Colon cleansing compositions and methods

• US 20070086978A1
• Filed: 12/08/2006
• Published: 04/19/2007
• Est. Priority Date: 10/25/2002
• Status: Active Grant

• Current Assignee: Norgine B.V.
• Original Assignee: Norgine Europe B.V.
• Inventors: Barras, Norman, Cox, Ian
• Granted Patent: US 7,658,914 B2
• Time in Patent Office: Days
• US Class Current: 424/78.380
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/375 Ascorbic acid, i.e. vitamin C; Salts thereof
• CPC Class Codes: A61K 31/765 Polymers containing oxygen
• CPC Class Codes: A61K 33/00 Medicinal preparations containing inorganic active ingredients
• CPC Class Codes: A61K 33/04 Sulfur, selenium or tellurium; Compounds thereof
• CPC Class Codes: A61K 33/06 Aluminium, calcium or magnesium; Compounds thereof , e.g. clay
• CPC Class Codes: A61K 33/14 Alkali metal chlorides; Alkaline earth metal chlorides
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/009 Sachets, pouches characterised by the material or function of the envelope with gastric retention A61K9/0065; sachets which are not administered but function merely as a container are classified according to the content, e.g. sachets comprising powder for reconstitution of a drink A61K9/0095
• CPC Class Codes: A61K 9/0095 Drinks; Beverages; Syrups; Compositions for reconstitution thereof, e.g. powders or tablets to be dispersed in a glass of water; Veterinary drenches A61K9/0007 takes precedence; eatable gels or foams A61K9/0056; oral mucosa adhesive forms A61K9/006
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/10 Laxatives
• CPC Class Codes: A61P 31/00 Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics

Abstract

A composition comprising, per litre of aqueous solution, from 30 to 350 g polyethylene glycol, from 3 to 20 g of an ascorbic acid component selected form the group consisting of ascorbic acid, a salt of ascorbic acid, or a mixture thereof, an alkali metal or alkaline earth metal sulphate, preferably from 1 to 15 g thereof, and optionally one or more electrolytes selected from sodium chloride, potassium chloride, and sodium hydrogen carbonate, and preferably also comprising flavourings, is effective in cleansing the gut in preparation for a endoscopy, especially colonoscopy. It is safer than conventional sodium phosphate-based gut cleansing compositions, and hence can be used for patients who would be at risk with sodium phosphate-based compositions, and is better tolerated than conventional PEG-based compositions, leading to better patient compliance and enabling effective out-patient use.

Claims

1. A dry composition for admixture with water wherein the dry composition comprises, per litre of aqueous solution to be made, the following components, the components of the composition being selected such that an aqueous solution made up to 1 litre has an osmolarity within the range of from 300 to 700 mOsmol/kg:

a) 80 to 350 g polyethylene glycol;

b) 3 to 20 g ascorbic acid, one or more salts of ascorbic acid or a mixture of ascorbic acid and one or more salts of ascorbic acid;

c) 1 to 15 g of an alkali metal or alkaline earth metal sulphate or a mixture of alkali metal or alkaline earth metal sulphates; and

d) optionally one or more electrolytes selected from sodium chloride, potassium chloride and sodium hydrogen carbonate.

2. The dry composition as claimed in claim 1, wherein an aqueous solution made up in 1 litre of water has an osmolarity of 330 mOsmol/kg or greater.

3. The dry composition as claimed in claim 1, wherein an aqueous solution made up in 1 litre of water has an osmolarity in the range 550 mOsmol/kg or lower.

4. The dry composition as claimed in claim 1, wherein the polyethylene glycol has an average molecular weight of 2000 Daltons or greater.

5. The dry composition as claimed in claim 1, wherein the polyethylene glycol has an average molecular weight of 4500 Daltons or lower.

6. The dry composition as claimed in claim 1, wherein the polyethylene glycol has an average molecular weight of 3350 or 4000 Daltons.

