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Determination of 6258-70, a new semi-synthetic taxane, in rat plasma and tissues: Application to the pharmacokinetics and tissue distribution study
Alternative TitleDetermination of 6258-70, a new semi-synthetic taxane, in rat plasma and tissues: Application to the pharmacokinetics and tissue distribution study
Zhao Simin; Zhang Yuanyuan; Ju Ping; Gu Liqiang; Zhuang Rui; Zhao Longshan; Tang Xing; Bi Kaishun; Chen Xiaohui
2016
Source PublicationJournal of Pharmaceutical Analysis
ISSN2095-1779
Volume6Issue:4Pages:219-225
AbstractCancer is the leading cause of death all over the world. Among the chemotherapy drugs, taxanes play an important role in cancer treatment. 6258-70 is a new semi-synthetic taxane which has a broad spectrum of antitumor activity. A fast and reliable high performance liquid chromatography-tandem mass spectrometry (HPLC–MS/MS) method was developed for quantification of 6258-70 in rat plasma and tissues in this paper. After extraction by liquid-liquid extraction method with methyl tert-butyl ether, the samples were separated on a Kinetex C18 column (50mm×2.1mm, 2.6μm, Phenomenex, USA) within 3min. The method was fully validated with the matrix effect between 87.7% and 99.5% and the recovery ranging from 80.3% to 90.1%. The intra- and inter-day precisions were less than 9.5% and the accuracy ranged from ?3.8% to 6.5%. The reliable method was successfully applied to the pharmacokinetics and tissue distribution studies of 6258-70 after intravenous administration in rats. The pharmacokinetic results indicated that the pharmacokinetic behavior of 6258-70 in rats was in accordance with linear features within tested dosage of 1 to 4mg/kg, and there was no significant difference between the two genders. The tissue distribution study showed that 6258-70 had an effective penetration, spread widely and rapidly and could cross blood-brain barrier. The results of pharmacokinetics and tissue distribution may provide a guide for future study.
Other AbstractCancer is the leading cause of death all over the world. Among the chemotherapy drugs, taxanes play an important role in cancer treatment. 6258-70 is a new semi-synthetic taxane which has a broad spectrum of antitumor activity. A fast and reliable high performance liquid chromatography-tandem mass spectrometry (HPLC–MS 18 column (50mm×2.1mm, 2.6μm, Phenomenex, USA) within 3min. The method was fully validated with the matrix effect between 87.7% and 99.5% and the recovery ranging from 80.3% to 90.1%. The intra- and inter-day precisions were less than 9.5% and the accuracy ranged from ?3.8% to 6.5%. The reliable method was successfully applied to the pharmacokinetics and tissue distribution studies of 6258-70 after intravenous administration in rats. The pharmacokinetic results indicated that the pharmacokinetic behavior of 6258-70 in rats was in accordance with linear features within tested dosage of 1 to 4mg
Keyword6258-70 HPLC–MS/MS Pharmacokinetics Tissue distribution Therapeutics. Pharmacology RM1-950
Indexed ByCSCD
Language英语
CSCD IDCSCD:5777147
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Document Type期刊论文
Identifierhttp://ir.imr.ac.cn/handle/321006/155811
Collection中国科学院金属研究所
Affiliation中国科学院金属研究所
Recommended Citation
GB/T 7714
Zhao Simin,Zhang Yuanyuan,Ju Ping,et al. Determination of 6258-70, a new semi-synthetic taxane, in rat plasma and tissues: Application to the pharmacokinetics and tissue distribution study[J]. Journal of Pharmaceutical Analysis,2016,6(4):219-225.
APA Zhao Simin.,Zhang Yuanyuan.,Ju Ping.,Gu Liqiang.,Zhuang Rui.,...&Chen Xiaohui.(2016).Determination of 6258-70, a new semi-synthetic taxane, in rat plasma and tissues: Application to the pharmacokinetics and tissue distribution study.Journal of Pharmaceutical Analysis,6(4),219-225.
MLA Zhao Simin,et al."Determination of 6258-70, a new semi-synthetic taxane, in rat plasma and tissues: Application to the pharmacokinetics and tissue distribution study".Journal of Pharmaceutical Analysis 6.4(2016):219-225.
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