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Claims for Patent: 8,258,132

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Claims for Patent: 8,258,132

Title:Pharmaceutical composition of a tachykinin receptor antagonist
Abstract: The present invention is directed to novel pharmaceutical compositions of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)phen- yl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine. The pharmaceutical compositions of this invention useful in the treatment or prevention of disorders such as psychiatric disorders including depression and anxiety, inflammatory diseases and emesis.
Inventor(s): Bosch; H. William (Bryn Mawr, PA), Liversidge; Elaine (West Chester, PA), Shelukar; Suhas D. (Lansdale, PA), Thompson; Karen C. (Lansdale, PA)
Assignee: Merck Sharp & Dohme Corp. (Rahway, NJ)
Application Number:10/317,948
Patent Claims: 1. A nanoparticulate composition comprising the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)phen- yl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine, or a pharmaceutically acceptable salt thereof, the compound having adsorbed on the surface thereof at least one surface stabilizer in an amount sufficient to maintain an effective average particle size of less than 400 nm, wherein the surface stabilizer is selected from the group consisting of hydroxypropyl cellulose-super low viscosity and sodium lauryl sulfate.

2. The composition of claim 1 wherein the nanoparticles have an effective average particle size of less than 250 nm.

3. A pharmaceutical composition comprising the nanoparticulate composition of claim 1 and a pharmaceutically acceptable carrier.

4. A pharmaceutical composition comprising the nanoparticulate composition of claim 1 which has been spray dried or spray coated on a solid support.

5. The pharmaceutical composition of claim 4 wherein the solid support is selected from microcrystalline cellulose spheres, sugar-starch spheres and lactose spheres.

6. A pharmaceutical composition comprising the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)phen- yl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine having a particle size of less than 400 nm, a surface stabilizer, a redispersing agent and a solid support, wherein the surface stabilizer is selected from the group consisting of hydroxypropyl cellulose-super low viscosity and sodium lauryl sulfate.

7. The pharmaceutical composition of claim 6 comprising about 5-60% by weight of 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-f- luoro)-phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine having a particle size of less than 400 nm; about 1-20% by weight of a surface stabilizer; about 0-50% by weight of a redispersing agent; about 0-90% by weight of a solid support; and about 0-5% by weight of a lubricant.

8. The pharmaceutical composition of claim 7 comprising about 25-50% by weight of 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-f- luoro)phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine having a particle size of less than 400 nm; about 5-15% by weight of a surface stabilizer; about 0-50% by weight of a redispersing agent; about 10-50% by weight of a solid support; and about 0-5% by weight of a lubricant.

9. A method for antagonizing the effect of substance P at its receptor site or for the blockade of neurokinin-1 receptors in a patient which comprises the administration to the patient of the composition of claim 1 in an amount that is effective for antagonizing the effect of substance P at its receptor site in the patient.

10. A method for treating emesis in a patient in need thereof which comprises administering to the patient an effective amount of the composition of claim 1.
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