摘要
目的 研究20（S）-人参皂苷Rg3经肌内注射后在大鼠体内的药动学情况,包括血药动力学研究,组织分布情况,在尿和胆汁中的排泄情况等方面的内容。方法本实验采用蒸发光散射检测法测定药物在血液和组织中的浓度,用3P97药动学程序进行数据处理,方法快捷、简便,结果的精密度、稳定性和回收率均好。结果20（S）-人参皂苷Rg3肌内注射后（1.5mg·kg^-1）,其药动学模型为一室模型,t1/2（ke）为0.75h,t（peak）为0.116h,ρmax为13.9mg·L^-1,AUC为16.6mg.h·L^-1;肌注后在心、肝、脾、肺、肾中可以检测到有20（S）-人参皂苷Rg3存在,而在脑、胃、肠、体脂、肌肉和生殖腺中均未检测到;药物主要经尿液排泄,给药8h内,20（S）-人参皂苷Rg3经尿液排出药物总量的72.1%,经胆汁排泄的药物占药物总量的10.1%;药物与蛋白的结合率为15%-17%,且不随浓度的变化而改变。结论20（S）-人参皂苷Rg3肌内注射后可以很快被吸收进入血液,迅速达到血药浓度的峰值,它在体内的代谢速度较快,且大部分药物经尿液由肾脏排出体外,在体内基本无蓄积。
OBJECTIVE To investigate the pharmacokinetics of 20 （S）-ginsenoside Rg3 in plasma , distribution in organs, and excretion by urine and bile after intramuscular administration to rats. METHODS Rat plasma samples were processed by solidphase extraction and the concentrations were detemined by HPLC/ELSD（Evaporative Light-scattering Detector） method. The program of 3P97 was applied to process the concentration-time curves of 20 （S）-ginsenoside Rg3 in rat plasma after intramuscular injection （im） of 1.5 mg · kg^-1. RESULTS The pharmacokinetics of 20 （S）-ginsenoside Rg3 followed first order kinetics and plasma concentration versus time data were adequately described by an one-compartment model. The concentrations of 20 （S） -ginsenoside Rg3 in heart, liver, spleen, lung and kidney were determined respectively. It was failed to detect the concentrations in brain, stomach, intestines, bodylipo, muscle and testicle. 72. 8% of the drug was eliminated during 8 h by urine and 10. 1% was eliminated by bile. CONCLUSION The drugs can be absorpded quickly into blud and distrubted into heart, lung, liver, spleen and kindey. Most of them are eliminated during 8 h by bile and urine.
出处
《中国药学杂志》
CAS
CSCD
北大核心
2007年第14期1087-1090,共4页
Chinese Pharmaceutical Journal
