Priprava i evaluacija novog derivata eritromicina – eritromicin taurat

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

Priprava i evaluacija novog derivata eritromicina – eritromicin taurat

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

Design and Evaluation of Diclofenac Sodium MegaloporousMatrix System Aimed forColonic Drug Delivery: Design of a matrix system for diclofenac delivery

Megaloporous controlled release tablets of diclofenac sodium (DS) were preparedwith two kinds of granules. One of them is the restraining-phase matrix granule(RMG) and it controls the release rate of the drug. The other one is the solublehousing-phase matrix granule (HMG) and controls liquid penetration into thesystem. Carnauba wax and Eudragit L100 polymers were used to constitute therestraining and housing matrix phases, respectively. The prepared tablets wereevaluated for various parameters. In vitrodrug release study was carried out insimulated gastric fluid (pH 1.2) for the first 2 h and in phosphate buffer (pH 7.2)for the next 10 h following USP25 paddle method. Two independent modelmethods, AUC and Lin Ju and Liaw's difference factor (ƒ1) and similarity factor (ƒ2)were used to compare various dissolution profiles. The fabricated megaloporousmatrix tablets released only 3 to 5% of DS in pH 1.2 depending on the proportionof carnauba wax used in the RMG. Increase in polymer content/hardness value ofthe tablet resulted in a significant decrease in AUC0-2h and AUC2-12h values . Thef1and f2analysis also confirms the discrimination between corresponding dissolutionpairs. The dissolution profiles of an ideal matrix formulation containing 15.77%carnauba wax and 6.76% Eudragit L100 was found to be comparable with thereference product (Voveran®SR) and theoretical release profile. The drug releasefrom all fabricated products and reference product followed better Higuchi modelthan the zero order and first order kinetic models. Ritger-Peppas model analysisindicated that the DS release followed non-Fickian transport mechanism. From theabove analysis, it is evident that the release mechanism of DS from matrix tabletis influenced by both hardness and polymer contents. The stability profiles indicatethat the physico-chemical properties of the tablets are not affected on storage at 45°C/75% RH up to 6 months