酮替芬、西咪替丁及红霉素对茶硷药动学影响的实验研究

研究酮替芬、西咪替丁及红霉素对家兔体内茶碱代谢的影响,结果表明:酮替芬可加快茶碱代谢,使茶碱的血清半衰期t1/2由2.74±0.75h缩短至2.33±0.56h,缩短14.96%;消除速率常数Ke由0.27±0.075/h增至0.32±0.066/h,增加20%.清除率由0.15±0.036增至0.18±0.047L/kg·h~(-1)。西咪替丁可抑制茶碱的代谢,使茶碱t1/2由2.06±0.33h延长至2.61±0.45h,延长26.69%,Ke由0.34±0.04/h减小至0.27±0.04/h下降20.59％,Cl由0.21±0.03降低至0.16±0.03L/kg·h~(-1),下降23.81%。红霉素亦可减慢茶碱代谢速率,使茶碱的t1/2由2.39±0.43h延长至3.54±0.89h,延长48.12%;Ke由0.30±0.06/h减小至0.21±0.07/h.降低30%,Cl由0.15±0.03下降至0.12±0.03L/kg·h~(-1),降低20%。

THE EFFECTS OF KETOTIFEN,CIMETIDINE & ERYTHRO-MYCIN ON THEOPHYLLINE PHARMACOKINETICS IN RABBITS

The effects of ketotifen, cimetidine & erythromycin on thebphy-lline pharmacokinetics in rabbits were studied. The results suggested that the elimination half-life of theophylline decresed from 2.74 ± 0.75 to 2.33 ± 0.56 h & the clearance of theophylline increased from 0.15±0.036 to 0.13 ± 0.047 1/kg·h-1 by ketotifen. The elimination half-life of theophylline increased from 2 .08 ± 0.33 to 2.6l±0.45 h & the clearance decreased from 0.2l±0.03 to 0.16±0.03 1/kg·h-1 by cimetidine. The elimination half-life of theophylline increased from 2.39 ± 0.43 to 3.54±0.89 h & the clearance decreased from 0.15±0.03 to 0.12±0.03 1/kg·h-1 by erythromycin.