独活香豆素组分对兔体内茶碱药动学参数的影响

Effect of total coumarins from Radix Angelicae Pubescentis on pharmacokinetics of theophylline in rabbits

目的:观察独活香豆素组分(TCP)对茶碱在家兔体内药动学的影响。方法:家兔16只随机分为A、B2组,A组静注单剂量氨茶碱15mg.kg-1;B组灌胃给予TCP50mg.kg-1,qd×3,末次给药1h后再静注等量氨茶碱,用紫外分光光度法测定茶碱血清浓度。结果:A、B2组茶碱的K分别为0.184,0.123h-1;t1/2为3.784,5.640h;Vd为1.112,1.119L;CL为0.204,0.138L.h-1;AUC为179.111,265.079mg.h.L-1。结论:TCP能抑制茶碱在兔体内的代谢,使K降低,t1/2延长,AUC增大,CL下降。

OBJECTIVE To investigate the effect of total coumarins from Radix Angelicae Pubescentis （TCP） on pharmacokinetics of theophylline in rabbits. METHODS Sixteen healthy rabbits were divided into group A and B randomly. Group A was intravenously injected with single-dose aminophylline 15 mg. kg^-1. group B was orally administered with TCP 50 mgo kg^-1, qd, for 3 days,and then given animophylline 15 mg.kg^-1. The serum concentrations of theophylline were determined with spectrophotometry. RESULTS The main pharmacokinetic parameters of theophylline in group A and B were as follows： elimination rate constant（K） were 0. 184 and 0. 123 h^-1 ; half life（t1/2） were 3. 784 and 5. 640 h; apparent volume of distribution（Vd） were 1.112 and 1. 119 L; clearance（CL） were 0. 204 and 0. 138 L.h^-1 ; and area under curve（AUC） were 179. 111 and 265. 079 g.h.mL^-1, respectively. CONCLUSION After administered with TCP, the rabbits serum concentrations and AUC of theophylline were significantly increased,t1/2 prolonged, K and CL decreased. It is concluded that TCP inhibits the normal metabolism of theophylline.