US2002161042A1PendingUtilityA1

Nitric oxide donor composition and method for treatment of anal disorders

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Assignee: CELLEGY PHARMA INCPriority: May 27, 1994Filed: Dec 11, 2001Published: Oct 31, 2002
Est. expiryMay 27, 2014(expired)· nominal 20-yr term from priority
Inventors:Stephen R. Gorfine
A61P 43/00A61P 9/14A61P 25/04A61P 29/00A61P 25/02A61P 3/00A61P 1/04A61K 31/47A61P 17/00A61P 1/00A61K 31/34A61K 33/00A61P 17/02A61K 31/21A61K 31/573
48
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Claims

Abstract

A pharmaceutical composition contains a nitric oxide donor and advantageously an optional corticosteroid and/or topical anesthetic. The composition is useful in a method for treating anal disorders such as anal fissure, anal ulcer, hemorrhoidal disease, levator spasm, and so forth, by topical application to or proximate the affected area.

Claims

exact text as granted — not AI-modified
What is claimed is:  
     
         1 . A pharmaceutical composition useful for topical treatment of an anal disease, said composition comprising an organic nitric oxide donor in combination with a carrier, in a form selected from the group consisting of a powder, an aerosol, a liquid to include a thickened liquid, an ointment and a suppository; wherein if the organic nitric oxide donor is only nitroglycerin and the composition is a soft paraffin or petroleum based ointment then the nitroglycerin is present in an amount excluding 2.0% by weight.  
     
     
         2 . The composition of  claim 1 , wherein the organic nitric oxide donor is nitroglycerin.  
     
     
         3 . The composition of  claim 2 , which is an ointment.  
     
     
         4 . The composition of  claim 1 , wherein nitroglycerin is the organic nitric oxide donor, present in an amount from about 0.25 to about 0.45 percent by weight, in an ointment.  
     
     
         5 . The composition of  claim 1 , wherein nitroglycerin is the organic nitric oxide donor, present in an amount from about 0.07 to about 0.15 percent by weight, in an ointment.  
     
     
         6 . The composition of  claim 1 , which is a suppository.  
     
     
         7 . The composition of  claim 1 , wherein the organic nitric oxide donor includes at least one organic nitrate represented by the following general formula:  
       R(—CR′R″—O—NO 2 ) x    
       wherein: 
 R, R′ and R″ are, independently at each occurrence, organic or hydro moiety or covalent bond, and  
 x is an integer from 1 to about 12.  
 
     
     
         8 . The composition of  claim 7 , wherein 
 R is a 2 to about 12 carbon hydrocarbon or oxygen-substituted hydrocarbon;    R′ is of 2 to 6 carbons and from 0 to 2 oxygen(s), a hydra moiety or a covalent bond;    R″ is a hydro moiety; and    x is from 2 to 6.    
     
     
         9 . The composition of  claim 8 , which excludes nitroglycerin; ethylene glycol dinitrate; isopropyl nitrate; glyceryl-1-mononitrate; glyceryl-1,2-dinitrate; glyceryl-1,3-dinitrate; butane-1,2,4-triol-trinitrate; erythrityl tetranitrate; pentaerythrityl tetranitrate; isosorbide mononitrate; and isosorbide dinitrate.  
     
     
         10 . The composition of  claim 1 , wherein the organic nitric oxide donor includes at least one organic nitrate selected from the group consisting of ethylene glycol dinitrate; isopropyl nitrate; glyceryl-1-mononitrate; glyceryl-1,2-dinitrate; glyceryl-1,3-dinitrate; butane-1,2,4-triol-trinitrate; erythrityl tetranitrate; pentaerythrityl tetranitrate; isosorbide mononitrate; and isosorbide dinitrate, in an ointment or suppository form.  
     
     
         11 . The composition of  claim 1 , wherein the organic nitrate donor is selected from the group consisting of one or more of erythrityl tetranitrate; pentaerythrityl tetranitrate; and isosorbide dinitrate.  
     
     
         12 . A pharmaceutical composition useful for treating anal disease comprising an organic nitric oxide donor in combination with a corticosteroid and a pharmaceutically acceptable topical carrier.  
     
     
         13 . The composition of  claim 12 , wherein the organic nitric oxide donor is nitroglycerin.  
     
     
         14 . The composition of  claim 13 , wherein the corticosteroid is hydrocortisone.  
     
     
         15 . The composition of  claim 12 , wherein a topical anesthetic is also present.  
     
     
         16 . A pharmaceutical composition useful for treating anal disease comprising an organic nitric oxide donor in combination with a topical anesthetic and a carrier.  
     
     
         17 . The composition of  claim 16 , wherein the organic nitric oxide donor is nitroglycerin.  
     
     
         18 . The composition of  claim 17 , wherein the topical anesthetic is dibucaine.  
     
     
         19 . A method for treating an anal disease comprising contacting an appropriate anal area with an effective amount of nitric oxide.  
     
     
         20 . The method of  claim 19 , wherein the nitric oxide is delivered by release from an organic nitric oxide donor.  
     
     
         21 . The method of  claim 20 , wherein the organic nitric oxide donor is an organic nitrate represented by the following general formula: 
       R(—CR′R″—O—NO 2 ) x    
       wherein: 
 R, R′ and R″ are, independently at each occurrence organic or hydro moiety or covalent bond, and  
 x is an integer from 1 to about 12.  
 
     
     
         22 . The method of  claim 21 , wherein 
 R is a 2 to about 12 carbon hydrocarbon or oxygen-substituted hydrocarbon;    R′ is of 2 to 6 carbons and from 0 to 2 oxygen(s), a hydro moiety or a covalent bond;    R″ is a hydro moiety; and    x is from 2 to 6.    
     
     
         23 . The method of  claim 20 , wherein the organic nitric oxide donor is nitroglycerin.  
     
     
         24 . The method of  claim 20 , wherein at least one agent selected from the group consisting of a corticosteroid and a topical anesthetic is employed in conjunction with the nitric oxide donor.  
     
     
         25 . The method of  claim 21 , wherein at least one agent selected from the group consisting of a corticosteroid and a topical anesthetic is employed in conjunction with the nitric oxide donor.  
     
     
         26 . The method of  claim 25 , wherein the corticosteroid is hydrocortisone, and the topical anesthetic is dibucaine.  
     
     
         27 . The method of  claim 19 , wherein anal pain is controlled thereby.  
     
     
         28 . The method of  claim 19 , wherein the anal disease is anal fissure or ulcer.  
     
     
         29 . The method of  claim 19 , wherein the anal disease is hemorrhoid disease.  
     
     
         30 . The method of  claim 19 , wherein the anal disease is levator spasm.  
     
     
         31 . The method of  claim 28 , wherein nitroglycerin is employed.  
     
     
         32 . The method of  claim 29 , wherein nitroglycerin is employed.  
     
     
         33 . The method of  claim 30 , wherein nitroglycerin is employed.  
     
     
         34 . The method of  claim 31 , wherein anal pain is controlled thereby.  
     
     
         35 . The method of  claim 32 , wherein anal pain is controlled thereby.  
     
     
         36 . The method of  claim 33 , wherein anal pain is controlled thereby.

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