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Chinese Journal of Clinical Pharmacology and Therapeutics ›› 2017, Vol. 22 ›› Issue (9): 984-991.

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HPLC-MS/MS based pharmacokinetic study of alkaloids of sinomenium acutum

XIE Tong 1, CHENG Xuefang 2   

  1. 1 Jiangsu Key Laboratory of Pediatric Respiratory Disease, Institute of Pediatrics, Nanjing University of Chinese Medicine, Nanjing 210023, Jiangsu, China; 2 Department of Clinical Pharmacy, Shanghai General Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai 200080, China
  • Received:2017-03-17 Revised:2017-08-10 Online:2017-09-26 Published:2017-09-30

Abstract:

AIM: To establish a LC-MS/MS method for the study of pharmacokintic characteristics of alkaloids of sinomenium acutum in sprague dawley rat, and lay the foundation for the extensive research and clinical use of sinomenium acutum. METHODS: (1)LC-MS/MS method for the quantification of alkaloids of sinomenium acutum in biological sample was developed. (2)The in vivo time course of sinomenium acutum extracts (10 g crude drug/kg) in rats after a single oral administration was investigated. Pharmacokinetic parameters were calculated from the concentration data determined by LC-MS/MS. RESULTS:The standard curves showed good linearity over the concentration range of sinoacutine (13.8-3 530.0 ng/mL, R2=0.999 9) and magnoflorine (5.8-2 960.0 ng/mL, R2=0.999 8) in rat plasma. The inter-day and intra-day precision and accuracy values of sinoacutine and magnoflorine at three levels of QC samples were less than 15%. Pharmacokinetic study in rats showed that the main parameters for sinoacutine and magnoflorine were Cmax (14.88) and (0.99) μg/mL, Tmax (55.00) and (57.50) min, T1/2 (2.64) and (6.08) h, AUMC(0-t) (369 127.25) and (32 143.44) μg·h·h·mL-1, AUC(0-t) (2 482.76) and (177.77) μg·h·mL-1, MRT(0-t) (2.50) and (3.12) h, respectively. CONCLUSION: A sensitive, specific, and suitable LC-MS/MS method is validated for simultaneously quantifying the concentrations of sinoacutine and magnoflorine in rat plasma. Pharmacokinetic parameters show that the alkaloids of sinomenium acutum in rats conform to the non-compartmental model, and the plasma concentration reaches its peak rapidly, the elimination process is slow with high blood concentration.

Key words: alkaloids of sinomenium acutum, LC-MS/MS, pharmacokinetics

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