Pharmacokinetics, tissue distribution, bioavailability, and excretion of nuciferine, an alkaloid from lotus, in rats by LC/MS/MS

Abstract

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 (0.2 mg/kg) and orally given a single dose of nuciferine (10.0 mg/kg). Blood samples were withdrawn via the ocular vein at specific times.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 (IV) to rats. The AUC_0→4 h values in tissues were in the order of kidney > lung > spleen > liver > brain > heart. The majority of excretion of nuciferine (50.7%) 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.

Keywords:

• Nuciferine
• pharmacokinetic
• bioavailability
• tissue distribution
• excretion

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work were supported by Shandong Province Higher Educational Science and Technology Program [Grant: J17KA250]; the Natural Science Foundation of Shandong Province [Grant: ZR2013HL062]; the Foundation of Overseas Distinguished Taishan Scholars of Shandong Province.