Pharmaceutical composition with improved bioavailability

The invention relates to solid dispersions of poorly water soluble compounds, in particular 4-{ [(2R,3S,4R,5S)-4-(4-chloro-2-fluorophenyl)-3-(3-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-pyrrolidine-2-carbonyl]amino} -3-methoxy-benzoic acid, formed by solvent co-precipitation or spray dry...

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Bibliographic Details
Main Authors Ma, Hua, Sandhu, Harpreet K, Matchett, Michael Allen, Shah, Navnit Hargovindas, Zhang, Yu-E, Lomuscio, Steve
Format Patent
LanguageEnglish
Published 31.07.2020
Subjects
CHEMISTRY
COMPOSITIONS BASED THEREON
COMPOSITIONS OF MACROMOLECULAR COMPOUNDS
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
ORGANIC MACROMOLECULAR COMPOUNDS
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
THEIR PREPARATION OR CHEMICAL WORKING-UP
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Summary:The invention relates to solid dispersions of poorly water soluble compounds, in particular 4-{ [(2R,3S,4R,5S)-4-(4-chloro-2-fluorophenyl)-3-(3-chloro-2-fluorophenyl)-4-cyano-5-(2,2-dimethylpropyl)-pyrrolidine-2-carbonyl]amino} -3-methoxy-benzoic acid, formed by solvent co-precipitation or spray drying with a stabilising polymer, resulting in improved bioavailability, safety and tolerability of said compounds, and where in the stabilising polymer is poly(methacrylic acid)-co-methyl methacrylate (EUDRAGITR L-100), poly(methacrylic acid)-co-methyl methacrylate (Eudragit L100-55) or poly(vinylpyrrolidone-co-vinyl acetate) (6+4).
Bibliography:Application Number: NZ20140708272