| 氟他胺的主要代谢产物2—羟基氟他胺在正常及CCl4中毒大鼠的药物动 … |
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| 引用本文： | 许长江 李端. 氟他胺的主要代谢产物2—羟基氟他胺在正常及CCl4中毒大鼠的药物动 …[J]. 中国药理学报, 1999, 20(7): 655-658 |
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| 作者姓名： | 许长江 李端 |
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| 摘 要： | 研究氟他胺的一个主要活性代谢产物２－羟基氟他胺在正常及ＣＣｌ４中毒大鼠的药物动力学。方法：正常及ＣＣｌ４中毒大鼠灌胃ＨＦ２５ｍｇ．ｋｇ＾－１，采用高压液相色谱法测定ＨＦ浓度，以氟他胺为内标，色谱柱填料为ＹＷＧ Ｃ１８，流动相为甲醇：水＝３：２，检测波长为２９５ｎｍ，结果：与正常大鼠比较，ＨＦ在ＣＣｌ４中毒大鼠的消除明显受到抑制。
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| 关 键 词： | 2－羟基氟他胺 药物动力学 四氯化碳中毒 |
Pharmacokinetics of 2-hydroxyflutamide, a major metabolite of flutamide, in normal and CCl4-poisoned rats. |
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| C J Xu,D Li. Pharmacokinetics of 2-hydroxyflutamide, a major metabolite of flutamide, in normal and CCl4-poisoned rats.[J]. Acta Pharmacologica Sinica, 1999, 20(7): 655-658 |
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| Authors: | C J Xu D Li |
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| Affiliation: | Department of Pharmacology, School of Pharmacy, Shanghai Medical University, China. dli@shmu.edu.cn |
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| Abstract: | AIM: To study the pharmacokinetics of 2-hydroxyflutamide (HF), a major active metabolite of flutamide (Flu), in normal and CCl4-poisoned rats. METHODS: Normal and CCl4-poisoned rats were given i.g. HF 25 mg.kg-1. HF concentrations of plasma were determined by HPLC with YWG C 18 column, Flu was used as an internal standard. The mobile phase was composed of methanol: water = 3:2 (vol), and absorbance was measured at lambda 295 nm. RESULTS: HF elimination was inhibited in CCl4-poisoned rats compared with normal rats. K decreased from (0.11 +/- 0.05) to (0.05 +/- 0.01) h-1 (P < 0.01), T1/2 was prolonged from (6.8 +/- 1.9) to (14 +/- 4) h (P < 0.01), Cl decreased from (0.18 +/- 0.06) to (0.12 +/- 0.02) L.kg-1.h-1 (P < 0.05), AUC increased from (149 +/- 47) to (226 +/- 54) mg.L-1.h (P < 0.05). CONCLUSION: This HPLC assay was sensitive and precise, and the elimination of HF was inhibited due to CCl4 poisoning. |
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