Low-Dose Carbachol Compositions And Methods For Treatment Of Night Vision Disturbance

Abstract

Ophthalmic formulations for acute and transient treatment of night vision disturbance syndrome (NVD) are presented. Preferred formulations comprise carbachol at very low concentrations that were demonstrated to unexpectedly provide an acute and transient therapeutic effect for a desirable magnitude and period of time.

What is claimed is: 
     
         1 . A topical ophthalmic composition for acute and transient treatment of night vision disturbance, comprising:
 carbachol in an amount of equal or less than 0.75% of the ophthalmic composition;   an aqueous buffer that renders pH of the ophthalmic composition to a pH of between about 6.5 to about 7.0;   a tonicity agent in an amount that renders osmolality of the ophthalmic composition to between about 260-340 mOsm/kg;   a viscosity modifier that renders viscosity of the ophthalmic composition to between about 170 cP to about 220 cP; and   wherein the composition is formulated such that, upon topical administration of the composition to an eye, a pupillary diameter of the eye is acutely and transiently reduced by between about 1 mm and 2 mm for a duration of equal or less than 3 hours.   
     
     
         2 . The topical ophthalmic composition of  claim 1 , comprising carbachol in an amount of equal or less than about 0.50%. 
     
     
         3 . The topical ophthalmic composition of  claim 1 , comprising carbachol in an amount of between about 0.25% and about 0.50%. 
     
     
         4 . The topical ophthalmic composition of  claim 1 , wherein the carbachol composition has a pH of about 7.0 and a viscosity of between about 180 cP to about 190 cP. 
     
     
         5 . The topical ophthalmic composition of  claim 1 , wherein the buffer comprises a borate buffer. 
     
     
         6 . The topical ophthalmic composition of  claim 1 , wherein the buffer has a buffer strength of at least 50 mM. 
     
     
         7 . The topical ophthalmic composition of  claim 1 , wherein the tonicity agent is selected from the group consisting of sodium chloride, glycerol, thioglycerol, mannitol, lactose, propylene glycol, and dextrose. 
     
     
         8 . The topical ophthalmic composition of  claim 7 , wherein the viscosity modifier is a cellulosic viscosity modifier. 
     
     
         9 . The topical ophthalmic composition of  claim 1 , wherein the viscosity modifier is hydroxypropyl methylcellulose. 
     
     
         10 . The topical ophthalmic composition of  claim 1 , wherein carbachol is present in an amount of between about 0.50 to about 0.75% of the ophthalmic composition, wherein the aqueous buffer is a borate buffer, and wherein the pH of the ophthalmic composition is between about 6.5 and about 7.0. 
     
     
         11 . The topical ophthalmic composition of  claim 1 , further comprising benzalkonium chloride in an amount of about 0.02% of the ophthalmic composition. 
     
     
         12 . The topical ophthalmic composition of  claim 1 , wherein the acute and transient reduction is non-curative. 
     
     
         13 . A method of acute and transient treatment of night vision disturbance in an individual, comprising:
 topically administering a carbachol composition to an eye of an individual to reduce pupillary diameter by between about 1 mm and about 2 mm for a duration of equal or less than 3 hours;
 wherein the carbachol is present in the composition in an amount of equal or less than about 0.75%; 
 wherein the carbachol composition has a pH of between about 6.5 and about 7.0 and a viscosity of between about 170 cP to about 220 cP. 
   
     
     
         14 . The method of  claim 13 , wherein the carbachol is present in the composition in an amount of equal or less than about 0.50%. 
     
     
         15 . The method of  claim 13 , wherein the carbachol is present in the composition in an amount of between about 0.25% and about 0.50%. 
     
     
         16 . The method of  claim 13 , wherein a miotic effect of the composition is equal or less than 30% reduction in pupillary diameter. 
     
     
         17 . The method of  claim 13 , wherein the carbachol composition further comprises benzalkonium chloride in an amount of about 0.02%. 
     
     
         18 . The method of  claim 13 , wherein the treatment reduces at least one of glare, starburst, halo, and double vision. 
     
     
         19 . The method of  claim 13 , wherein the individual has not undergone refractive surgery. 
     
     
         20 . The method of  claim 13 , wherein the acute and transient treatment is an on-demand and non-curative treatment.