Colonic purgative composition with soluble binding agent

• US 20080213393A1
• Filed: 03/13/2008
• Published: 09/04/2008
• Est. Priority Date: 11/19/2003
• Status: Active Grant

• Current Assignee: Salix Pharmaceuticals Incorporated (Bausch Health Cos., Inc.)
• Original Assignee: Salix Pharmaceuticals Incorporated (Bausch Health Cos., Inc.)
• Inventors: Do, Ngoc, Skiendzielewski, Stephen, Rose, Martin
• Granted Patent: US 7,718,197 B2
• Time in Patent Office: Days
• 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

1-29. -29. (canceled)

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

(a) administering to the patient the colonic purgative formulation in a solid dosage form comprising at least one soluble binder, wherein the at least one of the soluble binders comprises polyethylene glycol and a therapeutically effective amount of at least one purgative, and

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

31. The method of claim 30, wherein the gastrointestinal disorder comprises constipation.

35. The method of claim 30, wherein the patient is administered the colonic purgative formulation in at least one application.

36. The method of claim 30, wherein the administration occurs orally, through a feeding tube, or through a nasogastric tube.

38. The method of claim 30, wherein the formulation comprises a total daily dosage of 6 g sodium phosphate.

39. The method of claim 38, wherein the dosage produces mild catharsis.

40. The method of claim 30, wherein the formulation comprises a total daily dosage of 12 g sodium phosphate.

41. The method of claim 40, wherein the dosage produces mild catharsis.

42. The method of claim 30, wherein the purgative comprises an osmotic purgative.

43. The method of claim 42, wherein the osmotic purgative comprises magnesium citrate, magnesium chloride, magnesium hydroxide, magnesium phosphate, magnesium sulfate, magnesium tartrate, sodium phosphate, sodium tartrate, sodium sulfate, potassium tartrate, magnesium oxide, and/or sodium sulfate, and salts thereof.

44. The method of claim 43, wherein the sodium phosphate salt comprises monobasic sodium phosphate, dibasic sodium phosphate, and/or tribasic sodium phosphate.

45. The method of claim 30, wherein the at least one purgative comprises a non-osmotic purgative.

46. The method of claim 45, wherein the at least one 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.

47. The method of claim 45, wherein the at least one non-osmotic purgative comprises bisacodyl and/or picosulfate.

48. The method of claim 30, wherein the at least one purgative comprises a stimulant laxative.

49. The method of claim 42, wherein the formulation further comprises at least one non-osmotic purgative selected from one or more of mineral oil, aloe, bisacodyl, sodium picosulfate, casanthranol, cascara, castor oil, danthron, dehydrocholic acid, phenolphthalein, sennosides, docusate, bethanachol, colchicines, misoprostol, cisapride, norcisapride, paraffin, rhein, and tegaserod.

50. The method of claim 42, wherein the formulation further comprises at least one stimulant laxative.

51. The method of claim 42, wherein the formulation further comprises at least one bulk-forming purgative.

52. The method of claim 42, wherein the at least one bulk-forming purgative comprises methylcellulose, sodium carboxymethyl cellulose, bran, psyllium, sterculia, and/or testa ispaghula.

53. The method of claim 30, wherein the polyethylene glycol comprises an average molecular weight of at least 1,000.

54. The method of claim 30, wherein the polyethylene glycol comprises an average molecular weight of from 7,000 to 9,000.

55. The method of claim 30, wherein the polyethylene glycol comprises an average molecular weight of 8,000.

56. The method of claim 30, wherein the formulation further comprises a lubricant.

57. The method of claim 30, wherein the lubricant comprises magnesium stearate.

58. The method of claim 30, wherein the solid dosage form comprises a tablet, capsule, or caplet.

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

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

(a) administering to the patient the colonic purgative formulation in a solid dosage form comprising at least one soluble binder, wherein at least one of the soluble binders comprises polyethylene glycol and a therapeutically effective amount of at least one purgative, 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.

37. (canceled)