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Claims for Patent: 8,324,283

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Claims for Patent: 8,324,283

Title:Solid pharmaceutical compositions comprising a SIP receptor agonist and a sugar alcohol
Abstract: A solid pharmaceutical composition suitable for oral administration, comprising: (a) a S1P receptor agonist; and (b) a sugar alcohol.
Inventor(s): Oomura; Tomoyuki (Oita, JP), Pudipeddi; Madhusudhan (Edison, NJ), Ruegger; Colleen (Morris Plains, NJ), Royce; Alan E (Saylorsburg, PA), Sasaki; Masaki (Oita, JP), Tamura; Tokuhiro (Fukuoka, JP)
Assignee: Novartis AG (Basel, CH) Mitsubishi Pharma Corporation (Osaka, JP)
Application Number:12/189,323
Patent Claims: 1. A solid pharmaceutical composition suitable for oral administration, comprising: (a) a S1P receptor agonist which is selected from 2-amino-2-[4-(3-benzyloxyphenoxy)-2-chlorophenyl]propyl-1,3-propane-diol or 2-amino-2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]propyl-1,3-propane- -diol, 2-amino-2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-ethyl-1,3-pr- opane-diol, and its phosphates or a pharmaceutically acceptable salt thereof; and (b) a sugar alcohol.

2. The composition of claim 1, wherein the salt is the hydrochloride.

3. A composition according to claim 1, wherein the sugar alcohol is a non-hygroscopic sugar alcohol or a mixture thereof.

4. A composition according to claim 1, wherein the sugar alcohol comprises mannitol.

5. A composition according to claim 1, further comprising a lubricant.

6. A composition according to claim 5, wherein the lubricant comprises magnesium stearate.

7. A composition according to claim 1, comprising 0.01 to 20% by weight of the S1P receptor agonist.

8. A composition according to claim 7, comprising 0.5 to 5% by weight of the S1P receptor agonist.

9. A composition according to claim 1, comprising 75 to 99.99% by weight of the sugar alcohol.

10. A composition according to claim 9, comprising 90 to 99.5% by weight of the sugar alcohol.

11. A composition according to claim 5, comprising 0.01 to 5% by weight of the lubricant.

12. A composition according to claim 11, comprising 1.5 to 2.5% by weight of the lubricant.

13. A composition according to claim 1, wherein the S1P receptor agonist is micronized.

14. A composition according to claim 13, wherein the S1P receptor agonist is pre-screened with a 400 to 500 .mu.m mesh screen.

15. A composition according to claim 1, in the form of a tablet.

16. A composition according to claim 1 in the form of a capsule.

17. A method of treating organ or tissue transplant rejection, graft versus host disease, an autoimmune disease, an inflammatory condition, viral myocarditis or a viral disease caused by viral myocarditis in a subject in need thereof, comprising administering to said subject a pharmaceutical composition according to claim 1.

18. A method according to claim 17, wherein the disease or condition that is treated is multiple sclerosis.

19. A solid pharmaceutical composition suitable for oral administration, comprising mannitol and 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or a pharmaceutically acceptable salt thereof.

20. A composition according to claim 19, further comprising a lubricant.

21. A composition according to claim 20, wherein the lubricant comprises magnesium stearate.

22. A composition according to claim 19, wherein the compound 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol, or a pharmaceutically acceptable salt thereof, is present in an amount of 0.5 to 5% by weight, based on the total weight of the composition.

23. A composition according to claim 19, wherein mannitol is present in an amount of 90 to 99.5% by weight, based on the total weight of the composition.

24. A composition according to claim 19, wherein the lubricant is present in an amount of 1.5 to 2.5% by weight, based on the total weight of the composition.

25. A composition according to claim 19, wherein said composition is in the form of a tablet.

26. A composition according to claim 19, wherein said composition is in the form of a capsule.

27. A composition according to claim 19, wherein the mannitol has a mean particle size of 100 to 300 .mu.m.

28. A composition according to claim 27, wherein the mannitol has a mean particle size of 150 to 250 .mu.m.

29. A composition according to claim 19, wherein the mannitol has a bulk density of 0.4 to 0.6 g/mL.

30. A composition according to claim 29, wherein the mannitol has a bulk density of 0.45 to 0.55 g/mL.

31. A composition according to claim 19, wherein the mannitol has a single point surface area of 1 m.sup.2/g to 7 m.sup.2/g.

32. A pharmaceutical composition according to claim 1, wherein the S1P receptor agonist is 2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol or a pharmaceutically acceptable salt thereof.
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