Compositions containing difluprednate

• US 6,114,319 A
• Filed: 05/12/1998
• Issued: 09/05/2000
• Est. Priority Date: 05/14/1997
• Status: Expired due to Term

• Current Assignee: Mitsubishi Chemical Corporation (Mitsubishi Chemical Group Corp.), Senju Pharmaceutical Company Limited
• Original Assignee: Mitsubishi Chemical Corporation (Mitsubishi Chemical Group Corp.), Senju Pharmaceutical Company Limited
• Inventors: Kimura, Masako, Yasueda, Shin-ichi, Yamaguchi, Masazumi, Inada, Katsuhiro
• Primary Examiner(s): FAY, ZOHREH A
• Application Number:
  US09/076,124
• Time in Patent Office: 847 Days
• Field of Search: 514/177, 514/912
• US Class Current: 514/177
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61K 9/1075 Microemulsions or submicron emulsions; Preconcentrates or solids thereof; Micelles, e.g. made of phospholipids or block copolymers A61K9/0026 takes precedence
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/16 Otologicals

Abstract

The present invention relates to a liquid composition comprising difluprednate, oil, water and an emulsifier. The composition of the present invention has superior antiinflammatory action and antiallergic action. The composition of the present invention shows superior transfer to a lesion and uniform drug distribution upon administration, as compared to conventional preparations containing difluprednate, so that it shows sufficient efficacy in a smaller dose. The inventive composition is associated with extremely less uncomfortable feeling and foreign sensation upon administration, as compared to conventional preparations containing difluprednate, and it can be administered easily to local sites of eye, nose, ear and the like.

Claims

1. A difluprednate emulsion comprising difluprednate, oil comprising a fatty acid ester of glycerol, water and an emulsifier.

2. The emulsion of claim 1, comprising 10-100,000 parts by weight of oil, 100-100,000 parts by weight of water and 10-100,000 parts by weight of the emulsifier, per part by weight of difluprednate.

3. The emulsion of claim 1, comprising 10-10,000 parts by weight of oil, 100-50,000 parts by weight of water and 10-10,000 parts by weight of the emulsifier, per part by weight of difluprednate.

4. The emulsion of claim 1, comprising 10-5,000 parts by weight of oil, 500-50,000 parts by weight of water and 10-5,000 parts by weight of the emulsifier, per part by weight of difluprednate.

5. The emulsion of claim 1, wherein the fatty acid ester of glycerol is a member selected from the group consisting of castor oil, peanut oil, cotton seed oil, soybean oil, olive oil and a medium chain fatty acid triglyceride.

6. The emulsion of claim 1, wherein the emulsifier comprises a surfactant.

7. The emulsion of claim 6, wherein the surfactant is a nonionic surfactant.

8. The emulsion of claim 7, wherein the nonionic surfactant is a member selected from the group consisting of polyoxyethylene hydrogenated castor oil and a polyoxyethylenesorbitan fatty acid ester.

9. The emulsion of claim 8, wherein the polyoxyethylenesorbitan fatty acid ester is a member selected from the group consisting of polyoxyethylenesorbitan monooleate, polyoxyethylenesorbitan monolaurate, polyoxyethylenesorbitan monopalmitate and polyoxyethylenesorbitan monostearate.

10. The emulsion of claim 1 which is an oil-in-water type emulsion.

11. The emulsion of claim 1 which is in the form of an eye drop, a nasal drop or an ear drop.

12. The emulsion of claim 2, which is an oil-in-water type emulsion.

13. The emulsion of claim 3, which is an oil-in-water type emulsion.

14. The emulsion of claim 4, which is an oil-in-water type emulsion.

15. The emulsion of claim 2, which is in the form of an eye drop, a nasal drop or an ear drop.

16. The emulsion of claim 3, which is in the form of an eye drop, a nasal drop or an ear drop.

17. The emulsion of claim 4, which is in the form of an eye drop, a nasal drop or an ear drop.