摘要
目的:了解中国健康人静脉滴注和口服氟康唑的药物动力学。方法:9例健康志愿者随机分为2组,静脉和口服交叉给予单剂量氟康唑300mg,测定血、尿和唾液中药物浓度。结果:按非室模型计算针、片剂的药物动力学参数分别为:AUC=265±93和258±79μg·h/mL;MRT=43±25和69±66h;T12β=32±20和32±29h;Cl=1.3±0.4和1.2±0.4L/h;Vss=61±58和36±12L及AVE=3.7±1.3和3.5±1.1mg/L。结论:氟康唑的生物利用度为97%,具有吸收好。
AIM: To help deciding fluconazole administration schedule in Chinese. METHODS: Chinese healthy volunteers (M 5, F 4, age 36±s 9 a) received iv drip and po 300 mg fluconazole in a crossover design. Drug concentrations in plasma and saliva were assayed by high pressure liquid chromatography at 0.25, 0.5, 1, 2, 6, 12, 24, 48, 72 h. The pharmacokinetic parameters were calculated with a PKIA program by computer. RESULTS: The time course of plasma concentrations conformed to a noncompartment model. The pharmacokinetic parameters of po and iv drip were as follows: AUC=258±79 and 265±93 μg·h/mL, MRT=69±66 and 43±25 h, T 12β =32±29 and 32±20 h, Cl=1.2±0.4 and 1.3±0.4 L/h, V ss =36±12 and 61±58 L, AVE=3.5±1.1 and 3.7±1.3 mg/L, respectively. The bioavailability of fluconazole was 97%. CONCLUSION: Fluconazole was absorbed well, distributed widely in the body, and had a long half-life.
出处
《新药与临床》
CSCD
北大核心
1997年第2期69-71,共3页
关键词
氟康唑
高压液相色谱法
药物动力学
fluconazole
high pressure liquid chromatography
pharmacokinetics
clinical trials