дигидро-1Н-имидазо[4,5-b]пиридин-1-ил)пиперидин-1-ка
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