利塞膦酸钠油包固S/O混悬剂大鼠体内药物动力学研究

Objective The aim of this work was to examine the usefulness of a solid-in-oil nanosuspension (SONS) to improve the oral absorption of risedronate sodium (risedronare) by means of in vivo evaluations in rats. Methods Although risedronate itself is water-solouble at neutral pH, it can be readily nanosuspended in an oil phase via complex formation with sucrose esters (i.e. surfactant). From the results obtained, the SONSMCT which exhibited risedronate release was dependent on the lipase degradation of medium-chain triglycerides (MCT), the oil phase, and produced the greatest increase in the oral absorption of residronate. From comparisons of the in vivo data with/without co-administration of Ca2+, a precipitation reagent used to inhibit drug uptake in an aqueous medium, it was found that the drug-surfactant complexes acted as a mucosal delivery carrier to protect risedronate from forming non-absorbable complexes with Ca2+. Results In addition, an increase in the oral absorption of risedronate by the SONSMCT was associated with a reduction in the drug dosage, in which risedronate uptake was strongly affected by endogenous negative factors (e.g. Ca2+) in the GI tract. Conclusions the SONSMCT has been shown to be a novel carrier-based delivery system for improving the oral absorption of risedronate.