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Physically Stable Solid dispersion
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
申请号:
ARP140100191
公开号:
AR094548A1
申请日:
2014.01.22
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
Claim 1: Physically stable solid dispersion comprising a compound having an aqueous solubility of less than 1 mg / ml and a melting point>; 270 ° C together with a stabilizing polymer. Claim 2: Solid dispersion according to claim 1, wherein the compound having an aqueous solubility of less than 1 mg / ml is acid 4 - {[(2R, 3S, 4R, 5S) -4- (4-chloro- 2-fluorophenyl) -3- (3-chloro-2-fluorophenyl) -4-cyano-5- (2,2-dimethylpropyl) -pyrrolidin-2-carbonyl] -amino} -3-methoxybenzoic acid, of formula (1) . Claim 3: Solid dispersion according to claim 1 or 2,Among them, the stabilizer polymer is the hypnotic substance (hpmcas) of acetic acid and sultanin. 13. Claim 4: the solid of claim 1 or 2 is dispersed, and the stabilizer polymer is eudragitr L-100 or Eudragit l100-55. 115. Claim 5: the solid dispersion of claim 1 or 2, wherein the stabilizer polymer is copovidona (PVP VA 64). 6. Requirement 6: solid dispersion in accordance with any of the requirements of 2 to 5;Wherein, the ratio of the weight of formula compound (1) in claim 2 in solid diffusion to the weight of stabilizer polymer is 5:95 to 70:30. Claim 11: the unit dose of solid preparation in claim 10, including about 80% of solid scattering in the form of solid AMOLIN scattering in any one of claims 6 to 9, and about 7% of crossover sodium. About 6.8% of Manitoba, about 4% of croxvide, about 1.5% of silica coloidal and about 0.7% of stearin magnesium,It is then encapsulated or compressed and coated in flat form. 113. Claim 12: a method for preparing a solid dispersion of a compound and an ionic polymer having a water solubility of less than 1 mg / ml, including forming a compound and polymer solution in a dicarboxylate, or any other suitable solvent, and copolymerizing with the polymer using a deinsectizer. Claim 14: solid dispersion in any one of the 1-8 claims for drugs used to treat cancer, in particular the arbitration model law or prostate cancer.Reivindicación 1: Dispersión sólida físicamente estable que
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