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 dr...

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Main Authors SHAH NAVNIT HARGOVINDAS, MA HUA, ZHANG YU-E, LOMUSCIO STEVE, MATCHETT MICHAEL ALLEN, SANDHU HARPREET K
Format Patent
LanguageChinese
English
Published 19.02.2021
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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, resulting in improved bioavailability, safety and tolerability of said compounds. 本发明涉及通过溶剂共沉淀或喷雾干燥形成的水难溶性化合物,特别是4-{[(2R,3S,4R,5S)-4-(4-氯-2-氟苯基)-3-(3-氯-2-氟苯基)-4-氰基-5-(2,2-二甲基丙基)-吡咯烷-2-羰基]氨基}-3-甲氧基-苯甲酸的固体分散体,其导致所述化合物的改善的生物利用度、安全性和耐受性。
Bibliography:Application Number: CN202011052471