Eye drop containing roflumilast

• US 20090209599A1
• Filed: 06/09/2006
• Published: 08/20/2009
• Est. Priority Date: 06/09/2005
• Status: Abandoned Application

• Current Assignee: Santen Pharmaceutical Company Limited
• Original Assignee: Santen Pharmaceutical Company Limited
• Inventors: Endo, Yoko, Kimura, Akio
• Application Number:
  US11/921,694
• Publication Number:
  US 20090209599A1
• Time in Patent Office: Days
• US Class Current: 514/352
• CPC Class Codes: A61K 31/44 Non condensed pyridines; Hydrogenated derivatives thereof
• CPC Class Codes: A61K 9/0048 Eye, e.g. artificial tears
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: Y02A 50/30 Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Abstract

An object of the present invention is to enhance the efficacy of roflumilast in an eye drop containing roflumilast as an active ingredient. By formulating at least one type of viscosity-increasing agent in the eye drop containing roflumilast as an active ingredient, an eye drop in which the efficacy of roflumilast is enhanced can be prepared.

Claims

1. An eye drop comprising roflumilast as an active ingredient, wherein by formulating at least one type of viscosity-increasing agent therein, the efficacy of roflumilast is enhanced and also the viscosity of the eye drop at 25°

C. is made 1.5 to 500 mPa·

s.

2. The eye drop according to claim 1, wherein the viscosity of the eye drop at 25°

C. is 1.5 to 50 mPa·

s.

3. The eye drop according to claim 1, wherein the concentration of roflumilast is 0.00001 to 0.05% (w/v).

4. The eye drop according to claim 1, wherein the concentration of roflumilast is 0.0001 to 0.03% (w/v).

5. The eye drop according to claim 1, wherein the viscosity-increasing agent is hydroxypropylmethyl cellulose, polyvinyl alcohol or carboxyvinyl polymer.

6. The eye drop according to claim 1, wherein it is made a soluble type by further formulating a surfactant therein.

7. The eye drop according to claim 6, wherein the surfactant is at least one member selected from polysorbate 80, polyoxyethylene hydrogenated castor oil 60, polyoxyl 35 castor oil and polyoxyl 40 monostearate.

8. A method in which in an eye drop comprising roflumilast as an active ingredient, by formulating at least one type of viscosity-increasing agent therein, the efficacy of roflumilast is enhanced and also the viscosity of the eye drop at 25°

C. is made 1.5 to 500 mPa·

s.

9. A method of treating an eye disease comprising administering a pharmacologically effective amount of an eye drop comprising roflumilast as an active ingredient, in which by formulating at least one type of viscosity-increasing agent therein, the efficacy of roflumilast is enhanced and also the viscosity of the eye drop at 25°

C. is made 1.5 to 500 mPa·

s to a patient.

10. The treatment method according to claim 9, wherein the viscosity of the eye drop at 25°

C. is 1.5 to 50 mPa·

s.

11. The treatment method according to claim 9, wherein the concentration of roflumilast is 0.00001 to 0.05% (w/v).

12. The treatment method according to claim 9, wherein the concentration of roflumilast is 0.0001 to 0.03% (w/v).

13. The treatment method according to claim 9, wherein the viscosity-increasing agent is hydroxypropylmethyl cellulose, polyvinyl alcohol or carboxyvinyl polymer.

14. The treatment method according to claim 9, wherein the eye drop is made a soluble type by further formulating a surfactant therein.

15. The treatment method according to claim 14, wherein the surfactant is at least one member selected from polysorbate 80, polyoxyethylene hydrogenated castor oil 60, polyoxyl 35 castor oil and polyoxyl 40 monostearate.