摘要
本文报告了10名慢性阻塞性肺疾病患者服用红霉素前后稳态时氨茶碱药代动力学的变化。整个实验分四个期,Ⅰ期为单服氨茶碱3天至稳态;Ⅱ期为二药合并用药5天;Ⅲ期为二药合并用药10天;Ⅳ期为停用红霉素继续单服氨茶碱5天。各期测得的氨茶碱药代动力学参数,C_(TPK)^(SS)分别为9.84,12.14,13.37和11.66μg/ml;CL^(SS)分别为O.053,0.043,0.039和0.047/h/kg;t1/2分别为8.45,10.90,12.23和9.70h;V_d^(SS)分别为0.642,0.685,0.695和0.628 l/kg。结果经统计学处理,与Ⅰ期比较Ⅱ期、Ⅲ期的t1/2、CL^(SS),C_(TPK)^(SS)差异均有显著意义;而Ⅱ、Ⅲ、Ⅳ期的V^(SS)差异均无显著意义(P>0.0 5);Ⅱ、Ⅲ、Ⅳ期的C_(TPK)^(SS)与Ⅰ期比较分别升高了23.37,35.87及18.50%;Ⅱ、Ⅲ期的CL^(SS)与Ⅰ期比较分别下降了18.87和26.42%。
We compared steady-state theophylline pharmacokinetics in10 patients with chronic obstructive pulmonary disease (COPD) before andimmediately after erythromycin therapy. Theophylline (3mg/kg) was givenof four separate study stage: (1) All subjects received a three-day courseof oral aminophylline to steady-state at prior to staring erythromycin. (2)On the fifth day of erythromycin adminstration (1g daily). (3) On the tenth day of erythromycin administration. and (4) the fifth day after thecourse of erythromycin was completed. After the last dose of aminophy-lline during each study stage plasma was analyzed for theophylline, usingHigh Pressure Liquid Chromatography. Mean theophylline pharmacokineticparameter values on each of the 4 study stages were: Steady-state peakplasma concentration (C_(TPK)^(SS)), 9. 84, 12. 14, 13. 37 and 11 .66μg/ml; Steady-state clearance (CL^(SS)), 0 .053, 0 .043, 0.039 and 0 .047 l/h/kg; Eliminationhalf-life (t1/2), 8.45, 10. 90, 12.23 and 9.70h; and steady-state volume ofdistribution (V_d^(SS), 0. 642, 0 .685, 0 .695 and 0 .628 l/kg. Each subject actedas his own control. Mean peak theophylline levels increased by 23. 37,35.87% at the second and third study stage (p<0.001), Mean theophy-lline clearance decreased by 18.87, 26.42% at the second and third studystage (p<0.05). Erythromycin did not significantly affect theophyllinevolume of distribution (p>0.05).
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
1991年第4期221-224,206,共5页
The Chinese Journal of Clinical Pharmacology