Novel interstitial therapy for immediate symptom relief and chronic therapy in interstitial cystitis

Abstract

The present invention relates to u disorder of the lower urinary tract, and in particular, reducing the symptoms (including treatment) of interstitial cystitis in vivo. In a preferred embodiment, the present invention relates to treatment formulations and methods for reducing interstitial cystitis in patients.

1 . A composition for intravesical instillation into the bladder, wherein said composition consists of:
 (i) a heparinoid selected from the group consisting of sodium pentosanpolysulfate, chondroitin sulfate, heparan sulfate, and hyaluronic acid;   (ii) a local anesthetic agent selected from the group consisting of lidocaine, bupivacaine, and mepivacaine;   (iii) a buffer selected from the group consisting of phosphate buffer, MOPS buffer, HEPES buffer, and Tris buffer; and   (iv) optionally an osmolar component selected from the group consisting of sodium chloride, dextrose, dextran 40, dextran 60, starch and mannitol;   
       wherein said composition treats interstitial cystitis or at least one symptom thereof when instilled into the bladder; 
       wherein, when the heparinoid is sodium pentosanpolysulfate, the sodium pentosanpolysulfate is present in about 1 mg to about 600 mg per unit dose; 
       wherein, when the heparinoid is chondroitin sulfate, the chondroitin sulfate is present in about 1 mg to about 10,000 mg per unit dose; 
       wherein, when the heparinoid is heparan sulfate, the heparan sulfate is present in about 0.5 mg to about 10,000 mg per unit dose; and 
       wherein, when the heparinoid is hyaluronic acid, the hyaluronic acid is present in about 5 mg to about 600 mg per unit dose. 
     
     
         2 . The composition of  claim 1 , wherein the heparinoid is sodium pentosanpolysulfate. 
     
     
         3 . The composition of  claim 1 , wherein the buffer is phosphate buffer. 
     
     
         4 . The composition of  claim 1 , wherein the local anesthetic agent is lidocaine. 
     
     
         5 . The composition of  claim 4  wherein the lidocaine is present in the composition in the quantity of 10 mg up to 400 mg lidocaine per unit dose. 
     
     
         6 . The composition of  claim 1  wherein the heparinoid is sodium pentosanpolysulfate, the buffer is phosphate buffer, and the local anesthetic is lidocaine. 
     
     
         7 . The composition of  claim 1  wherein the osmolar component is present in a sufficient amount so that the final solution is substantially isotonic. 
     
     
         8 . The composition of  claim 6  wherein the osmolar component is selected from the group consisting of sodium chloride, dextrose, dextran 40, and dextran 60. 
     
     
         9 . The composition of  claim 1  wherein the heparinoid is selected from the group consisting of chondroitin sulfate and hyaluronic acid. 
     
     
         10 . The composition of  claim 1  wherein the local anesthetic agent is selected from the group consisting of bupivacaine and mepivacaine. 
     
     
         11 . A composition for intravesical instillation into the bladder, wherein said composition consists of an aqueous solution of:
 (i) a heparinoid selected from the group consisting of sodium pentosanpolysulfate, chondroitin sulfate, heparan sulfate, and hyaluronic acid;   (ii) a local anesthetic agent other than cocaine,   (iii) a buffer selected from the group consisting of phosphate buffer, MOPS buffer, HEPES buffer, and Tris buffer, and   (iv) optionally an osmolar component selected from the group consisting of sodium chloride, dextrose, dextran 40, dextran 60, starch and mannitol,   
       wherein the composition has a pH from about 7 to about 9, and 
       wherein the composition treats interstitial cystitis or at least one symptom thereof when instilled into the bladder. 
     
     
         12 . The composition of  claim 11  wherein the heparinoid is sodium pentosanpolysulfate. 
     
     
         13 . The composition of  claim 11  wherein the local anesthetic agent other than cocaine is selected from the group consisting of lidocaine, bupivacaine, and mepivacaine. 
     
     
         14 . The composition of  claim 13  wherein the local anesthetic agent is lidocaine. 
     
     
         15 . The composition of  claim 14  wherein lidocaine is present in the composition in the quantity of 10 mg up to 400 mg lidocaine per unit dose. 
     
     
         16 . (canceled) 
     
     
         17 . The composition of  claim 1  wherein the buffer is Tris buffer. 
     
     
         18 . The composition of  claim 11  wherein the buffer is phosphate buffer. 
     
     
         19 . The composition of  claim 11  wherein the buffer is Tris buffer.