摘要
本文采用同位素示踪技术对^(125)Ⅰ-α-苦瓜子蛋白进行药代动力学研究。药物经小鼠腹腔内吸收较快,给药后2h 吸收82.3%。大鼠静脉给药后的主要药代参数T_1/2α=1.61±0.41(h),T1/2β=48.98±8.02(h),V_c=30.94±4.18(dpm/kg),K_(21)=0.084±0.032(1/h),K_(10)=0.072±0.020(1/h),K_(12)=0.23±0.08(1/h)。消除相半衰期较长,说明药物排除缓慢。药物生物利用度76.6%,提示α-苦瓜子蛋白在体内易吸收。大鼠静脉注入^(125)Ⅰ-α-苦瓜子蛋白后,血中放射性-时间数据经拟合符合二室开放动力学模型。放射性分布结果证实,最高是肾,其次为胚胎、卵巢、子宫、肝、脂肪等组织。药物主要经尿排泄,给药24h 后,排出剂量的67.3%。胆汁排泄证实此药不易形成肠肝循环。用Sephadex G-75柱层析方法证实,代谢产物仍保持原有分子大小,未被降解。
α-MM is a abortifacient protein isolated from the seeds of bitter gourd Momordica Charantia.Inthis paper,the absorption,distribution,metabolism and excretion of α-MM in mice and rats werestudied by using[^(125)Ⅰ]labelled method.After injection of ^(125)Ⅰ-α-MM into the abdomen of mice,drug was absorpted rapidly.Rate of absorption was 80% within 2 hours.The blood radioactivityreached maximum lervel in about 1 hour and leveled off slowly.However,radioactivity was found tobe the highest in the kidney,moderate in embryon,ovaries,uterus,liver,fat,heart and muscle,lower in the brain.After intravenous injection of ^(125)Ⅰ-α-MM to rats,the pattern of decline of theblood level of ^(125)Ⅰ-α-MM exhibited the characteristics of a two-compartment open model.Thepharmacokinetic parameters are as follows:t1/2α=1.61±0.41(h).t1/2β=48.98±8.02(h),Vc=30.94±4.18(dpm/kg),K21=0.084±0.032(1/h),K10=0.072±0.020(1/h),K12=0.23±0.08(1/h).It obviously showed that ^(125)Ⅰ-α-MM was eliminated slowly.After injection of ^(125)Ⅰ-α-MMinto the abdomen of rat,the radioactivity excreted in urine,feces and bile within 48 hours was84.0%,1.3%,0.03% of the administered dose.125Ⅰ-α-MM in the urine was detected to beunchanged drug by chromatogram of Sephadex-G75 column.
出处
《生殖与避孕》
CAS
CSCD
北大核心
1993年第4期258-263,共6页
Reproduction and Contraception
关键词
苦瓜子蛋白
药代动力学
(125)_I-α -momorcharin (α -MM),Phatmacokinetics
