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 t 1/2 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 t 1/2 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.
Highlights
Cepharanthine (CPA), a biscoclaurine alkaloid isolated from Stephania cepharantha Hayata (Menispermaceae), has been reported to possess a wide range of pharmacological activities (Azuma et al 2006; Chea et al 2007; Desgrouas et al 2014)
This study investigates the pharmacokinetic characteristics after oral or intravenous administration of CPA by using a sensitive and rapid LC–MS/MS method
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
Summary
Cepharanthine (CPA), a biscoclaurine alkaloid isolated from Stephania cepharantha Hayata (Menispermaceae), has been reported to possess a wide range of pharmacological activities (Azuma et al 2006; Chea et al 2007; Desgrouas et al 2014). CPA exhibits potent anticancer activity in vitro for different cancer cells (Biswas et al 2006; Harada et al 2009; Seubwai et al 2010; Ikeda et al 2011; Chen et al 2012). Due to the potent pharmacological activities of CPA, it is of great significance to investigate the pharmacokinetic properties of CPA. Hao et al (2010) have developed a sensitive and reliable LC–MS/MS method to determine the concentration of CPA in human plasma, and investigate the pharmacokinetics profiles of CPA after single intravenous administration of 50 mg CPA. To enhance the development potential of CPA, there is an urgent need to investigate the pharmacokinetic profiles of CPA, especially its bioavailability characteristics. This study investigates the pharmacokinetic characteristics after oral or intravenous administration of CPA by using a sensitive and rapid LC–MS/MS method
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