RESUMEN
Nizatidine is an anti-secretogogue and a gastroprotective drug with a half-life of 1-2 h and is well absorbed in the stomach. This study aimed to optimize the process and develop floating microparticles of nizatidine that are based on low methoxyl pectin. Oil-in-oil dispersion method and Taguchi orthogonal array design were employed, and the prolonged residence time of the microparticles in the stomach was demonstrated. The constraints for independent variables, viz. A-polymer, B-internal solvent volume, C-surfactant, D-stirring rate and E-stirring time were set to generate the experimental runs. Particle size, percentage yield, micromeritic properties, entrapment efficiency, in vitro buoyancy and in vitro release were characterized. Surface morphology, zeta potential, in vitro release kinetics and in vivo floating performance of the optimized formulation was examined. The microparticles were free-flowing, irregular in shape and had a mean particle size distribution of 73-187 µ. Low methoxyl pectin played a predominant role in achieving buoyancy and optimum gastric retention for the modified release of the drug, suggesting Korsmeyer-Peppas model as the possible release mechanism. In vivo radiographic study in rabbits revealed that the drug was retained in the stomach for a period of 6 h. These results indicate that nizatidine floating microparticulate system provides modified drug release for the effective treatment of gastric ulcer
Asunto(s)
Animales , Masculino , Femenino , Conejos , Estómago/efectos de los fármacos , Nizatidina/antagonistas & inhibidores , Eficiencia/clasificación , Solventes/efectos adversos , Úlcera Gástrica/patología , Técnicas In Vitro/instrumentación , Preparaciones Farmacéuticas/administración & dosificación , Cinética , Espectroscopía Infrarroja por Transformada de Fourier/métodos , Liberación de FármacosRESUMEN
The present study investigates the anti-inflammatory activity of methanolic and chloroform extracts of Tragia cannabina. The whole plant of Tragia cannabina was extracted with methanol and chloroform by using soxhlet appara-tus. The effect of both extracts of Tragia cannabina was studied on carrageenan induced paw edema. The methanolic extract decreased the edema induced in hind paw. The percentage inhibition of paw edema was maximum with methanolic and chloroform extracts of Tragia cannabina at 300mg/kg body weight and has showed significant anti-inflammatory activity. It has been concluded that both the methanolic and chloroform extracts of Tragia cannabina showed significant anti-inflammatory activity comparable to that of reference standard Ibuprofen.
RESUMEN
The present study investigates the anti-inflammatory activity of methanolic and chloroform extracts of Tragia cannabina. The whole plant of Tragia cannabina was extracted with methanol and chloroform by using soxhlet appara-tus. The effect of both extracts of Tragia cannabina was studied on carrageenan induced paw edema. The methanolic extract decreased the edema induced in hind paw. The percentage inhibition of paw edema was maximum with methanolic and chloroform extracts of Tragia cannabina at 300mg/kg body weight and has showed significant anti-inflammatory activity. It has been concluded that both the methanolic and chloroform extracts of Tragia cannabina showed significant anti-inflammatory activity comparable to that of reference standard Ibuprofen.