重组水蛭素肠溶胶囊单次和多次给药在Beagle犬体内的药动学研究
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篇名: 重组水蛭素肠溶胶囊单次和多次给药在Beagle犬体内的药动学研究
TITLE:
摘要: 目的:研究重组水蛭素肠溶胶囊单次和多次给药在Beagle犬体内的药动学特征。方法:取12只Beagle犬按随机对照法分为单次ig组和单次iv组,每组6只,按0.2 mg/kg ig或iv重组水蛭素,收集血样;清洗2周后12只犬按0.2 mg/kg ig重组水蛭素,连续给药7 d,收集血样,作为多次ig组。采用酶联免疫吸附法测定血浆中重组水蛭素浓度,以DAS 2.0软件计算药动学参数。结果:单次ig和单次iv重组水蛭素在Beagle犬体内药动学特征均符合二室模型,ig重组水蛭素肠溶胶囊的绝对生物利用度为(14.908±1.868)%;单次ig组和多次ig组犬体内重组水蛭素的tpeak分别为(2.105±0.243)、(3.000±0.000) h,t1/2β分别为(8.660±2.965)、(14.870±2.710) h,cmax分别为(10.700±0.872)、(12.05±1.587) ng/mL,AUC0-1 440 min分别为(55.250±4.386)、(58.978±6.002) ng·h/mL,两组间差异无统计学意义(P>0.05)。结论:ig重组水蛭素肠溶胶囊可一定程度被吸收入血;连续多天ig重组水蛭素肠溶胶囊在犬体内不产生蓄积,不改变其药动学特征。
ABSTRACT: OBJECTIVE: To study the pharmacokinetic characteristics of Recombinant hirudin enteric-coated capsule by single and multiple administration in Beagle dogs. METHODS: 12 Beagle dogs were divided into single ig group and single iv group by random control method, 6 in each group. Recombinant hirudin 0.2 mg/kg was intragastrically administrated or intravenously injected, blood sample was collected; after 2 weeks of cleaning, 12 dogs were intragastrically administrated recombinant hirudin 0.2   mg/kg, for 7 d. Sample blood was collected, referred to multiple ig group. Recombinant hirudin concentration in plasma was determined by enzyme-linked immunosorbent assay, and pharmacokinetic parameters were calculated by DAS 2.0 software. RESULTS: The results showed that pharmacokinetics by ig and iv recombinant hirudin in Beagle dogs fitted to two-compartment model, absolute bioavailability of ig Recombinant hirudin enteric-coated capsule was (14.908±1.868)%; the pharmacokinetic parameters in single ig group and multiple ig group were tpeak of (2.105±0.243), (3.000±0.000) h, t1/2β of (8.660±2.965), (14.870±2.710) h, cmax of (10.700±0.872), (12.05±1.587) ng/mL, AUC0-1 440 min of (55.250±4.386), (58.978±6.002) ng·h/mL, without statistical significances in two groups(P>0.05). CONCLUSIONS: The ig Recombinant hirudin enteric-coated capsule can be absorbed into the blood to a certain extent. There is no accumulation for ig Recombinant hirudin enteric-coated capsule for several days, and it dose not change the pharmacokinetic characteristics.
期刊: 2017年第28卷第7期
作者: 杨辉,周远大,何海霞,范开
AUTHORS: YANG Hui,ZHOU Yuanda,HE Haixia,FAN Kai
关键字: 重组水蛭素;肠溶胶囊;注射液;单次给药;多次给药;药动学;Beagle犬
KEYWORDS: Recombinant hirudin; Enteric-coated capsule; Injection; Single administration; Multiple administration; Pharmacokinetics; Beagle dogs
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