Colonic purgative composition with soluble binding agent

• US 7,718,197 B2
• Filed: 03/13/2008
• Issued: 05/18/2010
• Est. Priority Date: 11/19/2003
• Status: Active Grant

• Current Assignee: Salix Pharmaceuticals Limited (Bausch Health Cos., Inc.)
• Original Assignee: Salix Pharmaceuticals Limited (Bausch Health Cos., Inc.)
• Inventors: Do, Ngoc, Skiendzielewski, Stephen, Rose, Martin
• Primary Examiner(s): Richter; Johann R
• Assistant Examiner(s): FISHER, ABIGAIL L
• Application Number:
  US12/075,772
• Publication Number:
  US 20080213393A1
• Time in Patent Office: 796 Days
• Field of Search: 424/606, 424/464, 514/75
• US Class Current: 424/606
• 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 31/77 of oxiranes
• CPC Class Codes: A61K 33/00 Medicinal preparations containing inorganic active ingredients
• CPC Class Codes: A61K 33/06 Aluminium, calcium or magnesium; Compounds thereof , e.g. clay
• CPC Class Codes: A61K 33/42 Phosphorus; Compounds thereof
• CPC Class Codes: A61K 36/47 Euphorbiaceae (Spurge family), e.g. Ricinus (castorbean)
• CPC Class Codes: A61K 36/886 Aloeaceae (Aloe family), e.g. aloe vera
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/10 Laxatives

Abstract

This invention relates to novel colonic purgative compositions in a solid dosage form, comprising at least one purgative and at least one soluble, or soluble, nonfermentable binder, such as polyethylene glycol. Further, this invention relates to methods of using the colonic purgative compositions. The present compositions and methods are designed to improve patient tolerance and compliance, while at the same time improving the quality of bowel cleansing. The formulations and methods of this invention are particularly useful to cleanse the bowel prior to diagnostic and surgical procedures and can also be employed in lower dosages as a laxative to promote elimination and/or to relieve constipation.

Claims

1. A method of treating a patient with, or susceptible to, a gastrointestinal disorder comprising

(a) orally administering to the patient a formulation in a solid dosage tablet form, wherein each tablet comprises between 7.5% and 15% of polyethylene glycol having an average molecular weight of 7,000 to 9,000 daltons, and about 1.5 grams of sodium phosphate, wherein the polyethylene glycol is admixed with the sodium phosphate in the tablet to maintain the tablet form, and

(b) maintaining or promoting the elimination of feces in the bowel.

2. The method of claim 1, wherein the gastrointestinal disorder comprises constipation.

6. The method of claim 1, wherein the patient is administered the formulation in at least one application.

7. The method of claim 1, wherein the formulation comprises a total daily dosage of 6 g sodium phosphate.

8. The method of claim 7, wherein the dosage produces mild catharsis.

9. The method of claim 1, wherein the formulation comprises a total daily dosage of 12 g sodium phosphate.

10. The method of claim 9, wherein the dosage produces mild catharsis.

11. The method of claim 1, wherein the sodium phosphate comprises monobasic sodium phosphate and/or dibasic sodium phosphate.

12. The method of claim 1, wherein the method further comprises administration of a non-osmotic purgative.

13. The method of claim 12, wherein the non-osmotic purgative comprises mineral oil, aloe, bisacodyl, sodium picosulfate, casanthranol, cascara, castor oil, danthron, dehydrocholic acid, phenolphthalein, sennosides, docusate, bethanachol, colchicines, misoprostol, cisapride, norcisapride, paraffin, rhein, and/or tegaserod.

