Comparative pharmacokinetics of bergenin, a main active constituent of Saxifraga stolonifera Curt., in normal and hepatic injury rats after oral administration

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• 作者：Rong-Hua PAN^a ; Hong-Mei HE^b ; ^# ; Yue DAI^c ; Yu-Feng XIA^b ; ^{yfxiacpu@126.com" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Bergenin ; Saxifrage stolonifera Curt ; HPLC ; Pharmacokinetic ; Hepatic injury
• 刊名：Chinese Journal of Natural Medicines
• 出版年：2016
• 出版时间：October 2016
• 年：2016
• 卷：14
• 期：10
• 页码：776-782
• 全文大小：956 K

文摘

Bergenin, isolated from the herb of Saxifrage stolonifera Curt. (Hu-Er-Cao) has hepatoprotective, anti-inflammatory, antitussive, and neuroprotective activities. The aim of the present study was to establish a simple, rapid, and sensitive RP-HPLC method for determination of bergenin in rat plasma and compare its oral pharmacokinetic behaviors in normal and CCl₄-induced hepatic injury rats. With norisoboldine as an internal standard, chromatographic separation was performed on a C₁₈ analytical column with acetonitrile and water (11 : 89, V/V) containing 0.1% formic acid as the mobile phase. A good linearity was obtained over the range of 100–10 000 ng·mL⁻¹. The lower limit of quantification was 50 ng·mL⁻¹. The developed method was successfully applied to a study of the pharmacokinetic difference of bergenin (100 mg·kg⁻¹) between normal and hepatic injury rats after oral administration. Marked alterations of pharmacokinetic parameters in hepatic injury rats were observed. Compared to normal rats, the AUC_(0−∞) of bergenin in hepatic injury rats was elevated to 2.11-fold and C_max was increased by 130%, whereas CL value was only 55% of the normal rats, suggesting that the systemic exposure of bergenin was significantly increased under hepatic injury status.