Anderson P L, Noormohamed S E, Henry K, Brundage R C, Balfour H H, Fletcher C V
Department of Experimental and Clinical Pharmacology, University of Minnesota Academic Health Sciences Center, Minneapolis, USA.
Pharmacotherapy. 2000 Aug;20(8):917-22. doi: 10.1592/phco.20.11.917.35263.
To characterize the concentration-time profiles of zidovudine and zidovudine-glucuronide in semen and serum of men infected with the human immunodeficiency-1 virus (HIV-1).
Open-label observational study.
University-affiliated teaching hospital and research center.
Four asymptomatic HIV-1-infected men.
Zidovudine administration was followed by an 8-hour intensive pharmacokinetic study on day 1. Over the next 8 days, a dose administration and timed single-sample strategy was employed to determine serum and semen concentration time profiles simultaneously.
Zidovudine and zidovudine-glucuronide concentrations were uniformly higher in semen than in serum except at 1 hour after the dose. The median area under the curve ratio (semen AUC0-48:serum AUC0-infinity) was 3.31 for zidovudine and 15.04 for zidovudine-glucuronide.
Zidovudine and zidovudine-glucuronide reach high levels in seminal plasma relative to serum. The virologic, pharmacodynamic, and public health implications of distribution to this compartment require further study.
描述齐多夫定及其葡糖醛酸结合物在感染人类免疫缺陷病毒1型（HIV-1）男性精液和血清中的浓度-时间曲线。
开放标签观察性研究。
大学附属医院及研究中心。
4名无症状HIV-1感染男性。
第1天给予齐多夫定后进行8小时强化药代动力学研究。在接下来的8天里，采用给药和定时单样本策略同时测定血清和精液浓度-时间曲线。
除给药后1小时外，精液中齐多夫定及其葡糖醛酸结合物的浓度均高于血清。齐多夫定的曲线下面积中位数比值（精液AUC0-48:血清AUC0-∞）为3.31，齐多夫定葡糖醛酸结合物为15.04。
相对于血清，齐多夫定及其葡糖醛酸结合物在精浆中达到较高水平。该成分分布对病毒学、药效学及公共卫生的影响需要进一步研究。
