PURPOSE: To obtain a pharmaceutical formulation which is discharged rapidly and completely at a site to be treated and which contains an active substance in a stable form as a micelle where a heterocyclic compd. contg. specified N-alkylated quaternary nitrogen and a hydrophobic pharmaceutically active substance are dispersed in a solvent.
CONSTITUTION: A pharmaceutical formulation comprises micelles of a compd. of the formula I [wherein X is N, N+4-(CH2)n-CH3, CH, C-OH or formula II; R1 is H, formula III or OH; R2 is R1 or CONH2; n is 8-20, preferably 15; Z- is an ion of Cl, Br, I, formate, acetate, propionate, maleate, hydrogensulfate, malate, fumarate, salicylated, alginate, gluconate, glucuronate, galacturonate, ethylsulfate, hydrogenphosphate] such as an N-alkyl-4-hydroxypyridinium and a hydrophobic pharmaceutically active substance dispersed in a solvent having pH≤7, in which a critical micelle concentration is within a range of 1.0×10-7-1.50×10-4 mol/l. The compd. of the formula has strong antibacterial and antifungal effects.
| JPS59134726A | 1984-08-02 | |||
| JPS60197611A | 1985-10-07 | |||
| JPS604117A | 1985-01-10 | |||
| JPS5927999A | 1984-02-14 | |||
| JPS56139462A | 1981-10-30 | |||
| JPS5710141A | 1982-01-19 |