IP Library Granted Patent US 10,335,403
Granted Patent B2
US 10,335,403 · App. 16/132,440 · Granted Jul 2, 2019

Niacin formulation

Inventors: Xavier Mulet (Elwood, AU); Gregory Yu Foo Szto (Elwood, AU); David Kannar (Elwood, AU)
Assignee: ZEENAR ENTERPRISE PTY LTD
A61K31/455A61K9/006A61K9/1075A61K9/20A61K31/201A61K31/22A61K36/00A61K45/06
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Quick Facts
Patent No.
US 10,335,403
App. No.
16/132,440
Granted
Jul 2, 2019
Kind
B2
Abstract

The present invention provides a composition including an amphiphilic compound capable of self-assembling into a liquid crystalline phase; and a niacin compound. In another aspect, the present invention provides a method for the treatment of a disease state comprising administering a therapeutically effective amount of a pharmaceutical composition incorporating that composition.

Claims (23)

1. A method for prolonging the release of niacin in a subject, comprising:

administering to the oral mucosa of a subject in need thereof a composition comprising an amphiphilic compound capable of self-assembling into a liquid crystalline phase upon contact with a hydrophilic solvent and a therapeutically effective amount of a niacin compound, and

prolonging release of the niacin compound in the subject for up to 12 hours.

2. The method of claim 1 , wherein release of the niacin compound is prolonged for 6 to 8 hours.

3. The method of claim 1 , wherein release of the niacin compound is prolonged for at least 4 to 6 hours.

4. The method of claim 1 , wherein the composition does not comprise prolonged release polymers.

5. The method of claim 1 , wherein administering the composition comprises sublingual administration.

6. The method of claim 1 , wherein the niacin compound comprises a unit dosage of 100 mg to 1,000 mg.

7. The method of claim 1 , wherein the weight of the amphiphilic compound in the composition when dry comprises at least 5% by weight of the combined weight of the dry niacin compound and the dry amphiphilic compound in the composition.

8. The method of claim 1 , wherein the weight of niacin compound when dry comprises at least 50% by weight of the combined weight of the dry niacin compound and the dry amphiphilic compound.

9. The method of claim 1 , wherein administering the composition comprises nighttime administration.

10. The method of claim 1 , wherein the niacin compound comprises nicotinyl alcohol tartrate, d-glucitol hexanicotinate, aluminium nicotinate, niceritrol, or d,l-alpha-tocopheryl nicotinate.

11. The method of claim 1 , wherein the niacin compound comprises niacin.

12. The method of claim 1 , wherein the amphiphilic compound comprises a monoglyceride of a fatty acid comprising a 6 to 24 carbon chain, a diglyceride of a fatty acid comprising a 6 to 24 carbon chain, or a combination thereof.

13. The method of claim 12 , wherein the carbon chain is unsaturated.

14. The method of claim 12 , wherein the amphiphilic compound comprises a mixture of monoacylglycerols, diacylglycerols, and glycerol.

15. The method of claim 12 , wherein the amphiphilic compound comprises a glycerol monooleate.

16. The method of claim 1 , wherein contacting the composition with excess PBS causes the composition to physically disintegrate and the amphiphilic compound to form a self-assembled structure detectable by small angle x-ray scattering (SAXS).

17. The method of claim 16 , wherein the detectable self-assembled structure comprises an inverse hexagonal bulk phase.

18. The method of claim 16 , wherein disintegration of the composition comprises 2 to 10 minutes.

19. The method of claim 1 , wherein the composition is a tablet.

20. The method of claim 1 , wherein the amphiphilic compound is self-assembled.

21. The method of claim 1 , wherein the composition is a colloidal dispersion, wherein the colloidal dispersion comprises a self-assembled amphiphilic compound in a continuous phase formed by one or more hydrophilic solvents.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 17, 2026
From: ZEENAR ENTERPRISES PTY LTD
To: CUBOPHARM PTY LTD
Reel/Frame 074992/0303 →
Priority Claims (2)
AU 2013901647 · May 9, 2013 · national
AU 2013903276 · Aug 28, 2013 · national
Continuity (2)
Continuation 14889878
Related Publication 20190015403A1 · Jan 17, 2019