The Open Drug Delivery Journal

2007, 1 : 28-35
Published online 2007 September 28. DOI: 10.2174/1874126600701010028
Publisher ID: TODDJ-1-28

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

R.P. Raffin , L.M. Colomé , E.E.S. Schapoval , D.S. Jornada , A.R. Pohlmann and S.S. Guterres
Departamento de Química Orgânica, Instituto de Química, Universidade Federal do Rio Grande do Sul. Av. Bento Gonçalves 9500, CP 15003, Porto Alegre, RS, Brazil, CEP 91501-970.

ABSTRACT

The aim of the present work was to verify the in vivo capacity of pantoprazole-loaded microparticles to protect the gastric mucosa against ulcer formation and to evaluate their stability under accelerated conditions. Pantoprazoleloaded microparticles were prepared by spray-drying in pilot scale, using Eudragit® S100 as polymer. Transparent glass vials containing drug-loaded microparticles were stored for 6 months at 40°C and 75% RH. Photostability was tested under UVA 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 stability study, samples showed complete encapsulation efficiency and were considered stable. The microencapsulation of pantoprazole reduced its photodegradation. The in vivo evaluation showed that the microparticles presented ulcer index lower than the solutions. Enteric microparticles had acceptable stability under accelerated conditions and were efficient in protecting the stomach against ulceration caused by ethanol.

Keywords:

Pantoprazole, microparticles, stability, photodegradation, gastro-resistance, anti-ulcer activity.