PURPOSE: To obtain a pharmaceutical formulation which is discharged rapidly and completely at a site to be treated and which containes an active substance in a stable form as a micelle where a heterocyclic compd. contg. a specified N-alkylated quaternary nitrogen and a hydrophobic pharmaceutically active substance are dispersed in a solvent.
CONSTITUTION: A pharmaceutical preparation comprises micelles of a compd. of formula I (wherein X is CH, C-OH or N; Y is N, S or CH; each of R1 and R2 is H, CH3 or OH; n is 8-20, preferably 15; Z- is ion of Cl, Br, I, formate acetate, propionate, maleate, hydrogensulfate, malate, fumarate, salicylate, alginate, gluconate, glucuronate, galacturonate, ethylsulfate, hydrogenphosphate] such as a 4-substd. 2-n-alkyl-pyrazolium compd. or 1-n-alkyl-4-subsd. imidazolium compd., 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.
| US4207326A | 1980-06-10 |