Claims for Patent: 9,566,246

Summary for Patent: 9,566,246

Title:	Pharmaceutical compositions and related methods of delivery
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.
Inventor(s):	Mamluk; Roni (Mazkeret Batya, IL), Tzabari; Moshe (Jerusalem, IL), Marom; Karen (Mevaseret Zion, IL), Salama; Paul (Ashdod, IL), Weinstein; Irina (Maale Adummim, IL)
Assignee:	CHIASMA INC. (Waltham, MA)
Application Number:	15/044,949
Patent Claims:	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.