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        Pharmacokinetics, tissue distribution and excretion of peimisine in rats assessed by liquid chromatography-tandem mass spectrometry

        Lihua Chen,Dongxun Li,Guosong Zhang,Wei Zhang,Lihua Zhang,Yongmei Guan,Weifeng Zhu,Hongning Liu 대한약학회 2015 Archives of Pharmacal Research Vol.38 No.6

        Peimisine, the common ingredient of ‘‘zhebeimu’’groups and ‘‘chuanbeimu’’ groups, is responsiblefor the expectorant and cough relieving effects. The aim ofthis study was to investigate the pharmacokinetics, tissuedistribution and excretion of peimisine in male and femaleSD (Sprague-Dawley) rats by a rapid and sensitive LC-MS/MS (liquid chromatography-tandem mass spectrometry)method used carbamazepine as the internal standard afteroral administration, carbamazepine was stated as an IS. The results showed that peimisine was slowly distributed,and eliminated from rat plasma and manifested lineardynamics in a dose range of 0.26–6.5 mg/kg. Tested byANOVA, there were gender differences in the pharmacokineticparameters of AUC0-t, AUC0-? among a singledose of 0.26, 1.3, 6.5 mg/kg (P\0.05). Drug blood andtissue levels in male rats were significantly higher than thefemale counterparts after oral administration, while boththe males and the females showed high drug levels inspleen, kidney, lung, liver and heart. On the other hand, thepeimisine levels that can be reached in uterus, ovary, testisand brain is low. The excretion study showed that littleadministered peimisine (\0.7 %) was recovered in themale and female bile. Approximately 13.46 and 15.05 %were recovered in female urine and feces, while 43.07 and7.49 % were recovered in male urine and feces, respectively,which indicated that the major elimination route ofmale rats was urine excretion. In addition, there was significantdifferences in total cumulative excretive ratio ofpeimisine in feces (P\0.05) and no significant differencesin the urine (P[0.05) at a dose of 1.3 mg/kg.

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