7. The dry composition as claimed in claim 1, comprising from 90 g or more of polyethylene glycol per litre.

8. The dry composition as claimed in claim 1, comprising from 150 g or less of polyethylene glycol per litre.

9. The dry composition as claimed in claim 1, comprising 100 g of polyethylene glycol per litre.

10. The dry composition as claimed in claim 1, comprising the alkali metal or alkaline earth metal sulphate or the mixture of alkali metal or alkaline earth metal sulphates in a quantity of 3 g or more per litre.

11. The dry composition as claimed in claim 1, comprising the alkali metal or alkaline earth metal sulphate or the mixture of alkali metal or alkaline earth metal sulphates in a quantity 9 g or less per litre.

12. The dry composition as claimed in claim 1, comprising the alkali metal or alkaline earth metal sulphate or the mixture of alkali metal or alkaline earth metal sulphates in a quantity of 7.5 g per litre.

13. The dry composition as claimed in claim 1, wherein the alkali metal or alkaline earth metal is magnesium.

14. The dry composition as claimed in claim 1, wherein the alkali metal or alkaline earth metal is sodium.

15. The dry composition as claimed in claim 1, which comprises sodium chloride.

16. The dry composition as claimed in claim 15, comprising sodium chloride in a quantity of 2 g or more per litre.

17. The dry composition as claimed in claim 1, which comprises potassium chloride.

18. The dry composition as claimed in claim 17, comprising potassium chloride in a quantity of from 0.5 g or more per litre.

19. The dry composition as claimed in claim 1, comprising ascorbic acid or a salt thereof in a quantity of 5 g or more per litre.

20. The dry composition as claimed in claim 1, comprising ascorbic acid or a salt thereof in a quantity of 15 g or less per litre.

21. The dry composition as claimed in claim 1, comprising sodium ascorbate.

22. The dry composition as claimed in claim 1, further comprising a flavouring.

23. The dry composition as claimed in claim 22, wherein the flavouring is lemon flavouring.

24. The dry composition as claimed in claim 1, further comprising a sweetener that is not a metabolic substrate for bacteria in the gut.

25. The dry composition as claimed in claim 1, further comprising a sweetener selected from the group consisting of aspartame, acesulfame K, saccharine and citric acid.

26. The dry composition as claimed in claim 1, in which the ascorbic acid and/or the salt of ascorbic acid is coated.

27. A colon cleansing preparation comprising an aqueous solution of a composition as claimed in claim 1.

28. A colon cleansing preparation sachet comprising the components of a composition as claimed in claim 1.

29. A colon cleansing composition kit comprising the components of a composition as claimed in claim 1, comprising at least two portions in which the ascorbic acid and/or the salts thereof are packaged in a first portion and the other components are packaged in a second portion.

30. A method of cleansing the colon of a mammal, comprising administering orally to the mammal a cleansing fluid comprising, per litre, the following components, the components being selected such that the cleansing fluid has an osmolarity within the range of from 300 to 700 mOsmol/kg:

a) 80 to 350 g polyethylene glycol;

b) 3 to 20 g ascorbic acid, one or more salts of ascorbic acid or a mixture of ascorbic acid and one or more salts of ascorbic acid;

c) 1 to 15 g of an alkali metal or alkaline earth metal sulphate or a mixture of alkali metal or alkaline earth metal sulphates; and

d) optionally one or more electrolytes selected from sodium chloride, potassium chloride and sodium hydrogen carbonate, the volume of fluid administered being from 1.5 to 3 litres for an adult human and pro rata for a mammal other than an adult human.

31. The method as claimed in claim 30, wherein the composition is administered over 1 to 4 hours.

32. The method as claimed in claim 30, wherein the colon is cleansed prior to carrying out a diagnostic, therapeutic or surgical procedure on the colon, rectum or anus or elsewhere in the abdomen.

33. A method as claimed in claim 30, wherein the colon is cleansed in the treatment of an acute gastrointestinal infection.

34. The method as claimed in claim 33, wherein the cleansing fluid is administered over a period of 1 to 4 hours.