Non-aqueous colonic purgative formulations

• US 6,162,464 A
• Filed: 03/31/1997
• Issued: 12/19/2000
• Est. Priority Date: 03/31/1997
• Status: Expired due to Term

• Current Assignee: Salix Pharmaceuticals Incorporated (Bausch Health Cos., Inc.)
• Original Assignee: InKine Pharmaceutical Co., Inc. (Bausch Health Cos., Inc.)
• Inventors: Jacob, Leonard S., Krell, Robert D., Williams, Taffy J.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): MCQUEENEY, PATRICIA E
• Application Number:
  US08/829,080
• Time in Patent Office: 1,359 Days
• Field of Search: 424/456, 424/464, 424/465, 424/451
• US Class Current: 424/456
• CPC Class Codes: A61K 31/19 Carboxylic acids, e.g. valproic acid salicylic acid A61K31/60
• 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 33/42 Phosphorus; Compounds thereof
• 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 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

Orally administered colonic purgative formulations and methods of its use for effecting partial or complete purgation of the colon in mammals, the formulations consisting of non-aqueous admixtures of a purgative salt selected from the group consisting of Mg₃ (PO₄)₂, MgHPO₄, Mg(H₂ PO₄)₂, MgSO₄, MgCl₂, Na₂ SO₄, sodium tartrate, potassium tartrate, magnesium tartrate and mixtures, thereof, administered in tablet or capsule form in purgative effective concentrations. Preferred embodiments make use of at least one or more magnesium phosphate salts, more preferably dibasic magnesium phosphate; other preferred embodiments include the addition of binders, dispersants and buffers which do not adversely affect osmolality or effectiveness of the purgative formulations.

Claims

1. An orally administerable composition in a solid dosage form capable of inducing purgation of the colon of a patient comprising a colonic purgative effective amount of a nonaqueous admixture of a salt selected from the group consisting of Mg₃ (PO₄)₂, MgHPO₄, Mg(H₂ PO₄)₂, MgSO₄, MgCl₂, Na₂ SO₄, sodium tartrate potassium tartrate, magnesium tartrate and mixtures, thereof, and wherein the purgation of the colon is sufficient to prepare the colon for a surgical or diagnostic procedure, wherein the composition in a solid dosage form can be administered directly to a patient in nonaqueous form.

2. The composition of claim 1, where the composition is in the form of a tablet.

3. The composition in a solid dosage form according to claim 1 wherein said salt is a phosphate salt.

4. The composition in a solid dosage form according to claim 3 wherein said phosphate salt is selected from the group consisting of monobasic magnesium phosphate, dibasic magnesium phosphate and tribasic magnesium phosphate.

5. The composition in a solid dosage form of claim 4 wherein said magnesium phosphate salt is included in an amount ranging from about 0.1 to about 1.2 grams per kilogram body weight of said patient.

6. The composition in a solid dosage form of claim 4 wherein said magnesium phosphate salt is dibasic magnesium phosphate included in an amount ranging from about 0.2 to about 0.7 grams per kilogram body weight of said patient.

7. The composition of claim 4, wherein the composition is in the form of a tablet.

8. The tablet of claim 2 further comprising a buffering agent selected from the group consisting of magnesium hydroxide, aluminum hydroxide, calcium carbonate and magnesium carbonate.

9. The tablet of claim 7 further comprising a buffering agent selected from the group consisting of magnesium hydroxide, aluminum hydroxide, calcium carbonate and magnesium carbonate.

10. The tablet of claim 2 further comprising a dispersal agent selected from the group consisting of anhydrous lactose, microcrystalline cellulose and a cross-linked starch.

11. The tablet of claim 9 further comprising a dispersal agent selected from the group consisting of anhydrous lactose, microcrystalline cellulose and a cross-linked starch.

12. The tablet of claim 2 further comprising a binding agent selected from the group consisting of non-ionic detergents, mechanical adhesives and microcrystalline cellulose.

13. The tablet claim 9 further comprising a binding agent selected from the group consisting of non-ionic detergents, mechanical adhesives and microcrystalline cellulose.

15. The method of claim 10 wherein step (a) further includes the step of adding to said purgative formulation at least one member selected from the group consisting of buffering agents, dispersal agents and binders.

24. The composition in a solid dosage form of claim 3 wherein said phosphate salt is dibasic magnesium phosphate or a mixture of dibasic magnesium phosphate and monobasic magnesium phosphate.

25. The composition in a solid dosage form of claim 1 wherein said salt is included in an amount ranging from about 0.05 grams per kilogram body weight to about 2.0 grams per kilogram body weight of said patient.

14. A method of inducing purgation of the colon in a patient comprising the steps of:

(a) preparing a non-aqueous admixture of a purgative salt selected from the group consisting of Mg₃ (PO₄)₂, MgHPO₄, Mg(H₂ PO₄)₂, MgSO₄, MgCl₂, Na₂ SO₄, sodium tartrate, potassium tartrate, magnesium tartrate and mixtures, thereof to form a purgative formulation;

(b) forming an orally administrable dosage form of said purgative formulation;

(c) orally administering a purgative effective dosage of said formulation to a patient; and

(d) allowing said administered dosage to induce purgation.

16. The method of claim 14 wherein said orally administrable dosage form is selected from the group consisting of capsules and tablets.

17. The method of claim 14 wherein the admixture formed in step (a) includes a purgative salt selected from the group consisting of dibasic magnesium phosphate, monobasic magnesium phosphate and mixtures, thereof.

18. The method of claim 17 wherein said purgative salt is dibasic magnesium phosphate included in an amount ranging from about 0.2 grams per kilogram body weight to 12.0 grams per kilogram body weight.

19. The method of claim 17 wherein said purgative salt is a mixture of dibasic magnesium phosphate and monobasic magnesium phosphate included in an amount ranging from about 0.2 grams per kilogram body weight to 12.0 grams per kilogram body weight.

20. The method of claim 18 wherein said dibasic magnesium phosphate is administered at a rate of from about 0.2 grams per kilogram body weight to 0.7 grams per kilogram body weight.

21. The method of claim 14 wherein step c) is repeated at least once.

22. The method of claim 17 wherein step c) is repeated at least once.

23. The method of claim 16 wherein the capsule is a gelatin capsule.