目的优选酸枣仁中3种具有镇静催眠作用的主要有效组分(总皂苷、总黄酮、总生物碱)最佳配伍。方法采用均匀设计法将70只小鼠随机分为7组,分别为对照组及给药A～F组,观察各组小鼠自主活动情况;采用阈上剂量戊巴比妥钠(45 mg/kg)协同睡眠试验,以小鼠的睡眠潜伏期和睡眠时间为评价指标,筛选酸枣仁镇静催眠有效组分的最佳配伍。对所得有效组分最佳配伍的药效进行比较和验证实验。结果与对照组比较,给药A、C、E组小鼠自主活动减少(P<0.05、0.01),C、D组小鼠站立次数略有减少(P<0.05)。在阈上剂量戊巴比妥钠协同试验中,给药组C～F睡眠潜伏期显著缩短(P<0.01),B～F组睡眠时间显著延长(P<0.01)。经多元统计分析,酸枣仁镇静催眠有效组分的最佳配伍组合为总皂苷200 mg/kg、总黄酮0 mg/kg、总生物碱20 mg/kg。结论应用均匀设计与药效学相结合确定中药有效组分配伍的方法是可行的。验证实验表明,酸枣仁有效组分的最佳配伍组合可以达到与原药材相同的疗效。

To optimize the compatibility of three sedative-hypnotic components (such as saponin, flavone, and alkaloid) in Ziziphi Spinosae Semen. Methods Seventy mice were divided into seven (control and experimental A-F) groups by uniform design, and their autonomic activites and synergistic effect were observed. After ip administration of pentobarbital sodium above threshold dose (45 mg/kg), taking sleep latency and sleep duration of mice as evaluating indicators, the best compatibility was screened. Then a further experiment for comparing and verifying the efficacy of the best compatibility was conducted. Results Compared with the control group, autonomic activities of mice in experimental group A, C, and E were reduced (P<0.05, 0.01), and time of standing in groups C and D was slightly reduced (P<0.05). In the synergistic effect of pentobarbital sodium above threshold dose, sleep latency in experimental groups C-F was remarkably shortened (P<0.01) and sleep duration in experimental groups B-F was prominently prolonged (P<0.01). The results of multiple regression analysis showed that the optimized ratio of sedative and hypnotic active components in Ziziphi Spinosae Semen was saponin 200 mg/kg, flavone 0 mg/kg, and alkaloid 20 mg/kg. Conclusion It is feasible to screen the compatibility ratio by combining uniform design with pharmacodynamics. The verification experiment indicates that the sedative and hypnotic effect of the optimized compatibility components are the same as Ziziphi Spinosae Semen's.

天津市卫生局科研基金项目(02020)