Reduced food interaction and enhanced gastrointestinal tolerability of a new system based on risedronate complexed with Eudragit E100: Mechanistic approaches from in vitro and in vivo studies

GUZMÁN ML; SORIA, ELIO; LAINO CARLOS HORACIO; MANZO RH; OLIVERA MARIA EUGENIA

EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS

ELSEVIER SCIENCE BV

Lugar: Amsterdam; Año: 2016 vol. 117 p. 263 - 263

0939-6411

ovel complexes consisting of Eudragit E100-risedronate are presented. The oral bioavailability of risedronatein rats was determined through its percentage excreted in urine after administration of complexedor free risedronate in fed and fasted conditions. The evaluation of the risedronate gastroduodenalirritation potential was carried out by macroscopic and histological analyses in an experimentalrat model. The degree of counterionic condensation between Eudragit E100 and risedronate was assessedby dialysis with, mechanistic information about the interaction with calcium and the release of risedronatefrom the complexes being obtained using physiological solution and simulated gastric fluid withoutpepsin. Non-significant differences were observed in the urinary excretion of risedronate when thecomplex or free risedronate was administered to fasted rats. However, the urinary excretion of risedronatein the complex group was 4-times higher than in the free risedronate group when animals w