Pharmacokinetics and metabolism of C hf197, a ligustrazine derivative, in rats

作者：Wenlong Li, Huiqing Liu, Chunmin Wei, Xinbing Wei, Mingtan Tang, Xianglin Kong, Hongfei Chen, Xinyong Liu, Ruichen Guo · 发表于：Fundamental and Clinical Pharmacology · 年份：2015 · DOI：10.1111/fcp.12133 · 被引用次数：5 · 研究领域：Traditional Chinese Medicine Analysis、Plant-based Medicinal Research、Berberine and alkaloids research

Ligustrazine is the most abundant and bioactive ingredient in Rhizoma Chuanxiong, a Chinese medicinal herb commonly used for the treatment of cardiovascular diseases. Chf197 is one of the structurally modified ligustrazine derivatives in a purpose of overcoming the rapid metabolism and short half-life of original. The plasma and urine pharmacokinetics of Chf197 in rats were studied after intravenous or intraperitoneal injection of Chf197 with the validated RP-HPLC method. The pharmacokinetic parameters of Chf197 injected intravenously 20 mg/kg were as follows: Cmax , 1.44 ± 0.4 mg/L; Tmax , 0.08 h; t1/2 , 3.03 ± 1.67 h; AUC, 3.85 ± 3.88 h/L; Vd , 31.66 ± 11.79L/kg; and CL, 9.29 ± 4.92 l/h/kg. Dose-dependent pharmacokinetics was observed, and a significantly higher dose-normalized AUC after intravenous administration was obtained than that after intraperitoneal administration. A possible metabolite was detected at about 3.1 min, and full-scan mass spectrum was adopted to predict its possible structure.