<abstract xmlns="http://www.w3.org/1999/xhtml">Morroniside is one of the most important iridoid glycosides from <italic>Cornus officinalis</italic> Sieb. et Zucc. In the present study, the pharmacokinetics and bioavailability studies of morroniside were conducted on Sprague-Dawley (SD) rats. A rat <italic>in situ</italic> 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 <italic>P</italic>eff 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 <italic>P</italic>app 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 <italic>P</italic>ratio 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).</abstract>

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).

The absorption of oral morroniside in rats: <italic>In vivo, in situ</italic> and <italic>in vitro</italic> studies

Key Laboratory for Biotech-Drugs Ministry of Health

Key Laboratory for Rare and Uncommon Diseases of Shandong Province

Key Laboratory of Drug Metabolism and Pharmacokinetics

Beijing Institute of Pharmacology and Toxicology

Acta Pharmaceutica

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

The absorption of oral morroniside in rats:  and  studies

Morroniside is one of the most important iridoid glycosides from Cornus officinalis Sieb. et Zucc. In the present study, the pharmacokinetics and...

The absorption of oral morroniside in rats: In vivo, in situ and in vitro studies

Published Online: Mar 28, 2019

Page range: 287 - 296

Accepted: Oct 14, 2018

DOI: https://doi.org/10.2478/acph-2019-0012

Keywords
morroniside, pharmacokinetics, absorption, rats, single-pass intestinal perfusion, Caco-2 cell

© 2019 Shan Xiong et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

The absorption of oral morroniside in rats: In vivo, in situ and in vitro studies

Published Online: Mar 28, 2019

Page range: 287 - 296

Accepted: Oct 14, 2018

DOI: https://doi.org/10.2478/acph-2019-0012

Keywordsmorroniside, pharmacokinetics, absorption, rats, single-pass intestinal perfusion, Caco-2 cell

© 2019 Shan Xiong et al., published by Sciendo

This work is licensed under the Creative Commons Attribution-NonCommercial-NoDerivatives 3.0 License.

Keywords
morroniside, pharmacokinetics, absorption, rats, single-pass intestinal perfusion, Caco-2 cell