Flocculated suspension of megestrol acetate

• US 20010048931A1
• Filed: 01/09/2001
• Published: 12/06/2001
• Est. Priority Date: 04/20/1998
• Status: Active Grant

• Current Assignee: Par Pharmaceutical Companies Incorporated (Endo International PLC)
• Original Assignee: Pharmaceutical Resources Incorporated (Endo International PLC)
• Inventors: Femia, Robert A., Chao, James C., Ross, Malcolm S.F., Ragunathan, N.
• Granted Patent: US 6,593,318 B2
• Time in Patent Office: Days
• US Class Current: 424/400
• CPC Class Codes: A61K 9/10 Dispersions; Emulsions A61K9/06 takes precedence; composition of dispersions, emulsions A61K47/00

Abstract

A novel oral pharmaceutical composition in the form of a stable flocculated suspension in water is described as comprising: megestrol acetate; at least one compound selected from the group consisting of polyethylene glycol, propylene glycol, glycerol, and sorbitol; and a surfactant, wherein polysorbate and polyethylene glycol are not simultaneously present.

Claims

1. An oral pharmaceutical composition in the form of a stable flocculated suspension in water comprising:

(a) megestrol acetate;

(b) at least one compound selected from the group consisting of polyethylene glycol, propylene glycol, glycerol, and sorbitol; and

(c) a surfactant, wherein polysorbate and polyethylene glycol are not simultaneously present in said composition.

2. The composition of

claim 1

, wherein the surfactant comprises a hydrophobic moiety having a straight carbon chain of up to 20 atoms.

3. The composition of

claim 2

, wherein the straight carbon chain is less than 10 carbon atoms in length.

4. The composition of

claim 1

, wherein the surfactant is non-ionic.

5. The composition of

claim 4

, wherein the surfactant is selected from the group consisting of alkanolamides, ethoxylated alcohols, carboxylic acids, amines, alcohol amides, alcohol phenol, glyceryl esters, sorbitan esters, polyoxyethylene esters and phosphate esters.

6. The composition of

claim 4

, wherein the surfactant is polysorbate.

7. The composition of

claim 4

, wherein the surfactant is polyoxyethylene 2, 4, 6, 8, 12, 20, 30, 40, 50, 100, or 150 stearate.

8. The composition of

claim 1

, wherein the surfactant is cationic.

9. The composition of

claim 8

, wherein the surfactant is selected from the group consisting of cetyldimethylethylammonium bromide and quaternary amines.

10. The composition of

claim 8

, wherein the surfactant is cetyldimethylethylammonium bromide.

11. The composition of

claim 1

, wherein the surfactant is anionic.

12. The composition of

claim 11

, wherein the surfactant is selected from the group consisting of salts of sulphonic acids, fatty alkyl sulphosuccinates, fatty alkyl ether sulphosuccinates, acyl sarcosinates, acyl taurides, paraffin sulphonates and salts of alkaline earth metals.

13. The composition of

claim 11

, wherein the surfactant is docusate sodium.

14. The composition of

claim 13

, wherein the concentration of docusate sodium is about 0.0001 to 0.03% weight/volume.

15. The composition of

claim 1

, wherein the megestrol acetate is micronized.

16. The composition of

claim 1

, wherein the concentration of megestrol acetate is about 10 to 200 mg per ml of said composition.

17. The composition of

claim 1

, wherein the concentration of megestrol acetate is about 40 mg per ml.

18. The composition of

claim 1

, wherein component (b) comprises a mixture of two compounds.

19. The composition of

claim 18

, wherein the compounds are glycerol and sorbitol.

20. The composition of

claim 19

, wherein the concentration of each of glycerol and sorbitol is up to about 20% weight/volume.

21. An oral pharmaceutical composition in the form of a stable flocculated suspension in water comprising on a percent weight/volume basis about 4% megestrol acetate, about 0.0005-0.030% docusate sodium, up to about 20% glycerol, up to about 20% sorbitol, about 0.1-0.35% xanthan gum, about 0.1-0.3% sodium benzoate, about 0.3% citric acid, about 0.06% sodium citrate, about 5% sucrose, about 0.08% flavor, and the remainder water.

22. An oral pharmaceutical composition in the form of a stable flocculated suspension in water comprising on a percent weight/volume basis about 4% megestrol acetate, about 0.0005-0.030% polyoxyethylene 40 stearate, up to about 20% glycerol, up to about 20% sorbitol, about 0.1-0.35% xanthan gum, about 0.1-0.3% sodium benzoate, about 0.3% citric acid, about 0.06% sodium citrate, about 5% sucrose, about 0.08% flavor, and the remainder water.