External preparation composition comprising fatty acid-based ionic liquid as active ingredient

Abstract

Disclosed is an external preparation composition having good transdermal absorbability. An external preparation composition having excellent transdermal absorbability can be produced by dissolving a medicinal substance or a salt thereof in a fatty acid-based ionic liquid to form a composite ionic composition of the medicinal substance. The external preparation composition can be used as a liquid preparation, an ointment, a cream, a plaster or the like, and enables to provide a preparation having excellent transdermal absorbability.

1 - 25 . (canceled) 
     
     
         26 . A nonaqueous external preparation composition comprising a drug or a salt thereof dissolved in a fatty acid-based ionic liquid having 5 to 20 carbon atoms,
 wherein the drug is a basic drug;   the fatty acid-based ionic liquid is an equimolar salt(s) of one or more fatty acid(s) and one or more organic amine compound(s), and is obtained from a fatty acid having 5 to 20 carbon atoms and an organic amine compound having 4 to 12 carbon atoms   
     
     
         27 . The external preparation composition according to  claim 26 , wherein the fatty acid having 5 to 20 carbon atoms is at least one selected from levulinic acid, capric acid, isostearic acid and oleic acid. 
     
     
         28 . The external preparation composition according to  claim 26 , wherein the organic amine compound having 4 to 12 carbon atoms is at least one selected from diethanolamine, triethanolamine, diisopropanolamine and triisopropanolamine. 
     
     
         29 . The external preparation composition according to  claim 26 , wherein the fatty acid-based ionic liquid comprises at least one selected from a combination of capric acid and diethanolamine; a combination of capric acid and triethanolamine; a combination of capric acid and diisopropanolamine; a combination oflevulinic acid and diethanolamine; a combination of levulinic acid and triethanolamine; and a combination of levulinic acid and diisopropanolamine. 
     
     
         30 . The external preparation composition according to  claim 26 , further comprising a fatty acid having 5 to 20 carbon atoms, in addition to the fatty acid-based ionic liquid. 
     
     
         31 . The external preparation composition according to  claim 26 , wherein the basic drug is a medicinal ingredient having at least one selected from primary amino group, secondary amino group and tertiary amino group. 
     
     
         32 . The external preparation composition according to  claim 26 , wherein the basic drug is a local anesthetic, a muscle relaxant, an analgesic or an opioid analgesic. 
     
     
         33 . The external preparation composition according to  claim 32 , wherein the local anesthetic is lidocaine. 
     
     
         34 . The external preparation composition according to  claim 32 , wherein the muscle relaxant is eperisone. 
     
     
         35 . The external preparation composition according to  claim 32 , wherein the analgesic is tramadol. 
     
     
         36 . The external preparation composition according to  claim 32 , wherein the opioid analgesic is morphine. 
     
     
         37 . A nonaqueous tape preparation comprising the external preparation composition according to  claim 26  formulated with a styrene-isoprene-styrene copolymer as a patch base. 
     
     
         38 . A transdermal absorption accelerator for a basic drug or a salt thereof, comprising as an active ingredient, a fatty acid-based ionic liquid which is an equimolar salt(s) of one or more fatty acid(s) having 5 to 20 carbon atoms and one or more organic amine compound(s) having 4 to 12 carbon atoms. 
     
     
         39 . The transdermal absorption accelerator for a basic drug or a salt thereof according to  claim 38 , wherein the fatty acid-based ionic liquid is equimolar salt(s) of one or more fatty acid(s) having 5 to 20 carbon atoms and one or more organic amine compound(s) having 4 to 12 carbon atoms, wherein the fatty acid is selected from levulinic acid, capric acid, isostearic acid or oleic acid and the organic amine compound is selected from diethanolamine, triethanolamine, diisopropanolamine or triisopropanolamine. 
     
     
         40 . The transdermal absorption accelerator for a basic drug or a salt thereof according to  claim 38 , wherein the fatty acid-based ionic liquid is a capric acid-based ionic liquid. 
     
     
         41 . The transdermal absorption accelerator for a basic drug or a salt thereof according to  claim 39 , wherein the fatty acid-based ionic liquid is a capric acid-based ionic liquid.