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    • 10. 发明授权
    • Solid dispersions or solid dispersion pharmaceutical preparations of phenylalanine derivatives
    • 固体分散体或固体分散体苯丙氨酸衍生物的药物制剂
    • US08518441B2
    • 2013-08-27
    • US11433589
    • 2006-05-15
    • Hiroyuki HiguchiHirokazu HagioKenichi OgawaAkira Yabuki
    • Hiroyuki HiguchiHirokazu HagioKenichi OgawaAkira Yabuki
    • A61K9/22A61K31/517A61K9/20
    • A61K9/14A61K31/517
    • The present invention provides solid dispersions or solid dispersion pharmaceutical preparations containing a water-soluble polymeric substance(s) and a phenylalanine compound of the formula (1) or pharmaceutically acceptable salts thereof, wherein A represents the formula (2) and the like, B represent an alkoxy group and the like, E represents a hydrogen atom and the like, D represents a substituted phenyl group and the like, T, U and V represent a carbonyl group and the like, Arm represents a benzene ring and the like, R1 represents an alkyl group and the like, R2, R3, and R4 may be the same or different from one another and each represent a hydrogen atom, a substituted amino group and the like, and J and J′ represent a hydrogen atom and the like; production methods thereof; and solubilized pharmaceutical preparations containing a solubilizer(s) and the compound (I) or pharmaceutically acceptable salts thereof. According to the solid dispersion pharmaceutical preparations or solubilized pharmaceutical preparations, though they contain the phenylalanine compound of the formula (1) that is a poorly-soluble drug as an active ingredient, the pharmaceutical preparations having high solubility and oral absorbability can be obtained.
    • 本发明提供了含有水溶性聚合物和式(1)的苯丙氨酸化合物或其药学上可接受的盐的固体分散体或固体分散体药物制剂,其中A表示式(2)等,B 表示烷氧基等,E表示氢原子等,D表示取代苯基等,T,U和V表示羰基等,Arm表示苯环等,R 1 表示烷基等,R 2,R 3和R 4可以相同或不同,表示氢原子,取代氨基等,J和J'表示氢原子等 ; 生产方法; 和含有增溶剂和化合物(I)的溶解药物制剂或其药学上可接受的盐。 根据固体分散药物制剂或溶解性药物制剂,虽然它们含有作为有效成分的难溶性药物的式(1)的苯丙氨酸化合物,但是可以获得具有高溶解度和口服吸收性的药物制剂。