14. The method of claim 12, wherein the non-osmotic purgative comprises bisacodyl and/or picosulfate.

15. The method of claim 1, wherein the formulation further comprises a stimulant laxative.

16. The method of claim 1, wherein the polyethylene glycol has an average molecular weight of 8,000.

17. The method of claim 1, wherein the formulation further comprises a lubricant.

18. The method of claim 17, wherein the lubricant comprises magnesium stearate.

19. The method of claim 1, wherein the formulation comprises 10% polyethylene glycol by weight.

3. A method of treating a patient suffering from, or susceptible to, constipation due to administration of a medication comprising:

(a) orally administering to the patient a formulation in a solid dosage tablet form, wherein each tablet comprises between 7.5% and 15% of polyethylene glycol having an average molecular weight of 7,000 to 9,000 daltons, and about 1.5 grams of sodium phosphate, wherein the polyethylene glycol is admixed with the sodium phosphate in the tablet to maintain the tablet form; and

(b) maintaining or promoting the elimination of feces in the bowel.

4. The method of claim 3, wherein the medication is chosen from the group consisting of antacids that contain aluminum;

antidepressants;

blood pressure medications;

calcium channel blockers;

calcium supplements;

chemotherapy medications;

cold medicines;

antihistamines;

diuretics;

iron supplements;

medications for Parkinson'"'"'s disease;

lipid-lowering agents;

pain medications;

opiates;

codeine; and

tranquilizers.

20. The method of claim 3, wherein the patient is administered the colonic purgative formulation in at least one application.

21. The method of claim 3, wherein the formulation comprises a total daily dosage of 6 g sodium phosphate.

22. The method of claim 21, wherein the dosage produces mild catharsis.

23. The method of claim 3, wherein the formulation comprises a total daily dosage of 12 g sodium phosphate.

24. The method of claim 23, wherein the dosage produces mild catharsis.

25. The method of claim 3, wherein the sodium phosphate comprises monobasic sodium phosphate and dibasic sodium phosphate.

26. The method of claim 3, wherein the formulation farther comprises a stimulant laxative.

27. The method of claim 3, wherein the polyethylene glycol has an average molecular weight of 8,000.

28. The method of claim 3, wherein the formulation further comprises a lubricant.

29. The method of claim 28, wherein the lubricant comprises magnesium stearate.

30. The method of claim 3, wherein the formulation comprises 10% polyethylene glycol by weight.

5. A method of treating a patient suffering from, or susceptible to, constipation comprising

(a) orally administering to the patient a formulation in a solid dosage tablet form, wherein each tablet comprises between 7.5% and 15% of polyethylene glycol having an average molecular weight of 7,000 to 9,000 daltons, and about 1.5 grams of sodium phosphate, wherein the polyethylene glycol is admixed with the sodium phosphate in the tablet to maintain the tablet form, and

(b) maintaining or promoting the elimination of feces in the bowel, wherein the constipation is due to at least one of travel;

change in daily routine;

lack of exercise;

immobility caused by injury, illness, or aging;

dehydration;

irritable bowel syndrome;

pregnancy;

diabetes;

hypothyroidism;

hypercalcemia;

cancer of the colon or rectum;

uterine prolapse;

vaginal vault prolapse;

rectal prolapse;

scarring from surgery;

injury of the colon or rectum;

Parkinson'"'"'s disease;

multiple sclerosis;

stroke;

hemorrhoids or anal fissures;

delaying bowel movements;

anxiety;

depression;

eating disorders; and

obsessive-compulsive disorder.

31. The method of claim 5, wherein the formulation comprises a total daily dosage of 6 g sodium phosphate.

32. The method of claim 5, wherein the dosage produces mild catharsis.

33. The method of claim 5, wherein the formulation comprises a total daily dosage of 12 g sodium phosphate.

34. The method of claim 5, wherein the sodium phosphate comprises monobasic sodium phosphate and dibasic sodium phosphate.

35. The method of claim 5, wherein the polyethylene glycol has an average molecular weight of 8,000.

36. The method of claim 5, wherein the formulation further comprises a lubricant.

37. The method of claim 36, wherein the lubricant comprises magnesium stearate.

38. The method of claim 5, wherein the formulation comprises 10% polyethylene glycol by weight.