| 摘要 |
A pharmaceutical composition (A) for oral administration of N-(5-chloro-3-(2-chlorophenyl)-1-(3,4-dimethoxy-phenylsulfonyl)-3-hydr oxy-2,3-dihydro-1H-indole-2-carbonyl)-pyrrolidine-2-carboxamide (I) contains a solubilizing/stabilizing system consisting of one or more polyethylene glycols of molecular weight 400-20000, polysorbate 20 and poloxamer 407. A pharmaceutical composition (A) for oral administration comprises: (a) a hydrophobic active agent consisting of one or more isomers of N-(5-chloro-3-(2-chlorophenyl)-1-(3,4-dimethoxy-phenylsulfonyl)-3-hydr oxy-2,3-dihydro-1H-indole-2-carbonyl)-pyrrolidine-2-carboxamide of formula (I); and (b) a solubilizing/stabilizing system consisting of one or more glycol-type nonionic hydrophilic compounds selected from polyethylene glycols of molecular weight 400-20000 and the two amphiphilic surfactants polysorbate 20 and poloxamer 407. Independent claims are also included for: (1) a pharmaceutical dosage form (B) for oral administration, consisting of a capsule containing (A); and (2) preparation of (B), by dissolving (I) at ca. 60 deg C in polyethylene glycol of molecular weight 400-1000 containing polysorbate 20, poloxamer 407 and optionally conventional carriers or excipients to give (A), then filling (A) into a capsule at this temperature (or 40 deg C or less in the case of a soft capsule).
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