Colonic purgative composition with soluble binding agent

• US 8,507,009 B2
• Filed: 01/20/2010
• Issued: 08/13/2013
• 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: Skiendzielewski, Stephen, Rose, Martin, Do, Ngoc
• Primary Examiner(s): FISHER, ABIGAIL L
• Application Number:
  US12/690,384
• Publication Number:
  US 20100159026A1
• Time in Patent Office: 1,301 Days
• Field of Search: 424/606, 424/466, 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 making a solid dosage colonic purgative formulation in a tablet form, comprising:

heating a formulation comprising sodium phosphate and polyethylene glycol 8000 to a temperature not exceeding the melting point of the polyethylene glycol; and

compressing the formulation into a tablet.

2. The method of claim 1, wherein the formulation comprises monobasic sodium phosphate and dibasic sodium phosphate.

3. The method of claim 1, wherein the method comprises cooling the formulation to below 30°

C. prior to compression.

4. The method of claim 3, wherein the method comprises cooling the formulation overnight at room temperature prior to compression.

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

6. The method of claim 5, wherein the lubricant comprises magnesium stearate.

7. The method of claim 1, wherein the formulation comprises between 7.5% and 15% of polyethylene glycol by weight.

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

9. The method of claim 1, wherein each tablet of the formulation comprises about 1100 milligrams of sodium phosphate monobasic.

10. The method of claim 9, wherein each tablet of the formulation comprises about 398 milligrams of sodium phosphate dibasic.

11. The method of claim 10, wherein each tablet of the formulation comprises about 8.4 milligrams of magnesium stearate.

21. The method of claim 1, wherein the step of heating a formulation comprising sodium phosphate and polyethylene glycol to the melting point of the polyethylene glycol further comprises mixing the formulation at a speed of about 10 rpm to about 100 rpm.

12. A method of making a solid dosage colonic purgative tablet formulation, comprising:

heating a formulation comprising 60%-90% sodium phosphate and 5% to 20% polyethylene glycol 8000 to a temperature not exceeding the melting point of polyethylene glycol;

allowing the formulation to cool below 30°

C.; and

compressing the formulation into tablets.

13. The method of claim 12, wherein each of said tablets comprises about 1102 milligrams of sodium phosphate monobasic and about 398 milligrams of sodium phosphate dibasic.

14. The method of claim 12, comprising adding magnesium stearate after the formulation has cooled below 30°

C.

15. The method of claim 12, wherein the mixture is allowed to cool down overnight prior to compressing the formulation into tablets.

16. The method of claim 12, wherein each of the tablets comprises about 10% w/w of polyethylene glycol 8000.

17. The method of claim 12, wherein the heating comprises heating the formulation to a temperature of about 54°

C. to 55°

C.

18. The method of claim 12, wherein the tablets weigh about 1676 mg following compression.

19. The method of claim 12, wherein the formulation comprises about 90% sodium phosphate.

20. The method of claim 12, wherein the formulation comprises about 10% polyethylene glycol 8000.

22. The method of claim 12, wherein the step of heating a formulation comprising 60%-90% sodium phosphate and 5% to 20% polyethylene glycol 8000 to a temperature not exceeding the melting point of polyethylene glycol further comprises mixing the formulation at a speed of about 10 rpm to about 100 rpm.