Microencapsulation of sodium alendronate reduces drug mucosal damage in rats.
Sodium alendronate is an effective treatment for osteoporosis, but its oral administration is associated with adverse gastrointestinal effects. The aim of this work was to evaluate gastroresistant sodium alendronate-loaded microparticles prepared by spray-drying using Eudragit S100 or a blend of Eudragit S100/Methocel E4M. Both formulations presented high encapsulation efficiencies, mean diameters below 17 microm, and similar collapsed shape. Dissolution experiments showed good gastro-resistance for the microparticles at pH 1.2. At pH 6.8, the blended microparticles retarded the drug release. In vivo studies showed that the formulations were able to protect the rat stomachs against ulcer formation by sodium alendronate. In conclusion, the microparticles seems to be promising oral carriers for sodium alendronate.
Cruz
Letícia
L
Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Porto Alegre, Brazil.
Assumpção
Evelise
E
Andrade
Sérgio Faloni
SF
Conrado
Daniela Joyce
DJ
Guterres
Sílvia Stanisçuaski
SS
Pohlmann
Adriana Raffin
AR
D019386:Alendronate / Q000009:adverse effects* / Q000138:chemical synthesis / Q000493:pharmacokinetics; D000818:Animals; D004339:Drug Compounding; D005260:Female; D005753:Gastric Mucosa / Q000187:drug effects* / Q000378:metabolism / Q000473:pathology; D007413:Intestinal Mucosa / Q000187:drug effects* / Q000378:metabolism / Q000473:pathology; D051381:Rats; D017208:Rats, Wistar
D019386:Alendronate