[~3H]冬凌草乙素在小鼠体内的吸收、分布和排泄  

Absorption,distribution and excretion of [~3 H] Rubescensine B in mice

作　　者：张覃沐[1] 王绵英 王庆端[1] 曹生海 王德喜 管顺朝[2] 仪明光 

机构地区：[1]河南省医学科学研究所 [2]河南省科学院同位素研究所 [3]中国科学院原子能研究所

出　　处：《郑州大学学报（医学版）》1990年第1期13-17,共5页Journal of Zhengzhou University(Medical Sciences)

摘　　要：采用液体闪烁计数技术研究[~3H]冬凌草乙素在小鼠体内的吸收、分布和排泄。给小鼠经口灌胃(ig)或尾静脉注射(iv)[~3H]冬凌草乙素后,很快被吸收并广泛分布到各组织中。其中以肺、胆囊和肝脏中放射性为最高;其次为肠、胃、胰腺等,肌肉、胸腺和骨中含量最少。iv[~3H]冬凌草乙素3.7×10~7Bq(1.23mg)/kg24h放射性自粪和尿中排泄占总注入量的58.3%。血中放射性—时间曲线表明药代动力学模型似符合二室开放模型。其各时相半衰期分别为T 1/2α=17.9min,T 1?2β=12.7h,其它动力学参数分别为K_(12)=1.38h^(-1),K_(21)=0.84h^(-1),K_(10)=0.15V_c=1.4L kg,V_d=3.9 L kg;ig[~3H]冬凌草乙素3.7×10~7Bq(1.23mg)kg,很快被吸收,其血中放射性—时间曲线似符合二室开放模型,其药代动力学参数分别为T_1 2Ka=17.0min,T_1 2K_e=11.3h.K_a=2.48h^(-1).K_e=0.001min^(-1).以ig和iv[~3H]冬凌草乙素血中放射性—时间曲线下面积计算生物利用度(F)为65%。Rubescensine B was isolated from Rabdosia rubescens Hemsl. After [~3H]rubescensine B 1.23mg (1 mci)/kg was injected iv to mice, it was rapidly takenup by various organs. The highest radioactivities were found in the lung,the gall bladder and the liver, then the intestine, the stomach and the pancreasThe lowest radioactivities were noticed in the muscle, thymus, bone aand brain. The excretion amounted to 58.3% of the injected radioactivitywithin. 24 h in feces and urine. After po and iv, the plasma radioactivity sh-owed an initial rapid drop and a subsequent slow decline. The disappearancecurve was analysed on the basis of a two exponential-curve representing amodel consisting of 2 compartments. After iv, T1 /2α=17.9min, T1/2β=12.7h,the central volume V_c=1.4L/kg. After po T1/2K_a=17min, T1/2.K_e=11.3h.The biologic availability of Rubescensine in mice 65%.

关 键 词：[~3H]冬凌草乙素 吸收 分布 排泄 小鼠 

分 类 号：R[医药卫生]