公开(公告)号：US20060204574A1

公开(公告)日：2006-09-14

申请号：US11433618

申请日：2006-05-15

申请人： Kenichi Ogawa ,  Hirokazu Hagio ,  Hiroyuki Higuchi ,  Motoki Ishikawa ,  Akira Yabuki

发明人： Kenichi Ogawa ,  Hirokazu Hagio ,  Hiroyuki Higuchi ,  Motoki Ishikawa ,  Akira Yabuki

IPC分类号： A61K9/22

CPC分类号： A61K31/517 ,  A61K9/282 ,  A61K31/519 ,  A61K31/53 ,  A61K31/549

摘要： The present invention provides sustained-release oral administration preparations containing the phenylalanine compound of the formula (1) wherein A represent the formula (2) and the like; B represents 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 each other and represent a hydrogen atom, substituted amino group and the like; and J and J′ represent a hydrogen atom and the like, or pharmaceutically acceptable salts thereof as an active ingredient in either form of a coating preparation or a matrix preparation. This active ingredient has a relatively shorter half-life in blood plasma, and the preparations having continuance of the effects are provided by the present invention.

摘要翻译： 本发明提供了含有式（1）的苯丙氨酸化合物的缓释口服制剂，其中A代表式（2）等; B表示烷氧基等; E表示氢原子等; D表示取代的苯基等; T，U和V表示羰基等; Arm表示苯环等; R1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; 并且J和J'表示氢原子等，或其药学上可接受的盐作为涂料制剂或基质制剂的任一种形式的活性成分。 该活性成分在血浆中的半衰期相对较短，本发明提供了具有持久性效果的制剂。

公开(公告)号：US08518441B2

公开(公告)日：2013-08-27

申请号：US11433589

申请日：2006-05-15

申请人： Hiroyuki Higuchi ,  Hirokazu Hagio ,  Kenichi Ogawa ,  Akira Yabuki

发明人： Hiroyuki Higuchi ,  Hirokazu Hagio ,  Kenichi Ogawa ,  Akira Yabuki

IPC分类号： A61K9/22 ,  A61K31/517 ,  A61K9/20

CPC分类号： A61K9/14 ,  A61K31/517

摘要： 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.

摘要翻译： 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。

公开(公告)号：US20060204572A1

公开(公告)日：2006-09-14

申请号：US11433589

申请日：2006-05-15

申请人： Hiroyuki Higuchi ,  Hirokazu Hagio ,  Kenichi Ogawa ,  Akira Yabuki

发明人： Hiroyuki Higuchi ,  Hirokazu Hagio ,  Kenichi Ogawa ,  Akira Yabuki

IPC分类号： A61K31/517 ,  A61K9/20

CPC分类号： A61K9/14 ,  A61K31/517

摘要： 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.