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LC and LC-MS Study of the Bioavailability and Metabolites of TM208 after Oral and Intravenous Administration to Rat
Wang, Jiao1; Song, Yan2; Zhang, Jianmei1; Li, Xiaona1; Ling, Xiaomei1,2; Li, Runtao2; Cui, Jingrong2
关键词Column liquid chromatography Mass spectrometry Bioavailability Metabolites Dithiocarbamate
刊名CHROMATOGRAPHIA
2010-09-01
DOI10.1365/s10337-010-1697-4
72期:5-6页:459-464
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Biochemical Research Methods ; Chemistry, Analytical
研究领域[WOS]Biochemistry & Molecular Biology ; Chemistry
关键词[WOS]3-CYANO-3,3-DIPHENYLPROPYL ESTER HYDROCHLORIDE ; TANDEM MASS-SPECTROMETRY ; HPLC
英文摘要

4-Methylpiperazine-1-carbodithioic acid 3-cyano-3,3-diphenylpropyl ester hydrochloride (TM208) is a new compound expected to become a new drug because of excellent in vivo and in vitro anticancer activity and low toxicity. A new, specific and sensitive LC method was set up for detecting the bioavailability of TM208 after oral administration. Samples were extracted with ethyl acetate after oral and intravenous administration. The retention times of TM208 and plunarizine (I.S.) were 5.5 and 9.9 min, respectively. The linear range was 0.125-50 mu g mL(-1). The accuracy (error, %) for three concentrations was 2.7-16.6%. Intra-day precision (as RSD) was 1.6-6.9% and inter-day precision was 7.6-11.5%. Extraction recovery of TM208 was 84.15-89.51% and that of the I.S. was 83.3%. Results from stability testing indicated that samples should be analyzed within 24 h or frozen immediately for later analysis. The bioavailable fraction (F) calculated by use of a non-compartment model was 63.3%. Pharmacokinetic data for TM208 were: mean residence time 24.3 and 5.1 h, V (d) 186.2 and 35.5 L kg(-1), and Cl 6.9 and 4.2 L h(-1) kg(-1) after oral and intravenous administration, respectively. LC-MS comparison of the metabolites after the two methods of administration showed the kind and content of metabolites of TM208 in rat urine after intravenous administration were more than after oral administration. The experimental results show that the low anticancer activity of TM208 after intravenous administration is related to rapid elimination of the drug, and that the kind and content of metabolites do not affect the bioactivity of TM208.

语种英语
WOS记录号WOS:000281174300013
项目编号7102107 ; K20090207 ; 2009ZX 09301-010
资助机构Natural Science Foundation of Beijing ; Open Foundation of the State Key Laboratory of Natural and Biomimetic Drugs ; National New Drug Research and Development Project of China
引用统计
被引频次:5[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/63822
专题北京大学药学院_化学生物学系
北京大学药学院_分子与细胞药理学系
作者单位1.Peking Univ, Sch Pharmaceut Sci, Dept Pharmaceut Anal, Beijing 100191, Peoples R China
2.Peking Univ, State Key Lab Nat & Biomimet Drugs, Beijing 100191, Peoples R China
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GB/T 7714
Wang, Jiao,Song, Yan,Zhang, Jianmei,et al. LC and LC-MS Study of the Bioavailability and Metabolites of TM208 after Oral and Intravenous Administration to Rat[J]. CHROMATOGRAPHIA,2010,72(5-6):459-464.
APA Wang, Jiao.,Song, Yan.,Zhang, Jianmei.,Li, Xiaona.,Ling, Xiaomei.,...&Cui, Jingrong.(2010).LC and LC-MS Study of the Bioavailability and Metabolites of TM208 after Oral and Intravenous Administration to Rat.CHROMATOGRAPHIA,72(5-6),459-464.
MLA Wang, Jiao,et al."LC and LC-MS Study of the Bioavailability and Metabolites of TM208 after Oral and Intravenous Administration to Rat".CHROMATOGRAPHIA 72.5-6(2010):459-464.
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