灯盏花素在家犬与家兔体内的药代动力学研究

目的:研究灯盏花素在家犬与家兔体内的药代动力学.方法:采用液-液萃取法制备血样供试品,HPLC法测定.结果:灯盏花素在家犬体内的过程符合双室模型,主要药动学参数为:A=56.93±23.14,B=1.61±1.11,α=0.2328±0.1321min-,β=0.0255±0.0187min-,T1/2α=2.98±1.42min,T1/2β=27.14±14.35min,K21=0.0312±0.0112min-,K10=0.1904±0.1319min-,K12=0.0367±0.0306min-1,CL=39.41±20.44ml·min-,AUC=3074±1055mg·min·L-;灯盏花素在家兔体内的过程符合双室模型,主要药动学参数为:A=2.64±1.12,B=0.28±0.12,α=0.1439±0.0681min-,β=0.0162±0.0456min-,t1/2α=4.82±1.65min,t1/2β=42.66±18.77min,K21=0.0285±0.0147min-,K10=0.0820±0.00378min-,K12=0.0496±0.0241min-,CL=337.05±156.48ml·min-1,AUC=356±114mg·min·L-1.结论:灯盏花素在家犬与家兔体内半衰期很短,其作用时间短,消除速度快.

Pharmacokinetics of Breviscapine in Dogs and Rabbits Following Single Intravenous Administration

OBJECTIVE: To study pharmacokinetics of breviscapine in dogs and rabbits after iv. single dose. METHODS: Lc/Lc extract was used to prepare test samples and HPLC was used to determine breviscapine. RESULTS: Breviscaplin was fitted to double-department model in dogs and rabbits after iv. single dose. The main parameters in dogs were: A = 56.93 +/- 23.14, B = 1.61 +/- 1.11, alpha = 0.2328 +/- 0.1321 min, beta = 0.0255 +/- 0.0187 min(-1), t(1/2alpha) = 2.98 +/- 1.42 min, t(1/2beta) = 27.14 +/- 14.35 min, K21 = 0.10312 +/- 0.0112 min(-1), K10 = 0.1904 +/- 0.1319 min(-1), K12 = 0.0367 +/- 0.0306 min(-1), CL = 39.41 +/- 20.44 ml x min(-1), AUC = 3074 +/- 1055 mg x min x L(-1), respectively. The main parameters in rabbits were:A = 2.64 +/- 1.12, B = 0.28 +/- 0.12, alpha = 0.1439 +/- 0.0681 min(-1), beta = 0.0162 +/- 0.0456 min(-1), t1/2alpha = 4.82 +/- 1.65 min, th1/2beta = 42.66 +/- 18.77 min, K21 = 0.0285 +/- 0.0147 min(-1), K10 = 0.0820 +/- 0.00378 min(-1), K12 = 0.0496 +/- 0.0241 min, CL = 337.05 +/- 156.48ml x min(-1), AUC = 356 +/- 114 mg x min x L(-1), respectively. CONCLUSION: Breviscapine has short half-life after intravenous administration to dogs and rabbits,which show breviscapine is eliminated rapidly and has short action time.