Transdermal delivery of doxylamine succinate and pyridoxine hydrochloride

Abstract

Pharmaceutical compositions for simultaneous transdermal delivery of Doxylamine and Pyridoxine comprising Doxylamine or its salts, Pyridoxine or its salts or its active metabolites and a vehicle system wherein pharmaceutical compositions are liquid formulations, semisolid formulations and polymer matrices. Further pharmaceutical compositions can be incorporated into transdermal delivery systems or transdermal patches. The invention provides a method for treatment of nausea and vomiting in general, and for pregnant women in particular by continuous and simultaneous transdermal delivery of Doxylamine and Pyridoxine. This is to be accomplished through topical application of pharmaceutical compositions or by application of a transdermal delivery system or transdermal patch to the surface of the skin wherein the duration of application is once in a day, once every two days, once every three days, once every four days, once every five days, once every six days, or once in a week.

What is claimed is: 
     
         1 . A transdermal pharmaceutical composition in a polymer matrix comprising:
 A first active agent selected from the group consisting of Doxylamine free base, a pharmaceutically acceptable salt of Doxylamine, and combinations thereof;   A second active agent selected from the group consisting of Pyridoxine free base, a pharmaceutically acceptable salt of Pyridoxine, active metabolites thereof, and combinations thereof; and   a vehicle system wherein the vehicle system comprises excipients selected from the group consisting of solvents, enhancers, plasticizers, polymers, pH adjusting agents, and combinations thereof.   
     
     
         2 . The transdermal pharmaceutical composition of  claim 1  wherein:
 Doxylamine is present in an amount selected from the group consisting of between 0.5-49 wt %, between 2-30 wt %, and between 5-20 wt %; 
 Pyridoxine is present in an amount selected from the group consisting of between 0.5-49 wt %, between 2-30 wt %, and between 5-20 wt %; and 
 wherein the vehicle system is present in an amount selected from the group consisting of between 2-99 wt %, between 40-96 wt %, and between 60-90 wt %. 
 
     
     
         3 . A method of treating and/or preventing nausea or nausea and vomiting in a patient comprising:
 selecting a patient in need of treating and/or preventing nausea or nausea and vomiting;   administering to the patient the transdermal pharmaceutical composition of  claim 1 ,   wherein nausea or nausea and vomiting is treated and/or prevented in the patient.   
     
     
         4 . The method of  claim 3 , wherein the application is topical and wherein frequency of topical application is selected from the group consisting of once in a day, once in two days, once in three days, once in four days, once in five days, once in six days, once in a week, once in ten days, and once in fifteen days. 
     
     
         5 . A method of treating and/or preventing nausea and vomiting in pregnancy (NVP) in a patient comprising:
 selecting a patient in need of treating and/or preventing NVP;   administering to the patient the transdermal pharmaceutical composition of  claim 1 ,   wherein NVP is treated and/or prevented in the patient.   
     
     
         6 . The method of  claim 5 , wherein the administering is topical application and wherein the frequency of topical application is selected from the group consisting of once in a day, once in two days, once in three days, once in four days, once in five days, once in six days, once in a week, once in ten days, and once in fifteen days. 
     
     
         7 . A transdermal pharmaceutical composition in a polymer matrix comprising:
 At least one active agent selected from the group consisting of Doxylamine free base, a pharmaceutically acceptable salt of Doxylamine, and combinations thereof; and   a vehicle system wherein the vehicle system comprises excipients selected from the group consisting of solvents, enhancers, plasticizers, polymers, pH adjusting agents, and combinations thereof.   
     
     
         8 . The pharmaceutical composition of  claim 7  wherein:
 Doxylamine is present in an amount selected from the group consisting of between 0.5-80 wt %, between 2-30 wt %, and between 5-20 wt %; and 
 wherein the vehicle system is present in an amount selected from the group consisting of between 20-99.5 wt %, between 70-98 wt %, and between 80-95 wt %. 
 
     
     
         9 . A method of treating and/or preventing nausea or nausea and vomiting in a patient comprising:
 selecting a patient in need of treating and/or preventing nausea or nausea and vomiting;   administering to the patient the transdermal pharmaceutical composition of  claim 7 ,   wherein nausea or nausea and vomiting is treated and/or prevented in the patient.   
     
     
         10 . The method of  claim 9 , wherein the application is topical and wherein frequency of topical application is selected from the group consisting of once in a day, once in two days, once in three days, once in four days, once in five days, once in six days, once in a week, once in ten days, and once in fifteen days. 
     
     
         11 . A method of treating and/or preventing nausea and vomiting in pregnancy (NVP) in a patient comprising:
 selecting a patient in need of treating and/or preventing NVP;   administering to the patient the transdermal pharmaceutical composition of  claim 7 ,   wherein NVP is treated and/or prevented in the patient.   
     
     
         12 . The method of  claim 11 , wherein the administering is topical application and wherein the frequency of topical application is selected from the group consisting of once in a day, once in two days, once in three days, once in four days, once in five days, once in six days, once in a week, once in ten days, and once in fifteen days. 
     
     
         13 . A transdermal pharmaceutical composition in a polymer matrix comprising:
 At least one active agent selected from the group consisting of Pyridoxine free base, a pharmaceutically acceptable salt of pyridoxine, active metabolites thereof, and combinations thereof; and   a vehicle system wherein the vehicle system comprises excipients selected from the group consisting of solvents, enhancers, plasticizers, polymers, pH adjusting agents, and combinations thereof.   
     
     
         14 . The pharmaceutical composition of  claim 13  wherein:
 Pyridoxine is present in an amount selected from the group consisting of between 0.5-80 wt %, between 2-30 wt %, and between 5-20 wt %; and 
 wherein the vehicle system is present in an amount selected from the group consisting of between 20-99.5 wt %, between 70-98 wt %, and between 80-95 wt %. 
 
     
     
         15 . A method of treating and/or preventing nausea or nausea and vomiting in a patient comprising:
 selecting a patient in need of treating and/or preventing nausea or nausea and vomiting;   administering to the patient the transdermal pharmaceutical composition of  claim 13 ,   wherein nausea or nausea and vomiting is treated and/or prevented in the patient.   
     
     
         16 . The method of  claim 15 , wherein the application is topical and wherein frequency of topical application is selected from the group consisting of once in a day, once in two days, once in three days, once in four days, once in five days, once in six days, once in a week, once in ten days, and once in fifteen days. 
     
     
         17 . A method of treating and/or preventing nausea and vomiting in pregnancy (NVP) in a patient comprising:
 selecting a patient in need of treating and/or preventing NVP;   administering to the patient the transdermal pharmaceutical composition of  claim 13 ,   wherein NVP is treated and/or prevented in the patient.   
     
     
         18 . The method of  claim 17 , wherein the administering is topical application and wherein the frequency of topical application is selected from the group consisting of once in a day, once in two days, once in three days, once in four days, once in five days, once in six days, once in a week, once in ten days, and once in fifteen days.