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量１０００ｍｇ·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１０００，５００，２５０ｍｇ·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４ｍｉｎ；心率在给药后２０ｓ内明显减少（Ｐ＜０．０５），２ｍｉｎ后则显著增加（Ｐ＜０．０５～０．００１），９ｍｉｎ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系（ｒ＝０．９９８５），给药后０．５～５ｍｉｎ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，其作用时间短暂，清除快。
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 dose 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,t 1/2(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 20 s(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 ,t 1/2(ED) about 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.
出处
《中国药学杂志》
CAS
CSCD
北大核心
1997年第2期97-100,共4页
Chinese Pharmaceutical Journal
基金
江苏省科研基金
