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Claims for Patent: 8,071,613

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Claims for Patent: 8,071,613

Title:Anti-constipation composition
Abstract: An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in a ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): ##STR00001## where X.sub.1 and X.sub.2 are preferably both fluorine atoms. The composition can be used to treat constipation without substantive side-effects, such as stomachache.
Inventor(s): Ueno; Ryuji (Potomac, MD)
Assignee: Sucampo AG (Zurich, CH)
Application Number:11/142,251
Patent Claims: 1. A method for relieving constipation in a constipated patient or cleansing the bowel of a patient, comprising administering to said patient a therapeutically effective amount of a composition comprising the bi-cyclic and mono-cyclic tautomers of 13,14-dihydro-15-keto-16,16-difluoro-prostaglandin E1, wherein the ratio of the bi-cyclic to mono-cyclic tautomer is at least 1:1.

2. The method according to claim 1, wherein the ratio of bi-cyclic to mono-cyclic tautomer is at least 20:1.

3. The method according to claim 1, wherein the ratio of bi-cyclic to mono-cyclic tautomer is about 96:4.

4. A method for relieving constipation in a constipated patient or cleansing the bowel of a patient, comprising administering to said patient a therapeutically effective amount of a composition comprising the bi-cyclic and mono-cyclic tautomers of 13,14-dihydro-15-keto-16,16-difluoro-prostaglandin E1,and at least one medium fatty acid triglyceride, wherein the ratio of the bi-cyclic to mono-cyclic tautomer is at least 1:1.

5. The method according to claim 4, wherein said medium chain fatty acid triglyceride is a triglyceride of fatty acid having 6-14 carbon atoms.

6. The method according to claim 4, wherein the triglyceride is present in an amount of 1-1,000,000 parts by weight based on one part by weight of the bi-cyclic structure.

7. The method according to claim 4, wherein the triglyceride is present in an amount of 5-500,000 parts by weight based on one part by weight of the bi-cyclic structure.

8. The method according to claim 4, wherein the triglyceride is present in an amount of 10-200,000 parts by weight based on one part by weight of the bi-cyclic structure.

9. The method according to claim 4, wherein said triglyceride is caprylic acid triglyceride and/or capric acid triglyceride.

10. The method according to claim 4, wherein the ratio of bi-cyclic to mono-cyclic tautomer is at least 20:1.

11. The method according to claim 4, wherein the ratio of bi-cyclic to mono-cyclic tautomer is about 96:4.

12. The method according to claim 1, wherein the composition is free of water.

13. The method according to claim 4, wherein the composition is free of water.

14. A method for treating constipation in a constipated patient or cleansing the bowel of a patient, comprising administering to said patient a therapeutically effective amount of a composition comprising the bi-cyclic and mono-cyclic tautomers of 13,14-dihydro-15-keto-16,16-difluoro-prostaglandin E1, wherein the ratio of the bi-cyclic to mono-cyclic tautomer is at least 1:1.

15. The method according to claim 14, wherein the ratio of bi-cyclic to mono-cyclic tautomer is at least 20:1.

16. The method according to claim 14, wherein the ratio of bi-cyclic to mono-cyclic tautomer is about 96:4.

17. The method according to claim 14, wherein the tautomers are present in the absence of water in the composition.

18. A method for treating constipation in a constipated patient or cleansing the bowel of a patient, comprising administering to said patient a therapeutically effective amount of a composition comprising the bi-cyclic and mono-cyclic tautomers of 13,14-dihydro-15-keto-16,16-difluoro-prostaglandin E1, and at least one medium fatty acid triglyceride, wherein the ratio of the bi-cyclic to mono-cyclic tautomer is at least 1:1.

19. The method according to claim 18, wherein said medium chain fatty acid triglyceride is a triglyceride of a fatty acid having 6-14 carbon atoms.

20. The method according to claim 18, wherein the triglyceride is present in an amount of 1-1,000,000 parts by weight based on one part by weight of the bi-cyclic structure.

21. The method according to claim 18, wherein the triglyceride is present in an amount of 5-500,000 parts by weight based on one part by weight of the bi-cyclic structure.

22. The method according to claim 18, wherein the triglyceride is present in an amount of 10-200,000 parts by weight based on one part by weight of the bi-cyclic structure.

23. The method according to claim 18, wherein said triglyceride is caprylic acid triglyceride and/or capric acid triglyceride.

24. The method according to claim 18, wherein the ration of bi-cyclic to mono-cyclic tautomer is at least 20:1.

25. The method according to claim 18, wherein the ratio of bi-cyclic to mono-cyclic tautomer is about 96:4.

26. The method according to claim 18, wherein the tautomers are present in the absence of water in the composition.
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