Claims for Patent: 8,691,874

Summary for Patent: 8,691,874

Title:	Treatment of ophthalmic disorders using urea
Abstract:	Methods for treating disorders of the eye and/or disorders of a nerve in a human or veterinary patient by delivering to the patient a therapeutically effective amount of a compound selected from the group of; urea, urea derivatives, thiourea, thiourea derivatives, guanidine, guanidine derivatives and compounds having General Formula I as set forth herein. For ophthalmic applications, the compound may be delivered by intravitreal injection such that the compound causes vitreal liquefaction, posterior vitreoretinal detachment and other affects.
Inventor(s):	Karageozian; Vicken H. (Laguna Beach, CA), Castillejos; David (Irvine, CA), Park; John (Santa Ana, CA)
Assignee:	Kato Pharmaceuticals, Inc. (Laguna Hills, CA)
Application Number:	13/445,822
Patent Claims:	1. A pharmaceutical composition for injection into a vitreous body of an eye, comprising a sterile aqueous solution, comprising: a) 3-30.0% urea by weight; b) 0.00001-1.0% citric acid by weight; c) 0.05-3.6% sodium chloride by weight; and d) sterile water for injection, Q.S. 100% by weight; wherein said pharmaceutical composition is stable and non-toxic when injected into the eye. 2. The pharmaceutical composition of claim 1, wherein the aqueous solution comprises 6.0-30.0% urea by weight. 3. The pharmaceutical composition of claim 1, wherein the aqueous solution comprises 15-30.0% urea by weight. 4. The pharmaceutical composition of claim 1, wherein the aqueous solution comprises urea in a concentration of about 7.5 mg urea per 50 .mu.l. 5. The pharmaceutical composition of claim 1, wherein the aqueous solution comprises 0.00007-0.007% citric acid by weight. 6. The pharmaceutical composition of claim 1, wherein the aqueous solution comprises about 0.007% citric acid by weight. 7. The pharmaceutical composition of claim 1, wherein the aqueous solution comprises 0.9-1.8% sodium chloride by weight. 8. The pharmaceutical composition of claim 1, wherein the aqueous solution comprises about 0.9% sodium chloride by weight. 9. The pharmaceutical composition of claim 1, wherein the aqueous solution has a pH from about 4.0 to about 9.0. 10. The pharmaceutical composition of claim 1, wherein the aqueous solution has a pH from about 4.0 to about 6.5. 11. The pharmaceutical composition of claim 1, wherein the pharmaceutical composition is stable when stored at room temperature for at least about one year. 12. A dry pharmaceutical composition, obtainable by lyophilization of the sterile aqueous solution of claim 1. 13. A dry pharmaceutical composition, comprising urea, citric acid and sodium chloride, wherein each of the urea, citric acid and sodium chloride are present in the dry pharmaceutical composition in an amount sufficient to yield an aqueous solution upon reconstitution with water, the aqueous solution comprising: a) 3-30.0% urea by weight; b) 0.00001-1.0% citric acid by weight; c) 0.05-3.6% sodium chloride by weight; and d) water, Q.S. 100% by weight; and wherein after reconstitution of the dry pharmaceutical composition, the aqueous solution is non-toxic when injected into a vitreous body of an eye. 14. The dry pharmaceutical composition of claim 13, wherein upon reconstitution with water, the aqueous solution comprises a urea concentration of 6.0-30.0% by weight. 15. The dry pharmaceutical composition of claim 13, wherein upon reconstitution with water, the aqueous solution comprises a urea concentration of 15-30.0% by weight. 16. The dry pharmaceutical composition of claim 13, wherein upon reconstitution with water, the aqueous solution comprises a citric acid concentration of 0.00007-0.007% by weight. 17. The dry pharmaceutical composition of claim 13, wherein upon reconstitution with water, the aqueous solution comprises a citric acid concentration of about 0.007% by weight. 18. The dry pharmaceutical composition of claim 13, wherein upon reconstitution with water, the aqueous solution comprises a sodium chloride concentration of 0.9-1.8% by weight. 19. The dry pharmaceutical composition of claim 13, wherein upon reconstitution with water, the aqueous solution comprises a sodium chloride concentration of about 0.9% by weight. 20. The dry pharmaceutical composition of claim 13, wherein upon reconstitution with water, the aqueous solution has a pH from about 4.0 to about 9.0. 21. The dry pharmaceutical composition as claimed in claim 13, wherein upon reconstitution with water, the aqueous solution has a pH from about 4.0 to about 6.5. 22. The dry pharmaceutical composition of claim 13, wherein the dry composition is stable for at least one year at room temperature. 23. A dry composition comprising: a) 9-90 mg urea; b) 0.00003-3 mg citric acid; and c) 0.15-10.8 mg sodium chloride; wherein said dry composition is suitable for reconstitution with sterile water for injection to yield an aqueous solution comprising 3-30.0% urea and wherein the aqueous solution is non-toxic when injected into a vitreous body of an eye. 24. The dry composition of claim 23, wherein the composition comprises 18-90 mg urea. 25. The dry composition of claim 23, wherein the composition comprises 45-90 mg urea. 26. The dry composition of claim 23, wherein the composition comprises 0.00021-0.021 mg citric acid. 27. The dry composition of claim 23, wherein the composition comprises 0.021 mg citric acid. 28. The dry composition of claim 23, wherein the composition comprises 2.7-5.4 mg sodium chloride. 29. The dry composition of claim 23, wherein the composition comprises 2.7 mg sodium chloride. 30. The dry composition of claim 23, wherein the composition is stable when stored at room temperature for one year. 31. A kit for the preparation of an aqueous solution comprising urea, the aqueous solution being suitable for injection into a vitreous body of an eye, the kit comprising: a) a first container containing a dry composition comprising: i) 9-90 mg urea; ii) 0.00003-3 mg citric acid; and iii) 0.15-10.8 mg sodium chloride; and b) a second container containing at least 300 .mu.L sterile water for injection. 32. The kit of claim 31, further comprising a syringe for intravitreal injection. 33. The kit of claim 31, wherein the dry composition comprises 45-90 mg urea. 34. The kit of claim 31, wherein the dry composition comprises 0.021 mg citric acid. 35. The kit of claim 31, wherein the first and second containers are glass vials. 36. The kit of claim 31, further comprising instructions for reconstitution and intravitreal injection.

Details for Patent 8,691,874

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Merck Sharp & Dohme Corp.	ZOSTAVAX	zoster vaccine live	For Injection	125123	05/25/2006		2020-03-02