Methods and compositions for treating pain of the mucous membrane

Abstract

Compositions useful for long-lasting pain relief from mucosal damage, such as mucosal inflamation, abrasions, ulcerations, lesions, trauma and incisions, without significant systemic absorption. The compositions of the invention are particularly suitable for application to the mucous membrane of the nasal cavity and buccal cavity. To relieve pain, the compositions or the invention are topically applied directly to the affected area.

What is claimed is:  
     
         1 . A composition comprising a mucoadhesive, a local anesthetic or a pharmaceutically-acceptable salt thereof, and an opioid or a pharmaceutically-acceptable salt thereof.  
     
     
         2 . The composition of  claim 1 , wherein an amount of the local anesthetic is within a range of from about 0.01 percent to about 0.5 percent of a total weight of the composition.  
     
     
         3 . The composition of  claim 1 , wherein an amount of the opioid is within a range of from about 0.05 percent to about 1 percent of a total weight of the composition.  
     
     
         4 . The composition of  claim 1 , wherein an amount of the mucoadhesive is within a range of from about 0.1 percent to about 40 percent of a total weight of the composition.  
     
     
         5 . The composition of  claim 1 , wherein an amount of the mucoadhesive is within a range of from about 15 percent to about 25 percent of a total weight of the composition.  
     
     
         6 . The composition of  claim 1 , wherein the mucoadhesive is a block copolymer of ethylene oxide and propylene oxide.  
     
     
         7 . The composition of  claim 1 , wherein the mucoadhesive is a block copolymer of ethylene oxide and propylene oxide of a formula I:  
       
         
           
           
               
               
           
         
       
       wherein x is an integer having an average value ranging from about 2 to about 128; y is an integer having an average value ranging from about 14 to about 80; and z is an integer having an average value ranging from 2 to about 128.  
     
     
         8 . The composition of  claim 1 , wherein the mucoadhesive is poloxamer 407.  
     
     
         9 . The composition of  claim 1 , wherein the local anesthetic is selected from the group consisting of lidocaine, tetracaine, bupivacaine, prilocaine, mepivacaine, procaine, chloroprocaine, ropivacaine, dibucaine, etidocaine, benzocaine, a pharmaceutically-acceptable salt thereof, and a mixture thereof.  
     
     
         10 . The composition of  claim 1 , wherein the local anesthetic is lidocaine or a pharmaceutically-acceptable salt thereof.  
     
     
         11 . The composition of  claim 1 , wherein the opioid is morphine or loperamide or a pharmaceutically-acceptable salt thereof.  
     
     
         12 . The composition of  claim 1 , wherein the opioid is morphine or a pharmaceutically-acceptable salt thereof.  
     
     
         13 . A container adapted for topical application containing a composition comprising a mucoadhesive, a local anesthetic or a pharmaceutically-acceptable salt thereof, and an opioid or a pharmaceutically-acceptable salt thereof.  
     
     
         14 . The container of  claim 13 , packaged in association with instructions, the instructions comprising: topically applying the composition onto a mucous membrane of a subject.  
     
     
         15 . The container of  claim 13 , wherein the mucoadhesive is a block copolymer of ethylene oxide and propylene oxide.  
     
     
         16 . The container of  claim 13 , wherein the mucoadhesive is a block copolymer of ethylene oxide and propylene oxide of a formula I:  
       
         
           
           
               
               
           
         
       
       wherein x is an integer having an average value ranging from about 2 to about 128; y is an integer having an average value ranging from about 14 to about 80; and z is an integer having an average value ranging from 2 to about 128.  
     
     
         17 . The container of  claim 13 , wherein the mucoadhesive is poloxamer 407.  
     
     
         18 . The container of  claim 13 , wherein the local anesthetic is selected from the group consisting of lidocaine, tetracaine, bupivacaine, prilocaine, mepivacaine, procaine, chloroprocaine, ropivacaine, dibucaine, etidocaine, benzocaine, a pharmaceutically-acceptable salt thereof, and a mixture thereof.  
     
     
         19 . The container of  claim 13 , wherein the local anesthetic is lidocaine or a pharmaceutically-acceptable salt thereof.  
     
     
         20 . The container of  claim 13 , wherein the opioid is morphine or loperamide or a pharmaceutically-acceptable salt thereof.  
     
     
         21 . The container of  claim 13 , wherein the opioid is morphine or a pharmaceutically-acceptable salt thereof.  
     
     
         22 . A method of inducing local anesthesia in a subject comprising topically applying a composition comprising a mucoadhesive, a local anesthetic or a pharmaceutically-acceptable salt thereof, and an opioid or a pharmaceutically-acceptable salt thereof to a subject.  
     
     
         23 . The method of  claim 22 , wherein the composition is applied to the buccal mucous membrane.  
     
     
         24 . The method of  claim 22 , wherein an amount of the local anesthetic is within a range of from about 0.01 percent to about 0.5 percent of a total weight of the composition.  
     
     
         25 . The method of  claim 22 , wherein an amount of the opioid is within a range of from about 0.05 percent to about 1 percent of a total weight of the composition.  
     
     
         26 . The method of  claim 22 , wherein an amount of the mucoadhesive is within a range of from about 0.1 percent to about 40 percent of a total weight of the composition.  
     
     
         27 . The method of  claim 22 , wherein an amount of the mucoadhesive is within a range of from about 15 percent to about 25 percent of a total weight of the composition.  
     
     
         28 . The method of  claim 22 , wherein the mucoadhesive is a block copolymer of ethylene oxide and propylene oxide.  
     
     
         29 . The method of  claim 22 , wherein the mucoadhesive is a block copolymer of ethylene oxide and propylene oxide of a formula I:  
       
         
           
           
               
               
           
         
       
       wherein x is an integer having an average value ranging from about 2 to about 128; y is an integer having an average value ranging from about 14 to about 80; and z is an integer having an average value ranging from 2 to about 128.  
     
     
         30 . The method of  claim 22 , wherein the mucoadhesive is poloxamer 407.  
     
     
         31 . The method of  claim 22 , wherein the local anesthetic is selected from the group consisting of lidocaine, tetracaine, bupivacaine, prilocaine, mepivacaine, procaine, chloroprocaine, ropivacaine, dibucaine, etidocaine, benzocaine, a pharmaceutically-acceptable salt thereof, and a mixture thereof.  
     
     
         32 . The method of  claim 22 , wherein the local anesthetic is lidocaine or a pharmaceutically-acceptable salt thereof.  
     
     
         33 . The method of  claim 22 , wherein the opioid is morphine or loperamide or a pharmaceutically-acceptable salt thereof.  
     
     
         34 . The method of  claim 22 , wherein the opioid is morphine or a pharmaceutically-acceptable salt thereof.