SOLID PHARMACEUTICAL COMPOSITION COMPRISING 4-CYANO-TRIFLUORO-3(4-FLUOROPHENYL-SULPHONYL)-2-HYDROXY-2-METHYLPROPIONO-M TOLUIDIDE AND PVP

• Main Authors: BATEMAN, NICOLA FRANCES, CAHILL, JULIE KAY
• Format: Patent
• Language: English; Hungarian
• Published: 28.01.2004
• Edition: 7
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

A találmány szerinti, a humán gyógyászatban mukozális adagolásrafelhasznátható gyógyászati készítmények hatóanyagként (I) képletű 4'-ciano-a,'a',a'-trifluor-3-(4-fluor-fenil-szulfonil)-2-hidroxi-2-metil-propiono-m-toluididot tartalmaznak PVP-vet képezett szilárd diszperzióformájában. A készítményekben a 4'-ciano-a',a',a'-trifluor-3-(4-fluor-fenil-szulfonil)-2-hidroxi-2-metil-propiono-m-toluidid előnyösen többmint 50 %-a R enantiomer formájában van jelen. Ó 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 plasma concentrations 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.