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Generated: August 19, 2017

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Title:Pharmaceutical compositions
Abstract: The present invention relates to pharmaceutical compositions and, more particularly, to a pharmaceutical composition containing the compound {1S-[1.alpha.,2.alpha.,3.beta.(1S*,2R*),5.beta.]}-3-(7-{[2-(3,4-difluorop- henyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-- 3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol.
Inventor(s): Banks; Simon (Loughborough, GB)
Assignee: AstraZeneca AB (Sodertalje, SE)
Application Number:11/841,030
Patent Claims: 1. A pharmaceutical composition comprising: {1S-[1.alpha.,2.alpha.,3.beta.(1S*,2R*),5.beta.]}-3-(7-{[2-(3,4-difluorop- henyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-- 3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol as the active ingredient; and further comprising: a filler consisting essentially of a mixture of mannitol and dibasic calcium phosphate dihydrate; a binder consisting essentially of hydroxypropyl cellulose; a disintegrant consisting essentially of sodium starch glycolate; and one or more lubricants.

2. A pharmaceutical composition according to claim 1 wherein the lubricant is magnesium stearate or sodium stearyl fumarate.

3. A pharmaceutical composition according to claim 1 wherein {1S-[1.alpha.,2.alpha.,3.beta.(1S*,2R*),5.beta.]}-3-(7-{[2-(3,4-difluorop- henyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-- 3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol is present in an amount of 20 to 45% by weight of the pharmaceutical composition as a whole.

4. A pharmaceutical composition according to claim 1 wherein the filler is present in an amount of 20 to 70% by weight of the pharmaceutical composition as a whole.

5. A pharmaceutical composition according to claim 1 wherein the binder is present in an amount of 3 to 6% by weight of the pharmaceutical composition as a whole.

6. A pharmaceutical composition according to claim 1 wherein the disintegrant is present in an amount of 2 to 6% by weight of the pharmaceutical composition as a whole.

7. A pharmaceutical composition according to claim 1 wherein the lubricant is present in an amount of 0.5 to 1% by weight of the pharmaceutical composition as a whole.

8. A pharmaceutical composition according to claim 1 wherein {1S-[1.alpha.,2.alpha.,3.beta.(1S*,2R*),5.beta.]}-3-(7-{[2-(3,4-difluorop- henyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-- 3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol is substantially present in the form of Polymorph II.

9. A pharmaceutical composition according to claim 1 wherein {1S-[1.alpha.,2.alpha.,3.beta.(1S*,2R*),5.beta.]}-3-(7-{[2-(3,4-difluorop- henyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-- 3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol is substantially present in the form of Polymorph III.

10. A pharmaceutical composition according to claim 1 wherein: the lubricant is magnesium stearate.

11. A pharmaceutical composition according to claim 1 comprising: {1S-[1.alpha.,2.alpha.,3.beta.(1S*,2R*),5.beta.]}-3-(7-{[2-(3,4-difluorop- henyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-- 3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol in an amount of 20 to 45% by weight of the pharmaceutical composition as a whole; mannitol in an amount of 20 to 45% by weight of the pharmaceutical composition as a whole; dibasic calcium phosphate dihydrate in an amount of 10 to 30% by weight of the pharmaceutical composition as a whole; hydroxypropylcellulose in an amount of 3 to 6% by weight of the pharmaceutical composition as a whole; sodium starch glycolate in an amount of 2 to 6% by weight of the pharmaceutical composition as a whole; and lubricant in an amount of 0.5 to 3% by weight of the pharmaceutical composition as a whole.

12. A pharmaceutical composition according to claim 1 which has been prepared by a wet granulation process.

13. A pharmaceutical composition according to claim 1 which has been prepared by a high shear wet granulation process.

14. A pharmaceutical composition according to claim 1 wherein the combined amount of filler, binder, and disintegrant is 50 to 90% by weight of the pharmaceutical composition as a whole.

15. A pharmaceutical composition according to claim 1 wherein the active ingredient is admixed with filler, binder, disintegrant, and one or more lubricants.

16. A pharmaceutical composition according to claim 1 wherein the composition is a tablet.

17. A pharmaceutical composition according to claim 1 wherein the composition is a core tablet.

18. An oral immediate release pharmaceutical composition comprising: {1S-[1.alpha.,2.alpha.,3.beta.(1S*,2R*),5.beta.]}-3-(7-{[2-(3,4-difluorop- henyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-- 3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol substantially present in the form of Polymorph II in an amount of 20 to 45% by weight of the pharmaceutical composition as a whole; mannitol in an amount of 20 to 45% by weight of the pharmaceutical composition as a whole; dibasic calcium phosphate dihydrate in an amount of 10 to 30% by weight of the pharmaceutical composition as a whole; hydroxypropyl cellulose in an amount of 3 to 6% by weight of the pharmaceutical composition as a whole; sodium starch glycolate in an amount of 2 to 6% by weight of the pharmaceutical composition as a whole; and one or more lubricants in an amount of 0.5 to 3% by weight of the pharmaceutical composition as a whole.

19. An oral pharmaceutical composition consisting of: {1S-[1.alpha.,2.alpha.,3.beta.(1S*,2R*),5.beta.]}-3-(7-{[2-(3,4-difluorop- henyl)cyclopropyl]amino}-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-- 3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol substantially present in the form of Polymorph II in an amount of 20 to 45% by weight of the pharmaceutical composition as a whole; mannitol in an amount of 20 to 45% by weight of the pharmaceutical composition as a whole; dibasic calcium phosphate dihydrate in an amount of 10 to 30% by weight of the pharmaceutical composition as a whole; hydroxypropyl cellulose in an amount of 3 to 6% by weight of the pharmaceutical composition as a whole; sodium starch glycolate in an amount of 2 to 6% by weight of the pharmaceutical composition as a whole; and one or more lubricants in an amount of 0.5 to 3% by weight of the pharmaceutical composition as a whole.
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