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Treatment of ophthalmic disorders using urea and urea derivatives

a technology of ophthalmic disorders and derivatives, applied in the direction of biocide, cardiovascular disorders, drug compositions, etc., can solve the problems of cystoid macular edema, idiopathic macular holes, rhegmatogenous retinal tears, etc., and achieve the effect of removing vitreoretinal traction

Inactive Publication Date: 2007-05-10
KATO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0028] Further in accordance with the present invention, there are provided methods for treating various ophthalmological disorders in human or veterinary patients by administering to the patient a therapeutically effective amount of urea, a urea derivative, thiourea, a thiourea derivative, guanidine, a guanidine derivative or a compound having General Formula I. The compound may be injected directly into the vitreous body of the eye (i.e., intravitreal injection) or may be administered by any other route that causes distribution of a therapeutically effective amount of the compound to the vitreous body. The compound may be administered for the purpose of treating specific ocular diseases or conditions associ

Problems solved by technology

The strong attachment of the cortical vitreous to the inner limiting lamina of the retina creates traction on the

Method used

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  • Treatment of ophthalmic disorders using urea and urea derivatives
  • Treatment of ophthalmic disorders using urea and urea derivatives
  • Treatment of ophthalmic disorders using urea and urea derivatives

Examples

Experimental program
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Effect test

example i

Treatment of Retinal Tears

[0043] Seven male and five female human patients having an average age of 47 years were observed to have single or multiple retinal tears, in addition 9 of the 12 patients had macular detachment. All patients received pneumatic Retinopexy treatment 3 days after intravitreal injection of 1.5 mg of urea in 50 μl of aqueous solution prepared according to the formulation set forth in Table II above. Ophthalmoscopic as well as biomicroscopic examination of all eyes showed no adverse effects of the intravitreal injection of the urea solution. Within 3-7 days after urea injection, 11 / 12 patients had developed PVD, only 1 / 12 patients had not developed PVD. Within 90 days of the urea injection that one patient also developed PVD.

[0044] Within 3 days of treatment 9 / 12 patients had complete retinal reattachment and macular attachment, and within 7 days all 12 patients had complete retinal reattachment and macular attachment. All patients were followed up for a perio...

example ii

Treatment of Idiopathic Macular Hole

[0046] A female patient 58 years old was observed to have a 450 μm idiopathic macular hole of 6 months duration. The macular defect was classified as a stage 3 macular hole, and the patient's visual acuity was recorded at 20 / 400 at a baseline time point prior to urea treatment. The subject was administered a single intravitreal injection of a formulation containing 1.5 mg of urea in a 50 μl solution prepared in accordance with the formulation of Table III above, and within 7 days the patient had a complete Posterior Vitreous Detachment (PVD). Ophthalmoscopic as well as Biomicroscopic examination of the patient's eye showed no adverse effects of the intravitreal injection of the urea solution. Seven days after the intravitreal urea injection the patient was administered an intravitreal injection of 0.3 ml of expandable gas (C3F8).

[0047] One week after administration of the gas, the size of the macular hole had decreased from 450 μm to a smaller s...

example iii

Intravitreal Urea Injection as an Adjuvant in Pneumatic Retinopexy

[0050] The present invention provides a method to reduce vitreoretinal traction and induce total posterior vitreous detachment (t-PVD) in subjects with primary regmatogen retinal detachment (PRRD) susceptible of treatment by pneumatic retinopexy was practiced by administering a formulation containing urea formulation set forth in Table II (VRT-1001) to the patients.

[0051] Consecutive patients of both genders with PRRD eligible for treatment with pneumatic retinopexy where enrolled after informed consent. A 0.3 ml intravitreal injection of the urea formulation set forth in Table II (VRT-1001, Vitreoretinal Technologies Inc., Irvine, Calif., USA) was administered, and pneumatic retinopexy was performed the next day, using 0.4 ml of 100% C3F8. Argon laser was applied as soon as possible to seal the retinal tears. Before, and 1, 7, 15, 30 and 90 days after the procedure, patients were monitored with biomicroscopy, poste...

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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.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS [0001] This application claims the benefit of U.S. Provisional Application Ser. No. 60 / 357,347, filed Feb. 13, 2002, and U.S. Provisional Application Ser. No. 60 / 357,574, filed Feb. 15, 2002. This application is also a continuation-in-part application of U.S. application Ser. No. 10 / 215,680, filed Aug. 9, 2002, which is a continuation application of U.S. application Ser. No. 09 / 517,798, filed Mar. 2, 2000, now U.S. Pat. No. 6,462,071. The contents of all the foregoing patent applications are hereby incorporated by reference in their entireties.FIELD OF THE INVENTION [0002] This invention relates generally to the use of stabilized aqueous solutions of urea or urea derivatives for administration to the eyes of humans or other mammals. Urea and urea derivatives liquefy the vitreous humor and induce a posterior vitreous detachment thereby separating the cortical vitreous from the inner limiting lamina of the retina. The strong attachment of the co...

Claims

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Application Information

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IPC IPC(8): A61K31/343A61K31/17A61K31/155A61K31/40
CPCA61K31/155A61K31/17A61K31/343A61K31/40A61K2300/00A61P27/02A61P9/10
Inventor KARAGEOZIAN, VICKEN H.CASTILLEJOS, DAVIDPARK, JOHN
Owner KATO PHARMA
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