Micronized tanaproget, compositions, and methods of preparing the same

摘要

The present invention provides compositions, desirably pharmaceutical compositions, containing micronized tanaproget and methods of making the same. The present invention comprises a process for preparing a pharmaceutical composition comprising micronized tanaproget or a pharmaceutically acceptable salt thereof, said process comprising: (i) mixing a first portion of microcrystalline cellulose and a first portion of anhydrous lactose; (ii) mixing the product of step (i) with a second portion of anhydrous lactose; (iii) mixing the product of step (ii) with micronized tanaproget, micronized sodium thiosulfate pentahydrate, and micronized edetate calcium disodium hydrous; (iv) mixing the product of step (iii) with a first portion of croscarmellose sodium; (v) mixing the product of step (iv) with a second portion of microcrystalline cellulose and a third portion of anhydrous lactose; and (vi) mixing the product of step (v) with a first portion of magnesium stearate. The -resent invention further comprises a process for preparing a pharmaceutical composition comprising micronized tanaproget or a pharmaceutically acceptable salt thereof, said process comprising: (i) mixing a first portion of microcrystalline cellulose and a first portion of 5 anhydrous lactose; (ii) mixing a second portion of anhydrous lactose, micronized sodium thiosulfate pentahydrate, cysteine, and micronized edetate calcium disodium hydrous; (iii) mixing the products of steps (i) and (ii); (iv) mixing the product of step (iii) with micronized tanaproget; 10 (v) mixing the product of step (iv) with a third portion of anhydrous lactose; (vi) mixing the product of step (v) with a first portion of croscarmellose sodium; (vii) mixing the product of step (vi) with a second portion of microcrystalline cellulose and a fourth portion of anhydrous lactose; and (viii) mixing the product of step (vii) with a first portion of magnesium stearate.