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目的 用麻醉猫研究异钩藤碱 (Iso)的心血管药理效应与血药浓度的关系。方法 异钩藤碱粉末 ,分别临用时配制 (FPI)和配好后室温放置 1周备用 (DPI)。以RM 6 0 0 0八道生理仪记录猫的收缩压、舒张压和心率的变化 ,相应时间点取血 1.0mL。用反相高效液相色谱法测定血药浓度。结果 Iso的降压及负性频率效应与其给药剂量及血药浓度呈明显的量 效关系 ,同剂量的DPI和FPI给药 ,FPI的起效时间、疗效维持时间及最大效应均强于DPI。结论 Iso的降压及负性频率效应与其给药剂量及血药浓度呈明显的量 效关系 ;Iso的溶液剂型不稳定 ,室温放置 1周后可降低其心血管药理效应。
Objective To study the relationship between cardiovascular pharmacological effects and plasma concentration of isorhline (Iso) in anesthetized cats. Method: Uncaria nicotine powder was prepared for FPI and DPI after 1 week at room temperature. The RM 60 000 physiological records of cats systolic blood pressure, diastolic blood pressure and heart rate changes, the corresponding time point to take blood 1.0mL. Determination of plasma concentration by reversed-phase high-performance liquid chromatography. Results The antihypertensive and negative frequency effects of Iso showed a dose-effect relationship with the dose and plasma concentration. The DPI and FPI administration at the same dosage showed that the onset time, the effect maintaining time and the maximum effect of FPI were all higher than those of DPI . Conclusions The antihypertensive effect and negative frequency effect of Iso showed a dose-effect relationship with the dose and plasma concentration of Iso. The solution dosage of Iso was unstable and could reduce the cardiovascular pharmacological effects after being left at room temperature for 1 week.