大鼠肌内注射20(S)-人参皂苷Rg3的药动学研究

 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,t_1/2(ke)为0.75h,t_(peak)为0.116h,ρ_max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。

Studies on Pharmacokinetics of 20(S)-Ginsenoside Rg3 After Intramuscular Administration to Rats

OBJECTIVE To investigate the pharmacokinetics of 20(S)-ginsenoside Rg3 in plasma ,distribution in organs,and excretion by urine and bile after intramus cular 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.