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Research on pharmacokinetics of high-dose tamoxifen in non-small cell lung cancer patients
作者姓名:陈玲  李旭  李蓉  赵新汉  李睿  郑晓辉  王嗣岑
作者单位:[1]Department of Medical Oncology, the First Affiliated Hospital, Medical School of Xi'an JiaotongUniversity, Xi'an 710061, China [2]Medical Laboratory Center of the First Affiliated Hospital, Medical School of Xi'an Jiaotong University, Xi'an 710061, China [3]Department of Pharmacy, Medical School of Xi'an Jiaotong University, Xi'an 710061, China
基金项目:This work was supported by grant from Science Investigation Fund of Ministry of Health of China(No. 96-1-250).
摘    要:Objective To study the pharmacokinetics of tamoxifen at a high dosage, which will offer a theoretical support for an appropriate clinical use of the medicine in non-small cell lung cancer (NSCLC) patients. Methods Three qualified NSCLC patients are selected and given tamoxifen (TAM) 160 mg per Os. Blood samples were collected at different times and then analyzed by high-performance liguid chromatography. The PK-GRAPH program was used to obtain the parameters. Results The concentration-time courses of the TAM 160 mg were fitted to one-compartment model. The pharmacokinetic parameters were estimated as follows: Tmax (6. 35±1. 24)h, Cmax (217. 39±7. 71)ng/mL, AUC (12 127.39±636.16)ng · h/mL and T1/2ke(34. 13±2.97)h. Conclusion TAM 160mg one day per Os cannot reach the effective maintenance concentration in vivo required for reversing MDR in vitro. Loading-maintenance dose strategy is recommended to study the pharmacodynamies of tamoxifen at a high dosage in NSCLC patients.

关 键 词:非小细胞肺癌  它莫西芬  药物代谢动力学  高性能液相色谱法
文章编号:1671-8267(2007)02-0204-04

Research on pharmacokinetics of high-dose tamoxifen in non-small cell lung cancer patients
Chen Ling,Li Xu,Li Rong,Zhao Xinhan,Li Rui,Zheng Xiaohui,Wang Sicen.Research on pharmacokinetics of high-dose tamoxifen in non-small cell lung cancer patients[J].Academic Journal of Xi’an Jiaotong University,2007,19(2):204-207.
Authors:Chen Ling  Li Xu  Li Rong  Zhao Xinhan  Li Rui  Zheng Xiaohui  Wang Sicen
Abstract:Objective To study the pharmacokinetics of tamoxifen at a high dosage, which will offer a theoretical support for an appropriate clinical use of the medicine in non-small cell lung cancer (NSCLC) patients. Methods Three qualified NSCLC patients are selected and given tamoxifen (TAM) 160 mg per Os. Blood samples were collected at different times and then analyzed by high-performance liguid chromatography. The PK-GRAPH program was used to obtain the parameters. Results The concentration-time courses of the TAM 160 mg were fitted to one-compartment model. The pharmacokinetic parameters were estimated as follows: Tmax (6.35±1.24)h, Cmax (217.39±7.71)ng/Ml, AUC (12 127.39±636.16)ng·h/Ml and T1/2ke (34.13±2.97)h. Conclusion TAM 160mg one day per Os cannot reach the effective maintenance concentration in vivo required for reversing MDR in vitro. Loading-maintenance dose strategy is recommended to study the pharmacodynamics of tamoxifen at a high dosage in NSCLC patients.
Keywords:tamoxifen  pharmacokinetics  high-performance liquid chromatography  non-small cell lung cancer  resistance to drug
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