天麻钩藤配伍对天麻素和钩藤碱体内药动学的影响

测定天麻素及钩藤碱体内药动学参数,研究天麻钩藤药对配伍后对天麻素和钩藤碱体内药动学行为的影响。结果天麻钩藤以9∶12配伍后,与二者单味药对照组相比,天麻素和钩藤碱C_(max)及AUC均显著增加,钩藤t_(max)后移1.5 h,天麻t_(max)后移0.25 h,二者由原来相同的达峰时间改变为前后相差1.25 h,说明配伍可显著改变药物体内药动学行为。从整体组方分析,天麻药性缓和滋补,钩藤寒凉苦降,配伍后天麻达峰较快且C_(max)及AUC增加,先发挥滋阴潜阳作用同时弥补钩藤达峰延后损失的药效;之后,在滋阴的前提下钩藤碱继续达峰且C_(max)及AUC增加,可弥补天麻半衰期较短的缺点,有利于更好地维持降压作用。二者配伍各自发挥优势互补,避免了单用钩藤苦寒过重累及伤阴,或单用天麻滋补有余,苦寒不足,充分说明钩藤、天麻二者共为君药、标本兼顾的治疗原则具有可靠的药动学依据。该研究通过对天麻钩藤药对配伍后的药动学特征进行研究,发现中医通过天麻、钩藤配伍实现对"肝阳上亢"整体施治目的是具有其药动学基础的,进一步为中医组方用药的科学性、合理性提供药动学依据。

Effect of combination of gastrodia and uncaria on pharmacokinetics of gastrodin and rhynchophylline

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, C_max and AUC of both gastrodin and rhynchophylline were significantly increased, and t_max was retroceded by 1.5 h for rhynchophylline and 0.25 h for gastrodin. The change of t_max 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 C_max 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 C_max 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.