Gastro-Resistant Microparticles Containing Sodium Pantoprazole: Stability Studies and In Vivo Anti-Ulcer Activity

摘要

The aim of the present work was to verify the in vivo capacity of pantoprazole-loaded microparticles to protectthe gastric mucosa against ulcer formation and to evaluate their stability under accelerated conditions. Pantoprazoleloadedmicroparticles were prepared by spray-drying in pilot scale, using Eudragit? S100 as polymer. Transparent glassvials containing drug-loaded microparticles were stored for 6 months at 40°C and 75% RH. Photostability was tested underUVA light. Ulcers were induced by the oral administration of absolute ethanol to rats. Sodium bicarbonate solution,pantoprazole solution and drug-loaded microparticles were tested. Regarding the drug content during the accelerate stabilitystudy, samples showed complete encapsulation efficiency and were considered stable. The microencapsulation of pantoprazolereduced its photodegradation. The in vivo evaluation showed that the microparticles presented ulcer index lowerthan the solutions. Enteric microparticles had acceptable stability under accelerated conditions and were efficient in protectingthe stomach against ulceration caused by ethanol.