The absorption of oral morroniside in rats: In vivo, in situ and in vitro studies
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 a...
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Sciendo
2019-06-01
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| Series: | Acta Pharmaceutica |
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| Online Access: | https://doi.org/10.2478/acph-2019-0012 |
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| author | Xiong Shan Li Jinglai Mu Yanling Zhang Zhenqing |
| author_facet | Xiong Shan Li Jinglai Mu Yanling Zhang Zhenqing |
| author_sort | Xiong Shan |
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| description | 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). |
| format | Article |
| id | doaj-art-f3fe922c51414a55823956cef2e0ab04 |
| institution | Kabale University |
| issn | 1846-9558 |
| language | English |
| publishDate | 2019-06-01 |
| publisher | Sciendo |
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| series | Acta Pharmaceutica |
| spelling | doaj-art-f3fe922c51414a55823956cef2e0ab042025-02-02T12:01:39ZengSciendoActa Pharmaceutica1846-95582019-06-0169228729610.2478/acph-2019-0012acph-2019-0012The absorption of oral morroniside in rats: In vivo, in situ and in vitro studiesXiong Shan0Li Jinglai1Mu Yanling2Zhang Zhenqing3Institute of Materia Medica, Shandong Academy of Medical Sciences, JinanChinaKey Laboratory of Drug Metabolism and Pharmacokinetics, Beijing Institute of Pharmacology and Toxicology, BeijingChinaInstitute of Materia Medica, Shandong Academy of Medical Sciences, JinanChinaKey Laboratory of Drug Metabolism and Pharmacokinetics, Beijing Institute of Pharmacology and Toxicology, BeijingChinaMorroniside 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).https://doi.org/10.2478/acph-2019-0012morronisidepharmacokineticsabsorptionratsin situ single-pass intestinal perfusioncaco-2 cell |
| spellingShingle | Xiong Shan Li Jinglai Mu Yanling Zhang Zhenqing The absorption of oral morroniside in rats: In vivo, in situ and in vitro studies Acta Pharmaceutica morroniside pharmacokinetics absorption rats in situ single-pass intestinal perfusion caco-2 cell |
| title | The absorption of oral morroniside in rats: In vivo, in situ and in vitro studies |
| title_full | The absorption of oral morroniside in rats: In vivo, in situ and in vitro studies |
| title_fullStr | The absorption of oral morroniside in rats: In vivo, in situ and in vitro studies |
| title_full_unstemmed | The absorption of oral morroniside in rats: In vivo, in situ and in vitro studies |
| title_short | The absorption of oral morroniside in rats: In vivo, in situ and in vitro studies |
| title_sort | absorption of oral morroniside in rats in vivo in situ and in vitro studies |
| topic | morroniside pharmacokinetics absorption rats in situ single-pass intestinal perfusion caco-2 cell |
| url | https://doi.org/10.2478/acph-2019-0012 |
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