Chu Yang, Wang Xiangyang, Guo Jiahua, Li Wei, Ma Xiaohui, Zhu Yonghong
Department of Pharmacology, Tainjin Tasty Insitutte, People's Republic of China.
Eur J Drug Metab Pharmacokinet. 2012 Sep;37(3):173-7. doi: 10.1007/s13318-012-0084-y.
In the present study, an in vivo microdialysis sampling method coupled to HPLC was applied for the determination of unbound forsythiaside in rat blood and bile. Microdialysis probes were inserted into the jugular vein and bile duct of rats, and then blood and bile dialysates were collected at regular time intervals after intravenous administration of forsythiaside (50 mg/kg). Dialysate were directly injected into HPLC system. Forsythiaside was separated on a C₁₈ column eluted with the mobile phase of acetonitrile-water-formic acid (16:84:0.2, v/v/v) at a flow rate of 0.8 mL/min. The wavelength of the ultraviolet detector was set at 332 nm. The lowest limit quantification was 0.2 μg/mL for forsythiaside. Excellent linearity was found to be over a concentrate range of 0.2-100 μg/mL. The main pharmacokinetic parameters of unbound forsythiaside in rat blood and bile were obtained, Furthermore, the bile-to-blood distribution ratio (AUC(bile)/AUC(blood)) of forsythiaside was 0.32 ± 0.06. The results indicated that forsythiaside went through hepatobiliary excretion.
在本研究中，采用体内微透析采样法结合高效液相色谱法测定大鼠血液和胆汁中游离的连翘苷。将微透析探针插入大鼠颈静脉和胆管，然后在静脉注射连翘苷（50 mg/kg）后定期收集血液和胆汁透析液。透析液直接注入高效液相色谱系统。连翘苷在C₁₈柱上分离，以乙腈-水-甲酸（16:84:0.2，v/v/v）为流动相，流速为0.8 mL/min。紫外检测器波长设定为332 nm。连翘苷的最低定量限为0.2 μg/mL。在0.2 - 100 μg/mL的浓度范围内发现具有良好的线性关系。获得了大鼠血液和胆汁中游离连翘苷的主要药代动力学参数，此外，连翘苷的胆汁与血液分布比（AUC(胆汁)/AUC(血液)）为0.32 ± 0.06。结果表明连翘苷经肝胆排泄。
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