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. 2017 Dec;55(1):1775-1779.
doi: 10.1080/13880209.2017.1328446.

Determination of cepharanthine in rat plasma by LC-MS/MS and its application to a pharmacokinetic study

Yingbin Deng  1 , Weijun Wu  1 , Sunzhi Ye  1 , Wei Wang  1 , Zhiyi Wang  1
Affiliations

Determination of cepharanthine in rat plasma by LC-MS/MS and its application to a pharmacokinetic study

Yingbin Deng et al. Pharm Biol. 2017 Dec.

Abstract

Context: Cepharanthine (CPA) has been reported to possess a wide range of pharmacological activities.

Objective: This study investigates the pharmacokinetic characteristics after oral or intravenous administration of CPA by using a sensitive and rapid LC-MS/MS method.

Materials and methods: A sensitive and rapid LC-MS/MS method was developed for the determination of CPA in Sprague-Dawley rat plasma. Twelve rats were equally randomized into two groups, including the intravenous group (1 mg/kg) and the oral group (10 mg/kg). Blood samples (250 μL) were collected at designated time points and determined using this method. The pharmacokinetic parameters were calculated.

Results: The calibration curve was linear within the range of 0.1-200 ng/mL (r = 0.999) with the lower limit of quantification at 0.1 ng/mL. After 1 mg/kg intravenous injection, the concentration of CPA reached a maximum of 153.17 ± 16.18 ng/mL and the t1/2 was 6.76 ± 1.21 h. After oral administration of 10 mg/kg of CPA, CPA was not readily absorbed and reached Cmax 46.89 ± 5.25 ng/mL at approximately 2.67 h. The t1/2 was 11.02 ± 1.32 h. The absolute bioavailability of CPA by oral route was 5.65 ± 0.35%, and the bioavailability was poor.

Discussion and conclusions: The results indicate that the bioavailability of CPA was poor in rats, and further research should be conducted to investigate the reason for its poor bioavailability and address this problem.

Keywords: Absorption; P-gp; bioavailability.

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Figures

Figure 1.
Figure 1.
Chromatograms of blank plasma (A); plasma spiked with CPA and rutin (B); rat plasma sample obtained 10 h after oral administration of CPA (C). 1: rutin; 2: CPA.
Figure 2.
Figure 2.
The pharmacokinetic profiles of CPA in rats after intravenous administration of CPA (A) at dosage of 1 mg/kg and oral administration of CPA (B) at 10 mg/kg.
See this image and copyright information in PMC

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