Priprava i evaluacija novog derivata eritromicina – eritromicin taurat

Abstract

Erythromycin taurate, a new derivative of erythromycin, was prepared by reacting the erythromycin base with tauric acid and its physico-chemical and biological properties were evaluated. The derivative has reasonably good solubility in organic solvents. The partition coefficient values in chloroform/water 1.17 and octanol/water 1.16 systems indicate its good distribution in various tissues in vivo. The in vitro antimicrobial potency of the derivative (833.33 microgramms per mg) is higher than the existing derivatives such as erythromycin estolate, erythromycin stearate, erythromycin ethyl succinate, erythromycin gluceptate, erythromycin lactobionate. The antimicrobial spectrum is comparable to that of the parent compound. Our results indicate that erythromycin taurate has a high potential for possible clinical application and is more efficient against Escherichia coli and Klebsiella pneumoniae than the parent base.Eritromicin taurat pripravljen je reakcijom eritromicin baze s taurinskom kiselinom. U radu su evaluirana fizičko-kemijska i biološka svojstva ovog novog derivata eritromicina. Eritromicin taurat je relativno dobro topljiv u organskim otapalima. Koeficijent razdjeljenja u sustavu kloroform/voda bio je 1,17 a u sustavu oktanol/voda 1,16 što ukazuje da se ova ljekovita tvar može dobro raspodijeliti u različitim tkivima in vivo. Antimikrobna aktivnost in vitro (833,33 g mg-1) je veća od aktivnosti postojećih derivata eritromicina: estolata, stearata, etil sukcinata, gluceptata, laktobionata. Spektar antimikrobnog djelovanja je sličan spektru samog eritromicina. Zbog svega toga moguća je klinička primjena eritromicin taurata

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