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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。
In this paper, isotope tracer technique was used to study the pharmacokinetics of ~ (125) Ⅰ -α-Momordicae protein. Absorption of drugs by intraperitoneal mice faster, after 2h absorption 82.3%. The main pharmacokinetic parameters of rats after intravenous administration were T 1 / 2α = 1.61 ± 0.41 (h), T1 / 2β = 48.98 ± 8.02 (h), Vc = 30.94 ± 4.18 (dpm / kg) ± 0.032 (1 / h), K_ (10) = 0.072 ± 0.020 (1 / h), K_ (12) = 0.23 ± 0.08 (1 / h). Elimination phase half-life is longer, indicating that the drug is excluded slowly. Drug bioavailability of 76.6%, suggesting that α-bitter melon protein in the body easily absorbed. After intravenous injection of ~ (125) Ⅰ -α-Momordicae protein into rat, radioactive-time data in the blood were fitted to two-compartment open kinetic model. Radioactive distribution results confirmed that the highest is the kidney, followed by embryos, ovaries, uterus, liver, fat and other tissues. The main drug excretion by urine, after administration of 24 hours, the discharge dose of 67.3%. Bile excretion confirmed that the drug is not easy to form enterohepatic circulation. Sephadex G-75 column chromatography confirmed that the metabolites remained the original size of the molecule, was not degraded.