title: Pharmacokinetics and metabolism of Chf197, a ligustrazine derivative, in rats.
abstract: 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.
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Jinan, China.|Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, China.
authors.forename: Wenlong
authors.initials: W
authors.lastname: Li
authors.affiliation: Department of Pharmacology, School of Medicine, Jinan, China.|Key Laboratory of Molecular Pharmacology and Drug Evaluation (Ministry of Education of China), School of Pharmacy, Yantai University, Yantai, China.
authors.forename: Huiqing
authors.initials: H
authors.lastname: Liu
authors.affiliation: Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, China.
authors.forename: Chunmin
authors.initials: C
authors.lastname: Wei
authors.affiliation: Department of Pharmacology, School of Medicine, Jinan, China.
authors.forename: Xinbing
authors.initials: X
authors.lastname: Wei
authors.affiliation: Department of Pharmacology, School of Medicine, Jinan, China.
authors.forename: Mingtan
authors.initials: M
authors.lastname: Tang
authors.affiliation: Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, China.
authors.forename: Xianglin
authors.initials: X
authors.lastname: Kong
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Jinan, China.
authors.forename: Hongfei
authors.initials: H
authors.lastname: Chen
authors.affiliation: School of Pharmaceutical Sciences, Shandong University, Jinan, China.
authors.forename: Xinyong
authors.initials: X
authors.lastname: Liu
authors.affiliation: Institute of Clinical Pharmacology, Qilu Hospital of Shandong University, Jinan, China.
authors.forename: Ruichen
authors.initials: R
authors.lastname: Guo
mesh_terms: D000818:Animals; D019540:Area Under Curve; D001711:Biotransformation; D056148:Chromatography, Reverse-Phase; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage / Q000493:pharmacokinetics*; D006207:Half-Life; D007274:Injections, Intraperitoneal; D007275:Injections, Intravenous; D008297:Male; D008657:Metabolic Clearance Rate; D008689:Methacrylates; D011719:Pyrazines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D017207:Rats, Sprague-Dawley; D015203:Reproducibility of Results; D021241:Spectrometry, Mass, Electrospray Ionization
chemical_list: C000608713:Chf197; D004365:Drugs, Chinese Herbal; D008689:Methacrylates; D011719:Pyrazines; C032802:hydroxypropyl methacrylate; C017953:tetramethylpyrazine
keywords: Chf197; cardiovascular diseases; ligustrazine; metabolism; pharmacokinetic