Stable emulsion compositions
View Patent ↗An emulsion composition containing a compound represented by the formula: wherein R, R 0 , Ar and n are as defined in the specification or a salt thereof or a prodrug thereof, wherein the composition is adjusted to have a pH of not more than about 6, shows improved stability of the compound, a salt thereof or a prodrug thereof, and realizes expression of superior efficacy.
1. An emulsion composition comprising a disperse phase particle in water, said particle having
an oil component;
an emulsifier; and
d-ethyl 6-[N-(2-chloro-4-fluorophenyl)sulfamoyl]-1-cyclohexene-1-carboxylate,
a salt thereof or a prodrug thereof; wherein said composition has a pH of not more than 6.
2. The composition according to claim 1 , which is an oil-in-water type.
3. The composition according to claim 1 , which has a pH of 3 to 6.
4. The composition according to claim 1 , which is used as an injection.
5. The composition according to claim 1 , wherein the oil component is selected from the group consisting of a vegetable oil, a partially hydrogenated vegetable oil, a simple glyceride, a mixed glyceride and a medium-size chain fatty acid glycerol ester.
6. The composition according to claim 1 , wherein the oil component is a vegetable oil.
7. The composition according to claim 6 , wherein the vegetable oil is a soybean oil, a cottonseed oil, a rapeseed oil, a peanut oil, a safflower oil, a sesame oil, a rice bran oil, a corn germ oil, a sunflower oil, a poppy oil or an olive oil.
8. The composition according to claim 7 , wherein the vegetable oil is a soybean oil.
9. The composition according to claim 1 , wherein the emulsifier is a phospholipid or a nonionic surfactant.
10. The composition according to claim 1 , wherein the emulsifier is a phospholipid.
11. The composition according to claim 10 , wherein the phospholipid is an egg yolk lecithin, a soybean lecithin, a hydrogenation product thereof, a phosphatidylcholine, a phosphatidylethanolamine, a phosphatidic acid, a phosphatidylserine, a phosphatidylinositol or a phosphatidylglycerol.
12. The composition according to claim 11 , wherein the phospholipid is an egg yolk lecithin.
13. The composition according to claim 1 , wherein the oil component is used in a proportion of about 1–about 30 wt % of the whole composition.
14. The composition according to claim 1 , wherein the emulsifier is used in a proportion of about 0.1 about 10 w/v %.
15. The composition according to claim 1 , wherein the emulsifier is contained in a proportion of about 0.1–about 150 wt % of the oil component.
16. The composition according to claim 1 , wherein said oil component is a vegetable oil and said emulsifier is a phospholipid.
17. The composition according to claim 1 , wherein said oil component is a soybean oil, said emulsifier is an egg yolk lecithin, said water is purified water and which further comprises a glycerol.
18. The composition according to claim 1 , which comprises said carboxylate, a salt thereof or a prodrug thereof in a proportion of about 0.001–about 95 wt % of the whole composition.
19. The composition according to claim 1 , which comprises said carboxylate, a salt thereof or a prodrug thereof in a proportion of about 0.01–about 30 wt % of the whole composition.
20. The composition according to claim 1 , wherein the disperse phase particle has an average particle size of about 25–about 500 nm.
21. The composition according to claim 1 , which is a nitric oxide and/or a cytokine production inhibitor.
22. The composition according to claim 1 , which is an agent for the treatment of a cardiac disease, an autoimmune disease, sepsis or septic shock.
23. A method for the treatment of a cardiac disease, an autoimmune disease, sepsis or septic shock, which comprises administering an effective amount of the composition of claim 1 to a mammal.