Pharmaceutical compositions and related methods of delivery
View Patent ↗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.
1. A method of treating a subject suffering from acromegaly, abnormal GI motility, flushing episodes associated with carcinoid syndrome, portal hypertension, an endocrine tumor, gastroparesis, diarrhea, pancreatic leak or pancreatic pseudo-cysts, the method comprising orally administering to the subject a pharmaceutical 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 octreotide, at least one salt of a medium chain fatty acid and polyvinylpyrrolidone (PVP), wherein the at least one salt of a medium chain fatty acid is present in the composition at an amount of at least 12% by weight and wherein the polyvinylpyrrolidone is present in the composition at an amount of 3% or more by weight.
2. The method of claim 1 , wherein the polyvinylpyrrolidone has a molecular weight of about 3000.
3. The method of claim 1 , wherein the medium chain fatty acid salt has a chain length from about 6 to about 14 carbon atoms.
4. The method of claim 3 , 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.
5. The method of claim 4 , wherein the fatty acid salt is sodium octanoate.
6. The method of claim 1 , wherein the medium chain fatty acid salt is present in the composition at an amount of 12% to 18% by weight.
7. The method 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.
8. The method of claim 1 , wherein the medium chain fatty acid salt is a lithium, potassium or ammonium salt.
9. The method of claim 1 , wherein the hydrophobic medium comprises glyceryl tricaprylate.
10. The method of claim 1 , wherein the pharmaceutical composition further comprises a surfactant.
11. The method of claim 1 , wherein the pharmaceutical composition comprises a therapeutically effective amount of octreotide and 12-20% 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, about 3-10% surfactant and about 1% water.
12. The method of claim 1 , wherein the pharmaceutical composition comprises a therapeutically effective amount of octreotide and 12-20% of sodium octanoate, about 5-10% of polyvinylpyrrolidone with a molecular weight of about 3000, about 20-80% of glyceryl tricaprylate, about 3-10% surfactant and about 1% water.
13. The method of claim 12 , wherein the octreotide is present at an amount of less than 33%.
14. The method of claim 13 , comprising 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.
15. The method of claim 14 , wherein the surfactant is glyceryl monocaprylate or polyoxyethylene sorbitan monooleate.
16. The method of claim 1 , wherein the solid form comprises a particle or a plurality of particles.
17. The method of claim 1 , wherein the solid form further comprises a stabilizer.
18. The method of claim 15 , wherein the solid form further comprises a stabilizer.
19. The method of claim 1 , wherein the pharmaceutical composition is additionally enteric coated.
20. The method of claim 7 , wherein the fatty acid is octanoic acid.
21. The method of claim 1 , 2 - 18 or 19 , wherein the method is a method of treating a subject suffering from acromegaly.
22. The method of claim 1 , 2 - 18 or 19 , wherein the method is a method of treating a subject suffering from diarrhea.
23. The method of claim 1 , 2 - 18 or 19 , wherein the method is a method of treating a subject suffering from portal hypertension.
24. The method of claim 1 , 2 - 18 or 19 , wherein the method is a method of treating a subject suffering from an endocrine tumor.
25. The method of claim 7 , wherein the triglyceride is a medium chain triglyceride.
26. The method of claim 12 , wherein the octreotide is present at an amount of less than 25%.
27. The method of claim 12 , wherein the octreotide is present at an amount of less than 10%.
28. The method of claim 12 , wherein the octreotide is present at an amount of less than 1%.
29. The method of claim 12 , wherein the octreotide is present at an amount of less than 0.1%.