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Last Updated: November 22, 2024

Claims for Patent: 10,828,298


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Summary for Patent: 10,828,298
Title:Pharmaceutical composition containing 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy]-N-(methylsu- lfonyl)acetamide
Abstract: A stabilized solid preparation containing 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsu- lfonyl)acetamide is provided, namely, a solid preparation containing 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsu- lfonyl)acetamide and D-mannitol having a specific surface area of 1.0 m.sup.2/g or less.
Inventor(s): Furuta; Shouji (Kyoto, JP), Mukai; Hironori (Kyoto, JP)
Assignee: NIPPON SHINYAKU CO., LTD. (Kyoto, JP)
Application Number:16/044,821
Patent Claims: 1. A tablet comprising: 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsu- lfonyl)acetamide; and D-mannitol having a specific surface area of larger than 0.2 m.sup.2/g and smaller than 0.7 m.sup.2/g; wherein the content of D-mannitol is: (a) such that the weight of D-mannitol is from 5 to 10000 parts by weight with respect to 1 part by weight of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsu- lfonyl)acetamide, (b) from 10 to 99 wt % of the total weight of the tablet, and (c) 20 wt % or more of the total weight of diluents contained in the tablet.

2. The tablet according to claim 1, wherein the amount of D-mannitol is from 10 to 9500 parts by weight with respect to 1 part by weight of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsu- lfonyl)acetamide.

3. The tablet according to claim 1, wherein the amount of 2-{4-[N-(5,6-diphenylpyrazin-2-yl)-N-isopropylamino]butyloxy}-N-(methylsu- lfonyl)acetamide is from 0.1 to 2 wt % of the total weight of the tablet.

4. The tablet according to claim 3, wherein the amount of D-mannitol is from 15 to 95 wt % of the total weight of the tablet.

5. The tablet according to claim 3, further comprising one substance selected from the group consisting of cornstarch, sucrose, and crystalline cellulose.

6. The tablet according to claim 3, further comprising hydroxypropyl cellulose.

7. The tablet according to claim 3, further comprising magnesium stearate.

8. The tablet according to claim 4, further comprising one substance selected from the group consisting of cornstarch, sucrose, and crystalline cellulose.

9. The tablet according to claim 4, further comprising hydroxypropyl cellulose.

10. The tablet according to claim 4, further comprising magnesium stearate.

11. The tablet according to claim 8, further comprising hydroxypropyl cellulose.

12. The tablet according to claim 8, further comprising magnesium stearate.

13. The tablet according to claim 11, further comprising magnesium stearate.

14. The tablet according to claim 1, wherein the amount of D-mannitol is from 15 to 95 wt % of the total weight of the tablet.

15. The tablet according to claim 1, further comprising one substance selected from the group consisting of cornstarch, sucrose, and crystalline cellulose.

16. The tablet according to claim 15, further comprising hydroxypropyl cellulose.

17. The tablet according to claim 15, further comprising magnesium stearate.

18. The tablet according to claim 1, further comprising hydroxypropyl cellulose.

19. The tablet according to claim 1, further comprising magnesium stearate.

20. The tablet according to claim 1, which is used for treating pulmonary arterial hypertension.

21. A method for treating pulmonary arterial hypertension, the method comprising the step of administering the tablet according to claim 1 to a subject.

22. A method for treating pulmonary arterial hypertension, the method comprising the step of administering the tablet according to claim 3 to a subject.

23. A method for treating pulmonary arterial hypertension, the method comprising the step of administering the tablet according to claim 4 to a subject.

24. A method for treating pulmonary arterial hypertension, the method comprising the step of administering the tablet according to claim 8 to a subject.

25. A method for treating pulmonary arterial hypertension, the method comprising the step of administering the tablet according to claim 11 to a subject.

26. A method for treating pulmonary arterial hypertension, the method comprising the step of administering the tablet according to claim 17 to a subject.

27. A method for treating pulmonary arterial hypertension, the method comprising the step of administering the tablet according to claim 12 to a subject.

28. A method for treating pulmonary arterial hypertension, the method comprising the step of administering the tablet according to claim 13 to a subject.

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