更昔洛韦在家兔体内药动学研究

熊增慧;吴海燕;黄砚青;郭秋月

中国药学杂志 ›› 1996, Vol. 31 ›› Issue (12) : 739-742.

中国药学杂志 ›› 1996, Vol. 31 ›› Issue (12) : 739-742.
临床药学

更昔洛韦在家兔体内药动学研究

  • 熊增慧;吴海燕;黄砚青;郭秋月
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Pharmacokinetic studies of ganciclovir

  • Xiong Zenghui
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摘要

目的:了解抗病毒药更昔洛韦静脉注射后在家兔体内的药动学特性。方法:采用高效液相色谱法浏定药物在兔血、尿、组织中浓度的经时变化。结果:家兔静注3种荆童更昔洛韦后血药浓度变化符合开放式三房室模型特征。消除半衰期1.7 h。药物在体内分布广泛,肾脏中血药浓度最高。AUC与剂量呈正相关。24 h尿中原型药物排出黄占给药贡的90.8%。结论:更昔洛韦在家兔体内消除较快,无明显蓄积。

Abstract

OBJECTIVE:The pharmacokinetics of ganciclovir was investigated in rabbits. METHODS:The serum urine and tissues level of ganciclovir was determined by high performance liquid chromatography. RESULTS:The pharmacokinetics of ganciclovir fitted to a three compartment model after iv of 5,10,20 mg/kg ganciclovir respectively. The mean values for maximum concentration of drug in serum were 20, 39,89 pg/ml. The eliminative half-life was 1.7h(1.4~1.8 h). The AUC was 12.94,25.35 and 40.0(pg·h)/ml after iv injection. The distribution of ganciclovir was wide. The level of drug in kidney was higher. We also recovered 90.8% (16.3%)of the administered ganciclovir from the urine as unchanged drug within 24 hours. CONCLUSION;The elimination of Ganciclovir was quickly in rabbits. There is no significant culmulation.

关键词

更昔洛韦 / 药动学 / 高效液相色谱

Key words

ganciclovir / pharmacokinetics / high performance liquid chromatography

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导出引用
熊增慧;吴海燕;黄砚青;郭秋月. 更昔洛韦在家兔体内药动学研究[J]. 中国药学杂志, 1996, 31(12): 739-742
Xiong Zenghui. Pharmacokinetic studies of ganciclovir[J]. Chinese Pharmaceutical Journal, 1996, 31(12): 739-742

参考文献

1Buhles WC jr, Mastre BJ, Tinker AJ, et al. Ganciclovir treatment of life or sight-threatening cytomegaiovirus infection. Experience in 314 immunocompromised patients. Rev Inf Dis,1988,10(Suppl 3):5495. 2Dieterich DT, Chachoua A, Lafleus F, et al. Ganciclovir treatment of gastrointestinal infections caused by cytomegalovirus in patients with AIDS. Rev Inf Dis,1988,10(Suppl):5532. 3Mark AJ, Paulo DM, Donna MC, et al. Human pharmacokinetics and tolerance of oral Ganciclovir. Antimicrobial Agents and Chemotherapy,1987, 31(8):1251. 4Courtney F,Ronald S,Barbara CH,et al. Human pharmacokinetics of the antiviral drug DHPG. Glin Pharmacol Ther,1986,40:281. 5Stephen AS. Ganciclovir therapy for CMV infection. New York:Marcel Dekker Inc.1991:1—33.

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