Formulations For Cathepsin K Inhibitors
AssigneeMerck Sharp & Dohme Corp.
InventorsWayne Parent, Mahtab Afaghi, David Breslin, Mireille Granger, Lei Wang, Jeff Zimmerman
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Abstract
The instant invention relates to pharmaceutical compositions containing cathespin K inhibitors. Also disclosed are processes for making said pharmaceutical compositions.
Claims6
A pharmaceutical composition comprising by weight, 12.5% of N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide, or a pharmaceutically acceptable salt thereof, and 87.5% by weight of excipients selected from diluents, a binder, a lubricant, and a disintegrant, wherein the diluents are lactose monohydrate and microcrystalline cellulose;
- the binder is hydroxypropyl cellulose;
- the lubricant is magnesium stearate;
- and the disintegrant is croscarmellose sodium.
-11. (canceled)
An intravenous pharmaceutical composition comprising N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methyl sulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide, or a pharmaceutically acceptable salt thereof, water, a modified cyclodextrin and a wetting agent.
A pharmaceutical composition comprising 50 mg N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methyl sulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide, or a pharmaceutically acceptable salt thereof, 160 mg of lactose monohydrate;
- 160 mg of microcrystalline cellulose;
- 16 mg of croscarmellose sodium;
- 12 mg of hydroxypropyl cellulose and 2 mg of magnesium stearate.
The pharmaceutical composition of claim 15 comprising 50 mg N1-(1-cyanocyclopropyl)-4-fluoro-N2-{(1S)-2,2,2-trifluoro-1-[4′-(methylsulfonyl)-1,1′-biphenyl-4-yl]ethyl}-L-leucinamide, 160 mg of lactose monohydrate;
- 160 mg of microcrystalline cellulose;
- 16 mg of croscarmellose sodium;
- 12 mg of hydroxypropyl cellulose and 2 mg of magnesium stearate.
Dependencies are inferred from the claim text.