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作者

Wang F. Cao J. Hou X. Li Z. Qu X.

作者单位

School of Pharmacy, Taishan Medical University, Taian, China Department of Pharmacology, China Minority Traditional Medical Center of Min Zu University of China, Beijing, China

刊名

Drug Development and Industrial Pharmacy

年份

2018

卷号

Vol.44 No.9

页码

1557-1562

ISSN

0363-9045;1520-5762

关键词

bioavailability excretion Nuciferine pharmacokinetic tissue distribution

摘要

Objective: In order to characterize the pharmacokinetics, tissue distribution, bioavailability, and excretion of nuciferine, a reliable gradient LC/MS/MS-based method was developed and validated. Methods: Sprague-Dawley rats were intravenously injected with a bolus of nuciferine and orally given a single dose of nuciferine . Blood samples were withdrawn via the ocular vein at specific times. Organs, including the liver, kidney, brain, lung, heart, and spleen, were collected at specific times af...更多

Objective: In order to characterize the pharmacokinetics, tissue distribution, bioavailability, and excretion of nuciferine, a reliable gradient LC/MS/MS-based method was developed and validated. Methods: Sprague-Dawley rats were intravenously injected with a bolus of nuciferine and orally given a single dose of nuciferine . Blood samples were withdrawn via the ocular vein at specific times. Organs, including the liver, kidney, brain, lung, heart, and spleen, were collected at specific times after oral administration of 10.0 mg/kg nuciferine. The plasma and tissue samples were assayed by LC/MS/MS. Results: The results indicated that nuciferine had rapid distribution and poor absorption into systemic circulation. The value of absolute bioavailability was only 1.9 ± 0.8% after administration of 10.0 mg/kg nuciferine by oral and administration of 0.2 mg/kg nuciferine intravenously to rats. The AUC0→4 h values in tissues were in the order of kidney > lung > spleen > liver > brain > heart. The majority of excretion of nuciferine was excreted through kidneys with parent drug after oral administration without liver metabolism. Conclusion: This study may provide a meaningful basis for clinical application of such a bioactive compound of herbal medicines.收起

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