共查询到18条相似文献,搜索用时 78 毫秒
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蛇毒神经生长因子在大鼠体内的药物代谢动力学与周围神经分布 总被引:1,自引:0,他引:1
用[125I]标记结合高效液相色谱法和酸沉法研究大鼠体内蛇毒神经生长因子(vNGF)药物代谢动力学.[125I]vNGF体外有刺激神经突起生长活性.药后血清存在游离和结合[125I]vNGF及[125I]降解物.12mg·kg-1iv后t1/2α为0.13h,t1/2β为3.8h;12和48mg·kg-1im后t1/2β为7.1和4.1h,AUC与剂量呈正比,CLS相近,生物利用度为0.62.体外[125I]vNGF与血清最大结合率24.6%±0.4%,平衡解离常数3.2±0.3nmol·L-1.im后颈上神经节,注药侧和对侧坐骨神经放射性明显高于血清,注药侧最高,不被100倍非标vNGF抑制.主要经尿排泄,2d排出约86%. 相似文献
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中华眼镜蛇蛇毒神经生长因子在大鼠体内分布的研究 总被引:2,自引:0,他引:2
中华眼镜蛇蛇毒神经生长因子经125I标记后从大鼠舌静脉注入,2h后观察其在体内的分布。结果显示:主要分布在肾、肺、肝等脏器及周围神经,脑、喷球及脊髓的含量几乎为零。肾组织含量最高,占72%,说明代谢物主要经肾组织从尿中排除。 相似文献
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用~(131)I按氯胺T法标记眼镜蛇毒细胞毒素14,观察其在大鼠体内的分布,静脉给药后0.5h,分布最多的是肾,每mg组织放射性达5979dpm,为对照组的14倍,肝、脾、胰、肾上腺亦有较高分布,给药后2h,脑组织亦见分布,其每mg组织放射性为50dpm,是对照组的3倍。 相似文献
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研究醋酸艾塞那肽(exendin-4)在Wistar大鼠体内的药物代谢动力学,组织分布以及排泄特征。IODOGEN(四氯二苯基苷脲)法制备^125I-exendin-4,大鼠皮下或静脉注射,^125I-exendin-4,以放射性核素示踪动力法检测血液中的药物浓度,由非房室模型评价药物动力学参数。同时研究了大鼠皮下注射^125I-exendin-4后的组织分布和排泄。大鼠皮下注射^125I-exendin-4后Tmax和t1/2分别是(0.25±0.02)h和(1.28±0.14)h,绝对生物利用度为(65.5±10.2)%;^125I-exendin-4的分布快速而广泛,其中以肾脏中最高,而在脑组织中只有微量^125I-exendin-4;^125I-exendin-4主要随尿液排泄。实验结果与国外公布的实验数据基本一致。醋酸艾塞那肽在大鼠中的药物代谢动力学参数为临床试验提供了科学依据。 相似文献
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目的:研究重组葡激酶在大鼠体内的药物动力学。方法:采用氯胺T法标计125I重组葡激酶(放化纯度>98%),给大鼠静注三种不同剂量后进行药物动力学试验,数据采用 3p87程序按二室模型计算药动学参数。结果:t1/2α约为0.913~1,336min,t1/2β约为22.51~23.89min。5min后各组织有较高放射量,以肾、脾、肝为最高。到120min各组织只有很少的放射量。尿、胆汁在3h内可明显测到放射性,24h内从尿中排出给药量的42.8%放射量,从粪中排出 7 5%,在33h内从胆汁中排出给药量的 9.4%放射量。 SpePAGE电泳结果表明,尿和胆汁中原形葡激酶甚微,排出物主要是分解产物。结论:125I-r-Sak静注,在大鼠体内分布快,分布广,消除快。 相似文献
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目的研究索西沙星在小鼠体内的药物代谢动力学,分析索西沙星的药物代谢动力学/药物效应动力学(PK/PD)参数。方法使用HPLC-MS/MS法,以莫西沙星为内标,以梯度甲醇-水为流动相,测定灌胃5 mg.kg-1后小鼠血液中索西沙星的含量。以WinNonlin软件计算动力学参数。结果小鼠血液中索西沙星Cmax为1.085μg.mL-1,Tmax为10 min,T1/2为1.425 h,AUC0~24为1.101μg.mL-1.h,对金黄色葡萄球菌、肺炎链球菌、流感嗜血杆菌、副流感嗜血杆菌和化脓链球菌的Cmax/MIC50均大于8。结论索西沙星在小鼠体内的吸收、分布及代谢较快,对多种细菌具有较好的活性。 相似文献
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二甲双胍在大鼠体内的药动学和组织分布 总被引:2,自引:0,他引:2
目的研究二甲双胍在大鼠体内的药动学和组织分布。方法大鼠腹腔注射二甲双胍(100 mg·kg~(-1))并在0、10、20、30、60、120、240、480和720 min共9个时间点采集血样(大鼠共3只)和各组织样品(大鼠共27只,每个时间点3个),测定血浆和组织样品中的二甲双胍的浓度。结果AUC为(4 676±s 171)mg·min·L~(-1),CL为(21.4±0.8)mL·min~(-1)·kg~(-1),t(1/2)为(50±5)min,t_(max)为(20.0±1.0)min,c_(max)为(59±4)mg·L~(-1):给药后10 min,所有的组织中都能检测到二甲双胍,给药后12 h,肝脏、肺、脾脏和大脑中已检测不到二甲双胍。结论二甲双弧的血药浓度-时间曲线符合一室模型,在体内叹收快,兮布广泛,清除迅速,且可能主要是由肾脏清除;二甲双胍能够进入大脑。 相似文献
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Pharmacokinetics,tissue distribution,and excretion of FGF‐21 following subcutaneous administration in rats 下载免费PDF全文
Zihong Wei Xingyan Zhang Jing Gao Xiaojie Wang Xiaokun Li Weidang Wu Wei Li Xiulin Yi Yong Zeng Changxiao Liu 《Drug testing and analysis》2018,10(7):1061-1069
