IP Library Granted Patent US 8,071,613
Granted Patent B2
US 8,071,613 · App. 11/142,251 · Granted Dec 6, 2011

Anti-constipation composition

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Quick Facts
Patent No.
US 8,071,613
App. No.
11/142,251
Granted
Dec 6, 2011
Kind
B2
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): where X 1 and X 2 are preferably both fluorine atoms. The composition can be used to treat constipation without substantive side-effects, such as stomachache.

Claims (26)

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.

Assignments (6)
RELEASE OF SECURITY INTEREST Recorded Aug 14, 2025
From: ACQUIOM AGENCY SERVICES LLC
To: SPECGX LLC; MALLINCKRODT ENTERPRISES LLC; MALLINCKRODT LLC; MALLINCKRODT PHARMA IP TRADING UNLIMITED COMPANY; MALLINCKRODT PHARMACEUTICALS IRELAND LIMITED; OCERA THERAPEUTICS LLC; STRATATECH CORPORATION; SUCAMPO PHARMA AMERICAS LLC; VTESSE LLC
Reel/Frame 072324/0740 →
RELEASE OF PATENT SECURITY INTERESTS RECORDED AT REEL 060434, FRAME 0536 Recorded Nov 16, 2023
From: DEUTSCHE BANK AG NEW YORK BRANCH, AS COLLATERAL AGENT
To: MALLINCKRODT ENTERPRISES LLC; MALLINCKRODT LLC; SPECGX LLC; OCERA THERAPEUTICS, INC.; STRATATECH CORPORATION; VTESSE LLC; MALLINCKRODT PHARMA IP TRADING UNLIMITED COMPANY; MALLINCKRODT PHARMACEUTICALS IRELAND LIMITED; SUCAMPO PHARMA AMERICAS LLC
Reel/Frame 065601/0347 →
RELEASE OF SECURITY INTERESTS IN PATENTS AT REEL 060389/FRAME 0913 Recorded Nov 15, 2023
From: WILMINGTON SAVINGS FUND SOCIETY, FSB, AS SECOND LIEN COLLATERAL AGENT
To: OCERA THERAPEUTICS LLC (F/K/A OCERA THERAPEUTICS, INC.); MALLINCKRODT LLC; MALLINCKRODT ENTERPRISES LLC; MALLINCKRODT PHARMA IP TRADING UNLIMITED COMPANY; SPECGX LLC; STRATATECH CORPORATION; SUCAMPO PHARMA AMERICAS LLC; VTESSE LLC; MALLINCKRODT PHARMACEUTICALS IRELAND LIMITED
Reel/Frame 065583/0465 →
SECURITY INTEREST Recorded Nov 15, 2023
From: MALLINCKRODT ENTERPRISES LLC; MALLINCKRODT LLC; MALLINCKRODT PHARMA IP TRADING UNLIMITED COMPANY; MALLINCKRODT PHARMACEUTICALS IRELAND LIMITED; OCERA THERAPEUTICS LLC; SPECGX LLC; STRATATECH CORPORATION; SUCAMPO PHARMA AMERICAS LLC; VTESSE LLC
To: ACQUIOM AGENCY SERVICES LLC
Reel/Frame 065595/0376 →
NOTICE OF GRANT OF SECURITY INTEREST IN INTELLECTUAL PROPERTY Recorded Jun 22, 2022
From: MALLINCKRODT ENTERPRISES LLC; MALLINCKRODT LLC; SPECGX LLC; OCERA THERAPEUTICS, INC.; STRATATECH CORPORATION; SUCAMPO PHARMA AMERICAS LLC; VTESSE LLC; MALLINCKRODT PHARMACEUTICALS IRELAND LIMITED; MALLINCKRODT PHARMA IP TRADING UNLIMITED COMPANY
To: DEUTSCHE BANK AG NEW YORK BRANCH
Reel/Frame 060434/0536 →
SECURITY INTEREST Recorded Jun 17, 2022
From: MALLINCKRODT ENTERPRISES LLC; MALLINCKRODT LLC; SPECGX LLC; OCERA THERAPEUTICS, INC.; STRATATECH CORPORATION; SUCAMPO PHARMA AMERICAS LLC; VTESSE LLC; MALLINCKRODT PHARMACEUTICALS IRELAND LIMITED
To: WILMINGTON SAVINGS FUND SOCIETY, FSB, AS SECOND LIEN COLLATERAL AGENT
Reel/Frame 060389/0913 →