Deng Yingbin, Wu Weijun, Ye Sunzhi, Wang Wei, Wang Zhiyi
a Department of Emergency Medicine , The Second Affiliated Hospital and Yuying Children's Hospital of Wenzhou Medical University , Wenzhou , China.
Pharm Biol. 2017 Dec;55(1):1775-1779. doi: 10.1080/13880209.2017.1328446.
Cepharanthine (CPA) has been reported to possess a wide range of pharmacological activities.
This study investigates the pharmacokinetic characteristics after oral or intravenous administration of CPA by using a sensitive and rapid LC-MS/MS method.
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.
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 was 6.76 ± 1.21 h. After oral administration of 10 mg/kg of CPA, CPA was not readily absorbed and reached C 46.89 ± 5.25 ng/mL at approximately 2.67 h. The t was 11.02 ± 1.32 h. The absolute bioavailability of CPA by oral route was 5.65 ± 0.35%, and the bioavailability was poor.
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.
据报道，千金藤素（CPA）具有广泛的药理活性。
本研究采用灵敏快速的液相色谱-串联质谱（LC-MS/MS）法，研究口服或静脉注射CPA后的药代动力学特征。
建立了一种灵敏快速的LC-MS/MS法，用于测定Sprague-Dawley大鼠血浆中的CPA。将12只大鼠随机均分为两组，包括静脉注射组（1mg/kg）和口服组（10mg/kg）。在指定时间点采集血样（250μL），并用该方法进行测定。计算药代动力学参数。
校准曲线在0.1-200ng/mL范围内呈线性（r = 0.999），定量下限为0.1ng/mL。静脉注射1mg/kg后，CPA浓度最高达到153.17±16.18ng/mL，t为6.76±1.21h。口服10mg/kg CPA后，CPA不易吸收，在约2.67h时达到C 46.89±5.25ng/mL。t为11.02±1.32h。CPA口服途径的绝对生物利用度为5.65±0.35%，生物利用度较差。
结果表明，CPA在大鼠体内的生物利用度较差，应进一步研究其生物利用度差的原因并解决该问题。
