Solid pharmaceutical composition comprising 4...

A - Human Necessities – 61 – K

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Details

A61K 31/277 (2006.01) A61K 9/14 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2443040

The present invention relates to a pharmaceutical formulation comprising the drug 4'-cyano-.alpha.',.alpha.',.alpha.'-trifluoro-3-(4-fluorophenylsulphonyl)- 2-hydroxy-2-methylpropiono-m-toluidide in a solid dispersion with PVP. In one embodiment, >50% of the drug is provided in the form of the R-enantiomer. The invention also relates to a daily pharmaceutical dose of the drug provided by such a formulation. In addition, the invention relates to the use of PVP in solid dispersion with the drug (in one embodiment wherein >50% of the 4'-cyano- .alpha.',.alpha.',.alpha.'-trifluoro-3-(4-fluorophenylsulphonyl)-2-hydroxy-2- methylpropiono-m-toluidide is provided in the form of the R-enantiomer) for increasing the bioavailability of the drug; for reducing inter-patient variability in plasmaconcentrations of the drug; for enhancing the storage stability of the drug; or for treating and/or reducing the risk of prostate cancer in a patient.

La présente invention concerne une formulation pharmaceutique contenant le médicament 4'-cyano-.alpha.', .alpha.', .alpha.'-trifluoro-3-(4-fluorophénylsulfonyl)-2-hydroxy-2-méthylpropiono-<i>m</i>-toluidiure dans une dispersion solide avec PVP. Dans un mode de réalisation, > 50 % du médicament se présente sous la forme de l'énantiomère R. L'invention concerne également une dose pharmaceutique quotidienne du médicament fourni par cette formulation. De plus, l'invention concerne l'utilisation de PVP dans une dispersion solide avec le médicament (dans un mode de réalisation dans lequel > 50 % du 4'-cyano-.alpha.', .alpha.', .alpha.'-trifluoro-3-(4-fluorophénylsulfonyl)-2-hydroxy-2-méthylpropiono-<i>m</i>-toluidiure se présente sous la forme de l'énantiomère R) afin d'augmenter la biodisponibilité du médicament; de manière à réduire la variabilité entre patients des concentrations dans le plasma du médicament; afin d'améliorer la stabilité de stockage du médicament ou afin de traiter et/ou réduire le risque de cancer de la prostate chez un patient.

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