Purpose. To study the pharmacokinetics of the 6 alkaloids (aconitine, mesaconitine, hypaconitine, benzoylaconine, benzoylmesaconine, and benzoylhypaconine) in raw Aconiti Kusnezoffii Radix (Caowu) (RC) and Chebulae Fructus- (Hezi-) processed Caowu (HC) in the rats being, respectively, administrated with RC and HC in the dosage forms of powder and decoction and to demonstrate the mechanism of detoxification of HC. Methods. The rats were randomly divided into 4 groups and, respectively, given RC powder, HC powder, RC decoction, and HC decoction by intragastric administration. The contents of the 6 alkaloids in the plasma of the rats were detected at different time points by the UPLC-MS/MS method, and DAS 3.2.7 software was used to calculate, compare, and analyze the detected pharmacokinetic parameters. Results. Compared with those of the RC powder, the values of and of the HC powder were all reduced, whereas the values of and were mostly increased. Compared with those of the RC powder, the values of , , and of the RC decoction were decreased and the value of of the RC decoction was increased. Compared with those of the RC decoction, the values of , , and of the diester diterpenoid alkaloids of the HC decoction were all increased. However, there was no marked difference between the pharmacokinetic parameters of the HC powder and the HC decoction. Conclusions. A decrease in the level of absorption and in the rate of elimination of the alkaloids can be detected when HC is administrated in the dosage form of the powder, explaining that in traditional Mongolian medicine (TMM), the purpose of using HC in the dosage forms of pills and powder is for decreasing the toxicity and prolonging the efficacy duration of HC. Decocting can greatly decrease the plasma concentration of the diester diterpenoid alkaloids in RC and increase their rate of elimination. The influence of decocting on RC is greater than that on HC, explaining the rationality of the steaming and boiling methods for processing Caowu and the rationality of boiling Caowu for a longer time beforehand in preparing an herb decoction containing Caowu in TCM.

中文翻译：

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UPLC-MS/MS研究不同剂型对生乌头（草乌）和荸荠-（和子-）草乌中6种生物碱药代动力学的影响

目的。研究乌头碱、中乌头碱、次乌头碱、苯甲酰乌头碱、苯甲酰美乌头碱和苯甲酰次乌头碱6种生物碱在生乌头(草乌)(RC)和荸荠(合子)加工草乌(HC)中的药代动力学。分别以散剂和煎剂的形式与 RC 和 HC 一起给药，以证明 HC 的解毒机制。方法. 将大鼠随机分为4组，分别灌胃RC粉、HC粉、RC汤、HC汤。采用UPLC-MS/MS法在不同时间点检测大鼠血浆中6种生物碱的含量，采用DAS 3.2.7软件对检测到的药代动力学参数进行计算、比较和分析。结果。与RC粉体相比，HC粉体的和值均降低，而和值大多增加。与RC散相比，RC煎剂的、、和的值降低，而 RC汤剂的增加。与RC汤相比，HC汤的二酯二萜生物碱的、、、、值均有所增加。然而，HC粉和HC汤剂的药代动力学参数没有显着差异。结论 . 当以粉末剂型施用HC时，可以检测到生物碱的吸收水平和消除率的降低，这解释了在传统蒙药（TMM）中，在剂型中使用HC的目的丸剂和散剂是为了降低HC的毒性和延长药效时间。煎剂可大大降低RC中二酯二萜生物碱的血药浓度，提高其清除率。煎剂对RC的影响大于对HC的影响，说明蒸煮处理草五的合理性和提前较长时间熬制草五中药汤剂的合理性。