摘要
目的:研究陈皮水溶性生物碱iv给药后对大鼠的升血压作用,探讨其量-效关系,并测算主要药动学参数。方法:将陈皮水溶性生物碱按含生药童1 000 mg·kg-1的剂量给大鼠iv后,记录不同时刻的动脉收缩压(SAP)、舒张压(DAP)及心率(HR),计算平均动脉压(MAP)及其净增百分率(E%)。大鼠按1 000,500,250 mg·kg-1的剂量给药后,以MAP的总平均上升百分率为药效指标,测算量-效、时-效关系,计算药动学参数K等。结果:陈皮水溶性生物碱可显著升高大鼠的血压,SAP的最大平均上升百分率平均达53%,维持升压4 min;心率在给药后20s内明显减少(P<0.05),2 min后则显著增加(P<0.05~0.001),9 min后恢复正常;大鼠的MAP平均上升百分率与上述3剂量的对数剂量间呈良好的线性关来(r=0.998 5),给药后0.5~5 min动物体内残余药量呈一级消除,经计算求出其药动学参数K=0.55min-1, t1/2=1.24min。结论:陈皮水溶性生物碱对大鼠有明显的升血压作用,且在一定剂量范围内量-效、时-效呈线性相关,其作用时间短哲,清除快。
Abstract
OBJECTIVE:To study the rising BP(blood pressure)effects of total soluble alkaloid(TSA),which was extracted from a Chinese medical herb-Chenpi(Pericarpium Citri Reticulatae),and its ose-response relationship and pharmacokinetics. METHODS: Given iv the TSA with 1 000 mg herbs·kg-1 in rats, we recorded the SAP, DAP and HR, calculated the MAP and its increased percentage. After rats were given iv TSA with 1 000, 500, 250 mg·kg-1,the total percentage of MAP increased. The dose-response relationship and the pharmacokinetical data K, t1/2(ED),etc. were calculated. RESULTS: TSA elevated the BP of rats significantly, with a maximal SAP increasing precentage of over 53%. The BP restored 5 minutes later. The HR of rats decreased visibly in the first 20s(P<0.05),but 2 minutes later, it increased significantly(P<0.05~0.001)and restored after 10 minutes. The dose-response relationship was linear( r=0.998 5).After given iv TSA 0.5 to 5 minutes, the drug was eliminated at I stage. The pharmacokinetical data K was about 0.55 minute-1,t1/2(ED) abut 1.24 minutes. CONCLUSION: TSA can elevate the BP of rats immediately. Its dose-response and time-response is in linear relationship. Its actions are short, and elimination is so fast.
关键词
陈皮 /
血压 /
量-效关系 /
药动学
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Key words
Chenpi /
blood pressure /
dose-response relationship /
phmacokinetics
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沈明勤;叶其正;常复蓉;.
陈皮水溶性总生物碱的升血压作用量-效关系及药动学研究[J]. 中国药学杂志, 1997, 32(02): 97-100
Shen Mingqin.
The rising BP effect of Chenpi's TSA and its dose-response relationship and pharmacokinetics[J]. Chinese Pharmaceutical Journal, 1997, 32(02): 97-100
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参考文献
1 王筠默.橘皮和柑皮的药理研究.上海中医药杂志,1957,(9):44.
2 朱思明.陈皮对循环系统的药理作用.江苏医学院学报,1957,(3):148.3 李仪奎,王钦茂.中药药理实验方法学.上海:上海科学技术出版社,1991:31.
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脚注
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基金
本文为江苏省科研基金资助项目,第BJ93154号
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