水合氯醛和苯巴比妥钠对大鼠体内氨茶碱药代动力学的影响

摘要

Objective To evaluate the effect of chloral hydrate and phenobarbital sodium on the pharmacokinetics of aminophylline in rats. Methods Thirty-six rats were divided into chloral hydrate group, phenobarbital sodium group and control group for a single dose tests. The blood concentrations of aminophylline were determined by high performance liquid chro-matography,then the pharmacokinetic parameters were calculated using DAS 2.0 software. Results In chloral hydrate group, phenobarbital sodium group and control group,the area under the plasma concentration time curve( AUC0.00) were (386. 503 ± 38.002), (140.704 ±13.634) and(414.497 ±33.909) mg · h-1 · L-1; the elimination half life(t1/2) were(3.442 ±0. 616), (4.824 ±1.333) and(3. 214 ±0.425) hours; the clearances ( CL) were(0. 056 ± 0. 006), (0. 149 ± 0. 013) and(0.050± 0.004) L· h-1 · kg-1;the maximum concentrations ( Cmax ) were ( 77. 457 ± 7. 780), (47. 403 ±6.644) and(77.637 ± 9.486) mg · L-1 ; the time of maximum concentration ( Tmax) were (1. 083 ± 0. 289), (1. 042 ± 0. 144) and (1.250 ± 0. 261) hours. There were statistically significant difference in AUC0.00 , t1/2, CL, Cmax and Tmax between phenobarbital sodium group and chloral hydrate group or control group(P <0.05) ,but there was no statistically significant difference in the parameters between chloral hydrate group and control group (P >0.05). Conclusion Phenobarbital sodium can significantly affect the pharmacokinetics of aminophylline in rats,but the effect of chloral hydrate on the pharmacokinetics of aminophylline is inconspicuous.%目的 观察麻醉剂量的水合氯醛和苯巴比妥钠对大鼠体内氨茶碱药代动力学的影响.方法 将36只大鼠分为水合氯醛组、苯巴比妥钠组和对照组,均进行单次给药试验,采用高效液相色谱(HPLC)法测定茶碱在大鼠体内的血药浓度,以DAS 2.0软件计算主要药代动力学参数.结果 水合氯醛组、苯巴比妥钠组和对照组的药代动力学参数中曲线下面积(AUC0-∞)为(386.503±38.002)、(140.704±13.634)和(414.497±33.909)mg h-1·L-1,消除半衰期(t1/2)为(3.442±0.616)、(4.824±1.333)和(3.214 ±0.425)h,清除率(CL)为(0.056±0.006)、(0.149±0.013)和(0.050±0.004)L·h-1·kg-1,达峰质量浓度(Cmax)为(77.457±7.780)、(47.403 ±6.644)和(77.637±9.486) mg·L-1,达峰时间(Tmax)为(1.083 ±0.289)、(1.042±0.144)和(1.250 ±0.261)h,苯巴比妥钠组与对照组、水合氯醛组的AUC0-∞、t1/2、CL、Cmax、Tmax比较差异均有统计学意义(P＜0.05),而水合氯醛组与对照组各项之间比较差异无统计学意义(P＞0.05).结论 苯巴比妥钠可显著影响大鼠体内氨茶碱的代谢,而水合氯醛对大鼠体内氨茶碱的代谢影响并不明显.