CAJ | 학술논문

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57．40mg／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=1436．227e^（-0．1334t）-1436．227e^（-0．237t），表观药动学参数为：一级消除速率常数Ke=0．1334h^-1，消除半衰期tlm=5．1949h，一级吸收速率常数Ka=0．237h^-1，吸收半衰期tv2ka=2．9241h，血药峰浓度cmax=1436．227mg，Icg，达峰时间tmnx=5．5474h，清除率CI=0．0553mg／kg·h，药一时曲线下面积AUC=16826．35mg／kg·h，表观分布容积V=O．4142mg／kg，滞后期to=0．0104h。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。
위료탐색천리광제취물동간분（SsE）적약물대사동역학특정，수차채용이종창도억제솔약리효응법측정SsE약동학삼수。결과발현，재일정제량범위내급소서복강주사SsE，능교신속지산생약리효응，사이종창도억제솔현저제고；SsE최저유효량위57．40mg／kg，재소서체내대사부합일급반응일실모형，모형표체식위：c=1436．227e^（-0．1334t）-1436．227e^（-0．237t），표관약동학삼수위：일급소제속솔상수Ke=0．1334h^-1，소제반쇠기tlm=5．1949h，일급흡수속솔상수Ka=0．237h^-1，흡수반쇠기tv2ka=2．9241h，혈약봉농도cmax=1436．227mg，Icg，체봉시간tmnx=5．5474h，청제솔CI=0．0553mg／kg·h，약일시곡선하면적AUC=16826．35mg／kg·h，표관분포용적V=O．4142mg／kg，체후기to=0．0104h。표명SsE구유량호적항염작용，재소서체내기효쾌，소제만，생물이용도고，재궤체내분포유한，교집중우혈장，조직섭입소。
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.