千里光提取物冻干粉药代动力学研究-抗炎药理效应法

Study on pharmacokinetics of Senecio scandens extract by the method of anti-inflammatory pharmacological effect

为了探索千里光提取物冻干粉(SsE)的药物代谢动力学特征,首次采用耳肿胀度抑制率药理效应法测定SsE药动学参数。结果发现,在一定剂量范围内给小鼠腹腔注射SsE,能较迅速地产生药理效应,使耳肿胀度抑制率显著提高;SsE最低有效量为57.40 mg/kg,在小鼠体内代谢符合一级反应一室模型,模型表达式为:C=1 436.227 e^(-0.133 4 t)-1436.227 e^(-0.237 t),表观药动学参数为:一级消除速率常数Ke=0.133 4 h-1,消除半衰期t1/2Ke=5.194 9 h,一级吸收速率常数Ka=0.237 h-1,吸收半衰期t1/2Ka=2.924 1 h,血药峰浓度Cmax=1 436.227 mg/kg,达峰时间tmax=5.547 4 h,清除率Cl=0.055 3mg/kg.h,药-时曲线下面积AUC=16 826.35 mg/kg.h,表观分布容积V=0.414 2 mg/kg,滞后期t0=0.010 4 h。表明SsE具有良好的抗炎作用,在小鼠体内起效快,消除慢,生物利用度高,在机体内分布有限,较集中于血浆,组织摄入少。

Abstract： To explore the pharmaeokinetic characteristics of the frozen powder of Senecio scamtens extract （ SsE ）, the model with the method of anti-inflammatory pharmacological effect was employed and the pharmacokinetic parameters were determined. The results showed that intraperitoneal injection with SsE could significantly inhibit the tumefaction of the mouse ear very fast, the minimal effective dose of SsE was 57.40 mg/kg, the distribution of SsE in the mice was coincident with the first grade responsive and single compartment model, and the pharmacok inetics model was C= I 436.227 e^ （-0.133 4 t） -1436.227 e^ （-0.237 t）, with the parameters as Ke=0.133 4 h-^-1, h1/2ke=5.194 9 h, Ka= 0.237 h-1, h1/2ka=2.924 I h, Cmax=1436.227mg·kg-1, tmax=5.547 4 h, C1=0.055 3 mg·kg-1·h-1, AUC=I6 826.35 mg·＇kg-1·h, V=0.414 2 mg·kg-1, t0=0.010 4 h. It indicated that SsE performed relatively good anti-inflammation effect with a quick-action and higher-bioavailability but slow-elimination model, which was resuhed from the very limited distribution in tissues but mainly in plasma.