Composition and method for stabilizing the same
View Patent ↗Disclosed is a novel composition comprising a novel bi-cyclic compound, which is expected to be pharmaceutically active, and a glyceride. The stability of the bi-cyclic compound can be improved significantly by dissolving the same in a glyceride.
1. A composition comprising:
i: the following bi-cyclic compound
7-[(1R,3R,6R,7R)-3-(1,1-difluoropentyl)-3-hydroxy-2-oxabicyclo[4.3.0]nonane-8-one-7-yl]heptanoic acid,
ii. the mono-cyclic tautomer of said compound; and
iii. at least one glyceride,
wherein the ratio of the bi-cyclic compound to mono-cyclic tautomer is at least 90:10.
2. The composition according to claim 1 , wherein the ratio of bi-cyclic compound to mono-cyclic tautomer is substantially 100:0.
3. The composition according to claim 1 , wherein said glyceride has between 6 and 24 carbon atoms.
4. The composition according to claim 1 , wherein said glyceride has between 6 and 20 carbon atoms.
5. The composition according to claim 1 , in which the glyceride is a mixture of 2 or more glycerides.
6. The composition according to claim 1 , wherein at least one glyceride is a triglyceride.
7. The composition according to claim 2 , wherein at least one glyceride is a triglyceride.
8. The composition according to claim 6 , wherein said triglyceride is caprylic acid triglyceride and/or capric acid triglyceride.
9. The composition according to claim 6 , wherein the triglyceride is present in an amount of 1-5,000,000 parts by weight based on one part by weight of the bi-cyclic structure.
10. The composition according to claim 6 , wherein the triglyceride is present in an amount of 5-1,000,000 parts by weight based on one part by weight of the bi-cyclic structure.
11. The composition according to claim 6 , wherein the triglyceride is present in an amount of 10-500,000 parts by weight based on one part by weight of the bi-cyclic structure.
12. The composition according to claim 1 , wherein said glyceride is admixed with other oil solvent.
13. The composition according to claim 12 , wherein said other oil solvent is mineral oil.
14. The composition according to claim 1 , which is in a dosage form suitable for oral administration.
15. The composition according to claim 14 , which is formulated as a capsule.
16. The composition according to claim 1 , which is in a dosage form suitable for topical administration.
17. The composition according to claim 16 , which is formulated as an eye drop.
18. A composition comprising:
i. the following bi-cyclic compound
7-[(1R,6R,7R)-3-[(3S)-1,1-difluoro-3-methylpentyl]-3-hydroxy-2-oxabicyclo[4.3.0]nonane-8-one-7-yl]heptanoic acid,
ii. the mono-cyclic tautomer of said compound; and
iii. at least one glyceride,
wherein the ratio of the bi-cyclic compound to mono-cyclic tautomer is at least 1:1.
19. The composition according to claim 18 , wherein the ratio of bi-cyclic compound to mono-cyclic tautomer is at least 90:10.
20. The composition according to claim 18 , wherein the ratio of bi-cyclic compound to mono-cyclic tautomer is substantially 100:0.
21. The composition according to claim 18 , wherein said glyceride has between 6 and 24 carbon atoms.
22. The composition according to claim 18 , wherein said glyceride has between 6 and 20 carbon atoms.
23. The composition according to claim 18 , in which the glyceride is a mixture of 2 or more glycerides.
24. The composition according to claim 18 , wherein at least one glyceride is a triglyceride.
25. The composition according to claim 24 , wherein said triglyceride is caprylic acid triglyceride and/or capric acid triglyceride.
26. The composition according to claim 24 , wherein the triglyceride is present in an amount of 1-5,000,000 parts by weight based on one part by weight of the bi-cyclic structure.
27. The composition according to claim 24 , wherein the triglyceride is present in an amount of 5-1,000,000 parts by weight based on one part by weight of the bi-cyclic structure.
28. The composition according to claim 24 , wherein the triglyceride is present in an amount of 10-500,000 parts by weight based on one part by weight of the bi-cyclic structure.
29. The composition according to claim 24 , wherein said glyceride is admixed with other oil solvent.
30. The composition according to claim 29 , wherein said other oil solvent is mineral oil.
31. The composition according to claim 18 , which is in a dosage form suitable for oral administration.
32. The composition according to claim 31 , which is formulated as a capsule.
33. The composition according to claim 18 , which in a dosage form suitable for topical administration.
34. The composition according to claim 33 , which is formulated as an eye drop.