| 摘要 |
PURPOSE: To obtain a medicine preparation containing an active substance in a stable form, capable of quickly and completely releasing the active substance, comprising a micelle prepared by dispersing a specific N-alkylated quaternary nitrogen-containing heterocyclic compound and a hydrophobic medicine active substance into a solvent. CONSTITUTION: This medicine preparation comprises a micelle which is obtained by dispersing a 2,5,6-substituted-N1 -alklpyrimidinium compound of the formula [(i) R1 =R2 =R3 =H, (ii) R1 =NH2 , R2 =OH, R3 =H, (iii) R1 =R2 =OH, R3 =H, F or CH3 , (iv) R1 =F, R2 =OH and R3 =H; (n) is 8-20, especially 15; Z<-> is each ion of Cl, Br, I, maleic acid, formic acid, acetic acid, propionic acid, hydrogensulfate, malic acid, fumaric acid, salicylic acid, alginic acid, gluconic acid, glucuronic acid, galacturonic acid, ethyl sulfate or hydrogenphosphate] and a hydrophobic medicine active substance into a solvent having pH<=7 and has 1.0×10<-7> to 1.5×10<-4> mol/L critical micelle formation concentration. The compound of the formula has strong antimicrobial and fungicidal effects. |
