Chinese Journal of Pharmacovigilance ›› 2021, Vol. 18 ›› Issue (7): 632-636.
DOI: 10.19803/j.1672-8629.2021.07.08

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Evaluation of Pharmacokinetics of Aconiti Lateralis Radix of Shenfu Prescription in Rats with Heart Failure

XIE Guanghui1, MA Zengchun1, MEI Yu1, ZHANG Xuemei1,2, TAN Hongling1, GAO Yue1,*   

  1. 1Institute of Radiation Medicine, Academy of Military Medical Sciences, Beijing 100850, China;
    2Guangdong Pharmaceutical University, Guangzhou Guangdong 510573, China
  • Received:2021-04-21 Online:2021-07-15 Published:2021-07-23

Abstract: Objective To study the pharmacokinetics of Aconiti Lateralis Radix of Shenfu prescription in rats with heart failure and provide data for toxicity reduction and enhanced efficacy of Ginseng and Aconiti Lateralis Radix. Methods An animal model with heart failure was established and evaluated in 40 SD rats (half male and half female). After surgery, SD rats were divided into three groups: normal, model and M+ginseng groups. Blood samples were collected at 0, 0.25, 0.5, 1, 2, 4, 8, 12, 24 and 48 h after oral administration of Fuzi extracts. UPLC-MS/MS was used for determination of blood drug concentrations while DAS software was used to analyze pharmacokinetic parameters. Results Evaluation of the model group showed that the heart failure markers in serum of rats were significantly higher. The coefficient of cardiac weight was increased. Meanwhile, mass death of myocardial cells was observed and the space between myocardial fibers was wider pathologically, suggesting that the establishment of the model was successful. The results of pharmacokinetic parameters showed that the AUC (0~48 h) became much smaller and t1/2z of AC and HA was significantly shortened in the model group compared with the normal group. In addition, compared to the model group, the AUC (0~48 h) and t1/2z of the M+ginseng group were increased. Conclusion The absorption of aconitum alkaloids in rats with heart failure is poor but the metabolic rate is faster, leading to a short retention time. Ginseng could improve the metabolic process of aconitum alkaloids in vivo significantly, which means better absorption and a longer action time. This may be the reason that the efficacy is enhanced.

Key words: aconiti lateralis radix, UPLC-MS/MS, ginseng, heart failure, pharmacokinetics

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