Morroniside is one of the most important iridoid glycosides from Cornus officinalis Sieb. et Zucc. In the present study, the pharmacokinetics and bioavailability studies of morroniside were conducted on Sprague-Dawley (SD) rats. A rat in situ intestinal perfusion model was used to characterize the absorption of morroniside. Caco-2 cells were used to examine the transport mechanisms of morroniside. The pharmacokinetic study of morroniside exhibited linear dose-proportional pharmacokinetic characteristics and low bioavailability (4.3 %) in SD rats. Its average Peff value for transport across the small intestinal segments changed from (3.09 ± 2.03) × 10-6 to (4.53 ± 0.94) × 10-6 cm s-1. In Caco-2 cells, the Papp values ranged from (1.61 ± 0.53) × 10-9 to (1.19 ± 0.22) × 10-7 cm s-1 for the apical to basolateral side and the Pratio values at three concentrations were all lower than 1.2. Morroniside showed poor absorption and it might not be a specific substrate of P-glycoprotein (P-gp).
Keywords: Caco-2 cell; absorption; in situ single-pass intestinal perfusion; morroniside; pharmacokinetics; rats.