| 埃博霉素B的大鼠体内药动学及组织分布 |
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| 引用本文： | 徐智儒,肖璘,廖建维,代常亮,秦燕.埃博霉素B的大鼠体内药动学及组织分布[J].中国医药工业杂志,2012,43(5):363-367. |
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| 作者姓名： | 徐智儒 肖璘 廖建维 代常亮 秦燕 |
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| 作者单位： | 1. 中国医药工业研究总院上海医药工业研究院,创新药物与制药工艺国家重点实验室,上海200040
2. 浙江海正药业股份有限公司,浙江台州,318000 |
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| 摘 要： | 分别建立了液相色谱-质谱法和高效液相色谱法测定大鼠血浆和组织中的埃博霉素B,并考察该化合物在大鼠体内的药动学及组织分布情况.大鼠按3个剂量(0.5、1和2 mg/kg)静脉给药后测定不同时间点的血浆浓度,数据经拟合处理,符合二室开放模型特征,主要药动学参数如下:t1/28(7.17±0.68)、(7.65±1.40)和(6.68±0.36)h,AUC0(_1) (60.4±6.5)、(160.4±37.8)和(428.8±67.1) ng·ml-1-h.荷瘤Wistar大鼠1 mg/kg静脉给药后,于不同时间点测定各组织药物浓度,结果显示药物迅速从血浆分布到组织,并且在肿瘤中的滞留时间较长.
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| 关 键 词： | 埃博霉素B 药动学 组织分布 液相色谱-质谱 高效液相色谱 测定 |
Pharmacokinetics and Tissue Distribution of Epothilone B in Rats |
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| Authors: | XU Zhiru XIAO Lin LIAO Jianwei DAI Changliang QIN Yan |
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| Institution: | 1(1.State Key Lab.of New Drug and Pharmaceutical Process,Shanghai Institute of Pharmaceutical Industry,China State Institute of Pharmaceutical Industry,Shanghai 200040;2.Zhejiang Hisun Pharmaceutical Co.,Ltd.,Taizhou 318000) |
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| Abstract: | The validated LC-MS and HPLC method were developed for the determination of epothilone B in rat plasma and tissue,respectively.The pharmacokinetic properties of epothilone B were examined after a single iv injection of 0.5,1 and 2 mg/kg to rats,respectively.The results suggested that the pharmacokinetic properties of epothilone B fitted well into a two-compartment open model with t1/2β of(7.17±0.68),(7.65±1.40) and(6.68±0.36)h,and AUC0→t of (60.4±6.5),(160.4±37.8) and(428.8±67.1)ng·ml-1·h according to the single dose of 0.5,1 and 2 mg/kg,respectively.A single dose(1 mg/ml) of epothilone B to tumor bearing Wistar rats resulted in a very rapid wide distribution from plasma to tissue.Plasma elimination was very rapid,while the elimination in tumor was rather slow. |
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| Keywords: | epothilone B pharmacokinetics tissue distribution LC-MS HPLC determination |
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