LC-MS/MS determination and pharmacokinetic study of bergenin, the main bioactive component of Bergenia purpurascens after oral administration in rats  

作　　者：Bao-Hong Li Jin-Dong Wu Xiang-Lu Li 

机构地区：[1]School of Pharmacy,Guangdong Medical College [2]Nature’s & US Limited Liability Corporation

出　　处：《Journal of Pharmaceutical Analysis》2013年第4期229-234,共6页药物分析学报（英文版）

基　　金：supported by the Natural Science Foundation of Guangdong Province (Nos. 9151008018000003)

摘　　要：Bergenin, a C-glucoside of 4-O-methyl gallic acid from Bergenia purpurascens, is a naturally antitussive and expectorant agent. A rapid and sensitive liquid chromatography tandem mass spectrometry （LC-MS/MS） method has been developed and validated for the determination of the active component--bergenin, in rat plasma after oral administration of aqueous B. purpurascens extract. The plasma samples were pretreated by protein precipitation with acetonitrile and chromatographic separation was achieved on a Diamonsil C18 column （150mim×4.6mm, 5μm） with isocratic elution using a mobile phase consisting of water- methanol （30：70, v/v） at a flow rate of 0.6 mL/min. The detection was accomplished by a triple- quadrupole tandem mass spectrometer in multiple-reaction monitoring （MRM） scanning via an electrospray ionization （ESI） source operating in the negative mode. The optimized mass transition ion-pairs （m/z） for quantitation were 327.3/192.0 for bergenin, and 431.1/311.1 for IS. The time for each analysis run was only 3.5 min between injections. The calibration curve exhibited good linearity （r2〉 0.99） over a range of 1.00-2000 ng/mL for bergenin. The lower limit of quantitation （LLOQ） was 1.00ng/mL. The intra- and inter-day precisions were no more than 11.8%, and relative errors （RE） were within the range of 0.0-4.4%. The validated method was successfully applied to investigate the pharmacokinetics of bergenin after oral administration of B. purpurascens extract in rats.Bergenin, a C-glucoside of 4-O-methyl gallic acid from Bergenia purpurascens, is a naturally antitussive and expectorant agent. A rapid and sensitive liquid chromatography tandem mass spectrometry （LC-MS/MS） method has been developed and validated for the determination of the active component--bergenin, in rat plasma after oral administration of aqueous B. purpurascens extract. The plasma samples were pretreated by protein precipitation with acetonitrile and chromatographic separation was achieved on a Diamonsil C18 column （150mim×4.6mm, 5μm） with isocratic elution using a mobile phase consisting of water- methanol （30：70, v/v） at a flow rate of 0.6 mL/min. The detection was accomplished by a triple- quadrupole tandem mass spectrometer in multiple-reaction monitoring （MRM） scanning via an electrospray ionization （ESI） source operating in the negative mode. The optimized mass transition ion-pairs （m/z） for quantitation were 327.3/192.0 for bergenin, and 431.1/311.1 for IS. The time for each analysis run was only 3.5 min between injections. The calibration curve exhibited good linearity （r2〉 0.99） over a range of 1.00-2000 ng/mL for bergenin. The lower limit of quantitation （LLOQ） was 1.00ng/mL. The intra- and inter-day precisions were no more than 11.8%, and relative errors （RE） were within the range of 0.0-4.4%. The validated method was successfully applied to investigate the pharmacokinetics of bergenin after oral administration of B. purpurascens extract in rats.

关 键 词：BERGENIN Bergenia purpurascens PHARMACOKINETICS Rat plasma LC-MS/MS 

分 类 号：R285.5[医药卫生—中药学]