RESUMEN
In an effort to discover new candidates with improved antimicrobial activities we report here the synthesis and in vitro biological evalution of various series of 2-(N-methylamino)-4-(N,N-dimethylamino)-6-(arylthioureido)-s-triazine (5a-j) and (N-methylamino)-4-(N,N-dimethylamino)-6-(arylureido)-s-triazine (6a-j). All the synthesized compounds were screened in vitro for their antibacterial activity against two different gram-positive bacteria (S. aureus, B. subtilis) and two different gram-negative bacteria (P. aeruginosa, E. coli) using the broth dilution method.
Asunto(s)
Antibacterianos/síntesis química , Antibacterianos/farmacología , Compuestos Heterocíclicos/síntesis química , Compuestos Heterocíclicos/farmacología , Triazinas/química , Antibacterianos/química , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Compuestos Heterocíclicos/química , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Espectrofotometría InfrarrojaRESUMEN
Transdermal films of the furosemide were developed employing ethyl cellulose and hydroxypropyl methylcellulose as film formers. The effect of binary mixture of polymers and penetration enhancers on physicochemical parameters including thickness, moisture content, moisture uptake, drug content, drug-polymer interaction, and in vitro permeation was evaluated. In vitro permeation study was conducted using human cadaver skin as penetration barrier in modified Keshary-Chein diffusion cell. In vitro skin permeation study showed that binary mixture, ethyl cellulose (EC)/hydroxypropyl methylcellulose (HPMC), at 8.5:1.5 ratio provided highest flux and also penetration enhancers further enhanced the permeation of drug, while propylene glycol showing higher enhancing effect compared to dimethyl sulfoxide and isopropyl myristate. Different kinetic models, used to interpret the release kinetics and mechanism, indicated that release from all formulations followed apparent zero-order kinetics and non-Fickian diffusion transport except formulation without HPMC which followed Fickian diffusion transport. Stability studies conducted as per International Conference on Harmonization guidelines did not show any degradation of drug. Based on the above observations, it can be reasonably concluded that blend of EC-HPMC polymers and propylene glycol are better suited for the development of transdermal delivery system of furosemide.