IP Library Granted Patent US 9,566,246
Granted Patent B2
US 9,566,246 · App. 15/044,949 · Granted Feb 14, 2017

Pharmaceutical compositions and related methods of delivery

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Quick Facts
Patent No.
US 9,566,246
App. No.
15/044,949
Granted
Feb 14, 2017
Kind
B2
Abstract

The pharmaceutical compositions described herein include a suspension which comprises an admixture in solid form of a therapeutically effective amount of a therapeutic agent and at least one salt of a medium chain fatty acid and a hydrophobic medium, e.g. castor oil or glyceryl tricaprylate or a mixture thereof. The pharmaceutical compositions described herein contain medium chain fatty acid salts and are substantially free of alcohols. The pharmaceutical compositions may be encapsulated in a capsule. Methods of treating or preventing diseases by administering such compositions to affected subjects are also disclosed.

Claims (30)

1. An enteric-coated oral dosage form comprising a composition comprising a suspension which comprises an admixture of a hydrophobic medium and a solid form wherein the solid form comprises a therapeutically effective amount of a polypeptide, at least one salt of a medium chain fatty acid and polyvinylpyrrolidone (PVP), wherein the polyvinylpyrrolidone is present in the composition at an amount of 3% or more by weight, and wherein the at least one salt of a medium chain fatty acid salt is present in the composition at an amount of at least 12% or more by weight.

2. The enteric-coated oral dosage form of claim 1 , wherein the medium chain fatty acid salt is present in the composition at an amount of 12% to 40% by weight.

3. The enteric-coated oral dosage form of claim 2 wherein the medium chain fatty acid salt is present in the composition at an amount of 12% to 18% by weight.

4. The enteric-coated oral dosage form of claim 1 where the polyvinylpyrrolidone is present in the composition at an amount of about 3% to about 20% by weight.

5. The enteric-coated oral dosage form of claim 4 where the polyvinylpyrrolidone is present in the composition at an amount of about 5% to about 15% by weight.

6. The enteric-coated oral dosage form of claim 1 , wherein the hydrophobic medium comprises glyceryl tricaprylate and the solid form consists of a polypeptide polyvinylpyrrolidone with a molecular weight of about 3000, and sodium octanoate.

7. The enteric-coated oral dosage form of claim 1 wherein the hydrophobic medium additionally comprises castor oil or glyceryl monocaprylate or a combination thereof and a surfactant.

8. The enteric-coated oral dosage form of claim 1 wherein the hydrophobic medium consists of glyceryl tricaprylate, glyceryl monocaprylate, and polyoxyethylene sorbitan.

9. The enteric-coated oral dosage form of claim 1 wherein the solid form consists essentially of polypeptide, polyvinylpyrrolidone with a molecular weight of about 3000, and sodium octanoate.

10. The enteric-coated oral dosage form of claim 1 wherein the composition comprises about 41% of glyceryl tricaprylate, about 27% castor oil, about 4% glyceryl monocaprylate, about 2% polyoxyethylene sorbitan monooleate, about 15% sodium octanoate, about 10% polyvinylpyrrolidone with a molecular weight of about 3000 and a therapeutically effective amount of polypeptide.

11. The enteric-coated oral dosage form of claim 1 wherein the composition comprises about 68% glyceryl tricaprylate, about 4% glyceryl monocaprylate, about 2% polyoxyethylene sorbitan monooleate, about 15% sodium octanoate, about 10% polyvinylpyrrolidone with a molecular weight of about 3000 and a therapeutically effective amount of polypeptide.

12. The enteric-coated oral dosage form of claim 1 , wherein the composition comprises a therapeutically effective amount of polypeptide, about 12-21% of sodium octanoate, about 5-10% of polyvinylpyrrolidone with a molecular weight of about 3000, about 20-80% of glyceryl tricaprylate, about 0-50% castor oil and about 3-10% surfactant.

13. The enteric-coated oral dosage form of claim 1 , wherein the composition comprises a therapeutically effective amount of polypeptide, about 12-21% of sodium octanoate, about 5-10% of polyvinylpyrrolidone with a molecular weight of about 3000, about 20-80% of glyceryl tricaprylate and about 3-10% surfactant.

14. The enteric-coated oral dosage form of claim 13 , wherein the polypeptide is present at an amount of less than 33%.

15. The enteric-coated oral dosage form of claim 14 , wherein the composition comprises about 15% of sodium octanoate, about 10% of polyvinylpyrrolidone with a molecular weight of about 3000, about 30-70% glyceryl tricaprylate and about 6% of surfactant.

16. The enteric-coated oral dosage form of claim 15 , wherein the surfactant is glyceryl monocaprylate or polyoxyethylene sorbitan monooleate.

17. The enteric-coated oral dosage form of claim 1 , wherein the solid form comprises a particle or a plurality of particles.

18. The enteric-coated oral dosage form of claim 16 , wherein the solid form further comprises a stabilizer.

19. The enteric-coated oral dosage form of claim 1 , wherein the solid form further comprises a stabilizer.

20. The enteric-coated oral dosage form of claim 13 , wherein the polypeptide is present at an amount of less than 25%.

21. The enteric-coated oral dosage form of claim 13 , wherein the polypeptide is present at an amount of less than 10%.

22. The enteric-coated oral dosage form of claim 13 , wherein the polypeptide is present at an amount of less than 1%.

23. The enteric-coated oral dosage form of claim 13 , wherein the polypeptide is present at an amount of less than 0.1%.

24. The enteric-coated oral dosage form of claim 1 , wherein the polyvinylpyrrolidone has a molecular weight of about 3000.

25. The enteric-coated oral dosage form of claim 1 , wherein the medium chain fatty acid salt has a chain length from about 6 to about 14 carbon atoms.

26. The enteric-coated oral dosage form of claim 25 , wherein the medium chain fatty acid salt is sodium hexanoate, sodium heptanoate, sodium octanoate, sodium nonanoate, sodium decanoate, sodium undecanoate, sodium dodecanoate, sodium tridecanoate or sodium tetradecanoate, or a corresponding potassium or lithium or ammonium salt or a combination thereof.

27. The enteric-coated oral dosage form of claim 26 , wherein the medium chain fatty acid salt is sodium octanoate.

28. The enteric-coated oral dosage form of claim 1 , wherein the hydrophobic medium comprises a mineral oil, a paraffin, a fatty acid a monoglyceride, a diglyceride, a triglyceride, an ether or an ester, or a combination thereof.

29. The enteric-coated oral dosage form of claim 1 , wherein the hydrophobic medium comprises glyceryl tricaprylate.

30. The enteric-coated oral dosage form of claim 1 , wherein the composition further comprises a surfactant.

Assignments (2)
MERGER AND CHANGE OF NAME Recorded Jan 7, 2026
From: AMRYT ENDO, INC.; AMYRT PHARMACEUTICALS INC.
To: AMRYT PHARMACEUTICALS INC.
Reel/Frame 073389/0551 →
CHANGE OF ADDRESS Recorded Mar 19, 2024
From: MCEVOY, JOHN
To: AMRYT ENDO, INC.
Reel/Frame 066833/0786 →