Transdermally absorbable base material containing lipid peptide compound

Abstract

A transdermally absorbable base material including: a lipid peptide compound including at least one of compound of Formula (1) below and the similar compounds or pharmaceutically usable salts thereof; a surfactant; a specific polyhydric alcohol; a fatty acid; and water, wherein R 1 is a C 9-23 aliphatic group; R 2 is a hydrogen atom or a C 1-4 alkyl group that optionally has a branched chain having a carbon atom number of 1 or 2; R 3 is a —(CH 2 ) n —X group; n is a number of 1 to 4; and X is amino group, guanidino group, —CONH 2 group, or a 5-membered cyclic group optionally having 1 to 3 nitrogen atoms, a 6-membered cyclic group optionally having 1 to 3 nitrogen atoms, or a condensed heterocyclic group constituted by a 5-membered cyclic group and a 6-membered cyclic group which optionally have 1 to 3 nitrogen atoms.

1 . A transdermally absorbable base material comprising:
 a lipid peptide compound including at least one of compounds of Formulae (1) to (3) below or pharmaceutically usable salts thereof;   a surfactant;   1,2-alkanediol or glycerin;   at least one fatty acid; and   water,   
       
         
           
           
               
               
           
         
         (wherein R 1  is a C 9-23  aliphatic group; R 2  is a hydrogen atom or a C 1-4  alkyl group that optionally has a branched chain having a carbon atom number of 1 or 2; R 3  is a —(CH 2 ) n —X group; n is a number of 1 to 4; and X is amino group, guanidino group, —CONH 2  group, or a 5-membered cyclic group optionally having 1 to 3 nitrogen atoms, a 6-membered cyclic group optionally having 1 to 3 nitrogen atoms, or a condensed heterocyclic group constituted by a 5-membered cyclic group and a 6-membered cyclic group which optionally have 1 to 3 nitrogen atoms.) 
       
       
         
           
           
               
               
           
         
         (wherein R 4  is a C 9-23  aliphatic group; R 5  to R 7  are each independently a hydrogen atom, a C 1-4  alkyl group that optionally has a branched chain having a carbon atom number of 1 or 2, or —(CH 2 ) n —X group; n is a number of 1 to 4; and X is amino group, guanidino group, —CONH 2  group, or a 5-membered cyclic group optionally having 1 to 3 nitrogen atoms, a 6-membered cyclic group optionally having 1 to 3 nitrogen atoms, or a condensed heterocyclic group constituted by a 5-membered cyclic group and a 6-membered cyclic group which optionally have 1 to 3 nitrogen atoms.) 
       
       
         
           
           
               
               
           
         
         (wherein R 8  is a C 9-23  aliphatic group; R 9  to R 12  are each independently a hydrogen atom, a C 1-4  alkyl group that optionally has a branched chain having a carbon atom number of 1 or 2, or —(CH 2 ) n —X group; n is a number of 1 to 4; and X is amino group, guanidino group, —CONH 2  group, or a 5-membered cyclic group optionally having 1 to 3 nitrogen atoms, a 6-membered cyclic group optionally having 1 to 3 nitrogen atoms, or a condensed heterocyclic group constituted by a 5-membered cyclic group and a 6-membered cyclic group which optionally have 1 to 3 nitrogen atoms.) 
       
     
     
         2 . The transdermally absorbable base material according to  claim 1 , wherein the lipid peptide compound is a compound of Formula (1), wherein R 1  is a linear aliphatic group having a carbon atom number of 15; R 2  is a hydrogen atom; and R 3  is 4-imidazole methyl group. 
     
     
         3 . The transdermally absorbable base material according to  claim 1 , being stick-shaped. 
     
     
         4 . The transdermally absorbable base material according to  claim 1 , further comprising at least one oleaginous base material. 
     
     
         5 . The transdermally absorbable base material according to an one of  claim 1 , further comprising at least one organic acid. 
     
     
         6 . The transdermally absorbable base material according to  claim 1 , comprising, as the surfactant, at least one compound selected from the group consisting of ethylene glycol alkyl ethers, phospholipid, and polyglycerin fatty acid esters. 
     
     
         7 . The transdermally absorbable base material according to  claim 1 , further comprising polyoxyethylene (20) sorbitan monolaurate (CAS registry number 9005-64-5) as the surfactant. 
     
     
         8 . The transdermally absorbable base material according to  claim 1 , wherein the fatty acid is stearic acid. 
     
     
         9 . The transdermally absorbable base material according to  claim 5 , wherein the organic acid is at least one selected from the group consisting of oxalic acid, citric acid, and ascorbic acid. 
     
     
         10 . The transdermally absorbable base material according to  claim 1 , being used for cosmetics or pharmaceutical products. 
     
     
         11 . A premix for a transdermally absorbable base material, the premix comprising:
 a lipid peptide compound including at least one of compounds of Formulae (1) to (3) below or pharmaceutically usable salts thereof;   a surfactant;   1,2-alkanediol or glycerin; and   at least one fatty acid,   
       
         
           
           
               
               
           
         
         (wherein R 1  is a C 9-23  aliphatic group; R 2  is a hydrogen atom or a C 1-4  alkyl group that optionally has a branched chain having a carbon atom number of 1 or 2; R 3  is a —(CH 2 ) n —X group; n is a number of 1 to 4; and X is amino group, guanidino group, —CONH 2  group, or a 5-membered cyclic group optionally having 1 to 3 nitrogen atoms, a 6-membered cyclic group optionally having 1 to 3 nitrogen atoms, or a condensed heterocyclic group constituted by a 5-membered cyclic group and a 6-membered cyclic group which optionally have 1 to 3 nitrogen atoms.) 
       
       
         
           
           
               
               
           
         
         (wherein R 4  is a C 9-23  aliphatic group; R 5  to R 7  are each independently a hydrogen atom, a C 1-4  alkyl group that optionally has a branched chain having a carbon atom number of 1 or 2, or —(CH 2 ) n —X group; n is a number of 1 to 4; and X is amino group, guanidino group, —CONH 2  group, or a 5-membered cyclic group optionally having 1 to 3 nitrogen atoms, a 6-membered cyclic group optionally having 1 to 3 nitrogen atoms, or a condensed heterocyclic group constituted by a 5-membered cyclic group and a 6-membered cyclic group which optionally have 1 to 3 nitrogen atoms.) 
       
       
         
           
           
               
               
           
         
         (wherein R 8  is a C 9-23  aliphatic group; R 9  to R 12  are each independently a hydrogen atom, a C 1-4  alkyl group that optionally has a branched chain having a carbon atom number of 1 or 2, or —(CH 2 ) n —X group; n is a number of 1 to 4; and X is amino group, guanidino group, —CONH 2  group, or a 5-membered cyclic group optionally having 1 to 3 nitrogen atoms, a 6-membered cyclic group optionally having 1 to 3 nitrogen atoms, or a condensed heterocyclic group constituted by a 5-membered cyclic group and a 6-membered cyclic group which optionally have 1 to 3 nitrogen atoms.)