用气相—电子捕获法研究硝酸甘油在人体内的药动学及药效学

应用气相－电子捕获法（ＧＣ－ＥＣＤ）对１６名健康志愿受试者（青年组８名，老年组８名）单剂量舌下含服硝酸甘油片剂０．５ｍｇ后的药物动力学及药效学进行了研究。于用药前和用药后２，４，６，７，８，１０，１５，２０ｍｉｎ取血测定，以ＭＣＰＫＰ药物动力学程序拟合药－时数据，结果表明，本药的处置符合一房室开放模型。本药经舌下含服后吸收迅速，在吸收和消除方面与外国人无显著差异。青年组与老年组比较，在Ｔ１／２Ｋａ、Ｔ１／２Ｋ，Ｔｍａｘ、Ｃｍａｘ方面具有显著性差异（Ｐ＜０．０５）。在药效学方面，应用ＧＰ－３０３血流动力学测定仪，我们选择了每搏量（ＳＶ）、平均动脉压（ＭＡＰ）、心率（ＨＲ）和体循环阻力（ＴＰＲ）作为药效学指标。研究表明，随着血药浓度增高，ＭＡＰ、ＴＰＲ下降，ＨＲ、ＳＶ增高，血药浓度与各药效学指标相关性依次为ＭＡＰ＞ＨＲ＞ＳＶ＞ＴＰＲ。受试者两组间药效学指标波动范围ｔ检验ＭＡＰ、ＨＲ之间无显著性差异（Ｐ＞０．０５），ＳＶ、ＴＰＲ具有显著性差异（Ｐ＜０．０５）。

Study on pharmacokinetics and pharmacokdynamics of nitroglycerin in healthy volunteers

Sixteen healthy volunteers (young group:8; old group:8) were given with nitroglycerin( 0.5mg ) sublingualy, the pharmacokinetics and pharmacodynamics were studied by chromatographic electron capture detection. The blood samples were determined 2,4,6,7,8,10,15,20 minutes before and after treatment respectively. MCPKP pharmacokinetics program was applied to imitate concentration time data. Nitroglycerin showed one compartment open model and it was absorbed quickly, there was no significant diefference T 1/2 K a, T 1/2 K , T max and C max between young group and old group. According to pharmacodynamics, the GP 303 instrument was used to detect the pharmacodynamics indexes such as SV,MAP,HR,and TPR. The results showed that following nitroglycerin concentration increasing, HR and SV were increased, MAP and TPR were decreased. The relationship between the blood concentration and pharmacodynamics was MAP>HR>SV>TPR. Between two groups through t test there was no significant difference in the wave range of pharmacodynamics indexes of MAP and HR, but existed significant difference in SV an TPR.