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天麻钩藤组合对天麻素和钩藤碱药代动力学的影响

[Effect of combination of gastrodia and uncaria on pharmacokinetics of gastrodin and rhynchophylline].

作者信息

Wu Li-Hong, Hou Jia, Wang Jue, Luo Man, Wang Li-Min, Wang Jian-Xin, Li Yong-Ji, Qin Jing

机构信息

Heilongjiang University of Chinese Medicine, Harbin 150040, China.

Weihai Municipal Hospital, Weihai 264200, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2017 Jul;42(13):2577-2582. doi: 10.19540/j.cnki.cjcmm.20170523.011.

Abstract

To investigate the effect of the combination of gastrodia and uncaria on the pharmacokinetics of gastrodin and rhynchophylline, and determine their pharmacokinetic parameters after administration of the combination of gastrodia and uncaria at the ratio of 12∶9. Compared with uncaria group or gastrodia group, Cmax and AUC of both gastrodin and rhynchophylline were significantly increased, and tmax was retroceded by 1.5 h for rhynchophylline and 0.25 h for gastrodin. The change of tmax resulted in a 1.25 h difference in the peak time between gastrodin and rhynchophylline , which was the same between them. Uncaria shows a more effect in suppressing hyperactive Yang, while gastrodia has a balancing effect by nourishing Yin and suppressing hyperactive Yang. As a result, gastrodia could exert the effect in nourishing Yin and suppressing effect of uncaria, which could avoid the deficiency of Yang affecting Yin due to mono-treatment of uncaria. On one hand, the enhanced AUC and Cmax of gastrodin could increase the average plasma drug concentration of gastrodin, and remedy the losing effect of uncaria at the early stage; On the other hand, the increased AUC and Cmax of rhynchophylline could make up the quick elimination of gastrodia in vivo at the late stage. Their combination could lead to an increased anti-hypertensive effect with the balance of Yin and Yang. They showed unique advantages compared with simple dosage increase of western medicines. The results were consistent with the principle of TCM treatment for the hypertension due to hyperactivity of the liver Yang. In short, this study gives a good pharmacokinetic explanation of the balance of Yin and Yang and TCM treatment for both symptoms and root cause.

摘要

研究天麻与钩藤配伍对天麻素和钩藤碱药代动力学的影响,并测定天麻与钩藤按12∶9比例配伍给药后的药代动力学参数。与钩藤组或天麻组相比,天麻素和钩藤碱的Cmax和AUC均显著升高,钩藤碱的tmax提前1.5小时,天麻素的tmax提前0.25小时。tmax的变化导致天麻素和钩藤碱的达峰时间相差1.25小时,两者相同。钩藤平肝阳作用较强,天麻滋阴平肝,两者配伍,天麻可制约钩藤单用致阳损及阴之弊。一方面,天麻素AUC和Cmax增大,可提高天麻素的平均血药浓度,弥补钩藤早期作用丢失;另一方面,钩藤碱AUC和Cmax增大,可弥补天麻后期体内快速消除之不足。二者配伍可增强降压作用,使阴阳平衡,与单纯增加西药剂量相比具有独特优势。结果符合中医平肝潜阳法治疗高血压病的原则。总之,本研究为阴阳平衡及中医标本兼治提供了较好的药代动力学解释。

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