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本文报道硝苯啶普通和缓释两种剂型在原发性高血压患者的药代动力学和药效学变化。12例患者随机分为2组,分别单次口服硝苯啶普通片或缓释片20mg。硝苯啶血浓度由高效液相色谱-紫外检测器检测,并观察卧位血压心率变化。结果:普通片达峰时间(tmax)1.59±0.16h较缓释片4.07±0.62h早,p<0.01;普通片峰浓度(Cmax) 57.9±4.78ng/ml较缓释片30.19±6.83ng/ml高,p<0.001普通片消除半衰期(t1/2ke)1.82±0.44h较缓释片3.70±1.15h短,p<0.001。两种剂型最大降压幅度无显著性差异,P>0.05,但后者降压作用的维持时间延长。两种剂型血药浓度与收缩压(SBP)、舒张压(DBP)和心率(HR)变化呈正相关。缓释片的副反应(如心率增快)小于普通片。总之,缓释片具有降压作用长,血药浓度平稳,副反应小,且能减少服药次数的优点。
This article reports the nifedipine normal and sustained release of two formulations in patients with essential hypertension pharmacokinetics and pharmacodynamic changes. Twelve patients were randomly divided into two groups, each receiving a single oral nifedipine or sustained release tablets 20mg. The concentration of nifedipine was detected by high performance liquid chromatography-ultraviolet detector, and the changes of heart rate and heart rate in the supine position were observed. Results: The peak time of common tablets (1.59 ± 0.16h) was earlier than that of 4.07 ± 0.62h (P <0.01), and the peak value of common tablets (57.9 ± 4.78ng / ml) was 30.19 ± 6.83ng / ml high, p <0.001 ordinary tablets elimination half-life (t1 / 2ke) 1.82 ± 0.44h slower release tablets 3.70 ± 1.15h shorter, p <0.001. The maximum depressurization amplitude of the two formulations no significant difference, P> 0.05, but the maintenance of antihypertensive effect of the latter extended. The plasma concentrations of the two dosage forms were positively correlated with changes of SBP, DBP and HR. Side effects of sustained-release tablets (such as faster heart rate) is less than ordinary tablets. In short, sustained-release tablets with antihypertensive effect of long, steady blood concentration, side effects, and can reduce the number of medication advantages.