Formulation comprising a drug of low water solubility and...

A - Human Necessities – 61 – K

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A61K 9/107 (2006.01) A61K 31/423 (2006.01) A61K 31/428 (2006.01) A61K 31/47 (2006.01) A61K 31/503 (2006.01) A61K 31/517 (2006.01) A61K 47/24 (2006.01)

Patent

CA 2626579

A pharmaceutical composition comprises a drug-carrier system having a small- molecule drug of low water solubility, e.g., N [4 (3-amino-1H-indazol-4- yl)phenyl]-N'-(2-fluoro-5-methylphenyl)urea (ABT-869), and (+)-1-(5-tert-butyl- l-y1)-3-( lH-indazol-4-yl)-urea (ABT-102), in solution in a substantially non- aqueous carrier that comprises at least one phospholipid and a pharmaceutically acceptable solubilizing agent. The drug-carrier system, when mixed with an aqueous phase, typically forms a non-gelling, substantially non- transparent liquid dispersion. The composition is suitable for administration by a suitable route, e.g., orally, to a subject in need thereof.

L'invention concerne une composition pharmaceutique comprenant un système de vecteur de médicament comportant un médicament à petite molécule faiblement soluble dans l'eau, tel que, par exemple, N [4 (3-amino-1H-indazol-4-yl)phényl]-N'-(2-fluoro-5-méthylphényl)urée (ABT-869), et (+)-1-(5-tert-butyl-1-yl)-3-( 1H-indazol-4-yl)-urée (ABT-102), en solution dans un vecteur sensiblement non aqueux qui comprend au moins un phospholipide et un agent de solubilisation de qualité pharmaceutique. Ce système de vecteur de médicament, lorsqu'il est mélangé à une phase aqueuse, forme généralement une dispersion liquide sensiblement non transparente, ne formant pas un gel. La composition peut être administrée par une voie adaptée, telle que par voie orale, à un patient nécessitant cette composition.

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