中国男性健康志愿者单剂量用盐酸多西环素的药代动力学研究  

Pharmacokinetics of a single dose of Doxycycline hydrochloride for injection in healthy Chinese male

作　　者：李佩琼[1] 王九辉[1] 曾祥周[1] 王小蒙[1] 邝少轶[1] 云天佑[1] 刘军保[1] 

机构地区：[1]海南医学院药理学教研室,海南海口571101

出　　处：《海南医学院学报》2009年第9期1044-1047,共4页Journal of Hainan Medical University

基　　金：海南医学院科研基金资助学报项目(0020090137)~~

摘　　要：目的:研究单剂量静脉滴注盐酸多西环素在中国男性健康志愿者体内的药代动力学特征。方法:选择100mg和200mg2个剂量,11名健康男性受试者随机分为两组,采用单剂量2周期交叉给药,以HPLC法对血、尿标本中的多西环素浓度进行检测,以DAS软件进行药代动力学参数计算。结果:静脉滴注用盐酸多西环素的血药浓度-时间曲线符合二房室模型,100mg和200mg剂量组的Cmax分别为(1.80±0.36)mg/L和(3.63±0.59)mg/L,AUC0→∝分别为(21.30±4.86)mg/(h.L)和(44.18±10.63)mg/(h.L),t1/2分别为(17.68±3.51)h和(17.36±3.11)h、Vd分别为(120.13±20.67)L和(114.83±18.37)L,两剂量组96h尿药排泄率分别为(26.7±11.5)%和(22.8±10.6)%。结论:本研究结果提供了单剂量静脉滴注盐酸多西环素在中国健康男性受试者中的药代动力学参数和资料,为制定临床给药方案提供依据。Objective：To investigate the pharmacokinetics of a single dose of intravenous doxycycline drip hydrochloride in healthy Chinese male. Methods： Eleven healthy male Chinese volunteers were recruited and were randomly divided into two groups （Group A and B）. Doses of 100 mg and 200 mg doxycycline hydrochloride were prepared. A single dose of 100 mg and 200 mg doxycycline hydrochloride for injection was used intravenously respectively in two cycles crossly, the concentrations of drug in serum and urine were determined by HPLC, and the pharmacokinetics parameters were calculated by DAS software. Results： The concentration-time curves of 100 mg and 200 mg doxycycline hydrochloride for injection were consistent with two compartments model. The main pharmacokinetic parameters of 100 mg and 200 mg dose were as follow： Cmax were （1.80 ±0.36）mg/L and （3.63 0.59） mg/L, respectively; AUC0→∝were （21.30 ±4.86） mg/（ h .L） and （44.18 ±10.63） mg/（ h · L）, respectively ; tl/2 were （ 17.68 ±3.51 ） h and （ 17.36 ± 3.11 ） h, respectively ; Vd were （ 120.13 ±20.67 ） L and （114.83 ±18.37）L, respectively; the cumulative excretion rate of doxycycline in urine in 96h were （26.7 ± 11. 5 ）% and （22.8 ±10.6）%, respectively. Conclusion： Pharmacokinetics parameters of a single dose of doxyeycline hydroehloride for injection in healthy Chinese male acquired in this study may provide reference for clinical use of the drug.

关 键 词：盐酸多西环素 药代动力学 HPLC 男性 

分 类 号：R978.14[医药卫生—药品] R969.1[医药卫生—药学]