Quantitative LC/MS/MS method and in vivo pharmacokinetic studies of vitexin rhamnoside, a bioactive constituent on cardiovascular system from hawthorn.
A simple and accurate liquid chromatography coupled with tandem mass spectrometry method was developed for determination and in vivo pharmacokinetic studies of vitexin rhamnoside in rat plasma. After protein precipitation using methanol, the analytes were separated by a Luna C(18) column with an isocratic elution and analyzed by mass spectrometry in multiple reaction monitoring mode using the respective negative ion at m/z 577.2-293.0 for vitexin rhamnoside and m/z 593.2-413.0 for internal standard (IS) vitexin glucoside. The method was validated systematically within the concentration range 5-5000 microg/L (R > 0.996) and the lower limit of quantitation was 5 microg/L. Acceptable precision and accuracy were acquired for concentrations over the standard curve range. It was further applied to assess pharmacokinetics and bioavailability of vitexin rhamnoside after intravenous and oral administration to rats. The oral bioavailability of vitexin rhamnoside was only 3.57%, which indicated that vitexin rhamnoside had poor absorption or underwent extensive first-pass metabolism. Practical utility of this new LC/MS/MS method was confirmed in pilot pharmacokinetic studies in rats following both intravenous and oral administration.
Liang
Mingjin
M
Department of Natural Medicinal Chemistry, Second Military Medical University, Shanghai 200433, People's Republic of China.
Xu
Wen
W
Zhang
Weidong
W
Zhang
Chuan
C
Liu
Runhui
R
Shen
Yunheng
Y
Li
Huiliang
H
Wang
Xiaolin
X
Wang
Xiangwei
X
Pan
Qiongqun
Q
Chen
Chunlin
C
D000818:Animals; D047310:Apigenin / Q000493:pharmacokinetics* / Q000494:pharmacology; D001682:Biological Availability; D002319:Cardiovascular System / Q000187:drug effects*; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D027825:Crataegus / Q000737:chemistry*; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D015203:Reproducibility of Results; D053719:Tandem Mass Spectrometry / Q000379:methods*
D047310:Apigenin; C032731:vitexin