As one of the fibroblast growth factor (FGF) superfamily, FGF‐21 has been extensively investigated for its functions and roles since its discovery. It has been demonstrated to be one of the key regulators for glucose and lipid metabolism, and exhibits beneficial effects on cardiovascular disease. However, studies focusing on its pharmacokinetic behavior in vivo as a novel therapeutic agent have not been reported. In the present study, rapid and sensitive analytical approaches including radioactivity assay and assay after precipitation/separation by high performance liquid chromatography (HPLC) were established to determine the content of FGF‐21 tagged with 125I in plasma, tissue, and excrement. The results indicated that FGF‐21 were quickly absorbed into systematic circulation and slowly eliminated; Cmax and exposure increased in a dose‐dependent manner, exhibiting a typical linear pharmacokinetic pattern. Tissue distribution also confirmed that the kidney is the primary organ for FGF‐21 to be distributed, even though radioactivity of FGF‐21 was recovered in all tissues examined. In addition, the results also supported that urinary excretion was the critical route for FGF‐21 to be eliminated. The study fully clarifies the pharmacokinetic behavior of FGF‐21 and can provide valuable information and support further safety and toxicology development. 相似文献
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ELISA法对神经生长因子在大鼠体内药代动力学的研究 总被引:2,自引:1,他引:1
目的研究神经生长因子(NGF)在大鼠体内的药代动力学。方法制备兔抗NGF抗体,用双抗体夹心酶联免疫吸附实验(ELISA)法测定大鼠血浆NGF浓度。结果大鼠iv32μg·kg-1后血药浓度时间曲线符合二室开放模型,T1/2α为0330h,T1/2β为15h。大鼠NGFim32μg·kg-1后血药浓度时间曲线符合一室一级吸收,血浆NGF浓度达峰时间为371h,T1/2(Ke)为430h,24h吸收百分率为691%。结论NGF肌注吸收良好,血浆NGF浓度可在较长时间内维持在有效浓度以上。 相似文献
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黄芪甲苷在兔体内的药动学和在大鼠的排泄(英文) 总被引:6,自引:0,他引:6
目的 :研究黄芪甲苷在家兔体内的药动学和在大鼠的排泄。方法 :健康家兔和大鼠一次静脉注射 (静注 )给予黄芪甲苷 4mg·kg- 1,高效液相色谱 蒸发光散射检测器法检测兔血浆和大鼠尿及粪黄芪甲苷浓度 ,用 3P97药动学软件对兔血浆浓度 时间数据进行动力学分析和计算药动学参数 ,并估算大鼠体内的排泄情况。结果 :黄芪甲苷静注给药后 ,T12 α 为 0 .10h ,T12 β 为 1.4h ,Vc 为 0 .15L·kg- 1,VD 为 0 .6L·kg- 1,Cl为 0 .32L·h- 1·kg- 1,AUC为 15mg·L- 1·h。大鼠静注给药后 ,原形从尿和粪排出量分别为给药量的 16 %和 3.2 %。结论 :家兔体内黄芪甲苷的动力学过程符合二室模型 ,大鼠仅有少量原形药物从尿和粪排泄。 相似文献
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Minematsu T Sonoda T Hashimoto T Iwai M Oppeneer T Felder L Shirai N Miyashita A Usui T 《Biopharmaceutics & drug disposition》2012,33(3):160-169
YM155 monobromide is a novel small-molecule survivin suppressant. The pharmacokinetics, distribution and excretion of YM155/[14C]YM155 were investigated using males and pregnant or lactating female rats after a single intravenous bolus administration. For the 0.1, 0.3 and 1 mg/kg YM155 doses given to male rats, increases in area under the plasma concentration-time curves were approximately proportional to the increase in the dose level. After administering [14C]YM155, radioactivity concentrations in the kidney and liver were highest among the tissues in both male and pregnant rats: e.g. 14.8- and 5.24-fold, respectively, and higher than in plasma at 0.1 h after dosing to male rats. The YM155 concentrations in the brain were lowest: 25-fold lower than in plasma. The transfer of radioactivity into fetuses was low (about 2-fold lower than in plasma). In lactating rats, the radioactivity was transferred into milk at a level 8- to 21-fold higher than for plasma. Radioactivity was primarily excreted in feces (64.0%) and urine (35.2%). The fecal excretion was considered to have occurred mainly by biliary excretion and partly by secretion across the gastrointestinal membrane from the blood to the lumen. 相似文献