Nahata M C, Brady M T
College of Pharmacy, Ohio State University, Wexner Institute for Pediatric Research, Children's Hospital, Columbus 43210, USA.
Eur J Clin Pharmacol. 1995;48(3-4):291-3. doi: 10.1007/BF00198314.
The objective of this study was to determine the pharmacokinetics of fluconazole after oral administration in children with human immunodeficiency virus (HIV) infection. After an overnight fast, a single dose of either 2 mg.kg-1 or 8 mg.kg-1 was administered in a suspension; five children received 2 mg.kg-1 and four 8 mg.kg-1 (ages 5-13 years). Blood samples were collected at various times on day 1, and once daily on days 2-7 after the dose. Fluconazole serum concentrations were measured by gas chromatography. At the dose of 2 mg.kg-1, the Cmax, AUC (0-infinity), and t1/2 ranged from 2.3-4.4 micrograms.ml-1, 84.9-136 micrograms.h.ml-1, and 19.8-34.8 h, respectively. At the dose of 8 mg.kg-1 the Cmax, AUC (0-infinity), and t1/2 ranged from 5.4-12.1 micrograms.ml-1, 330-684 micrograms h.ml-1, and 25.6-42.3 h, respectively. When compared with published data in healthy adults, fluconazole achieved similar serum concentrations in the present group of children, indicating a nearly complete degree of absorption.
本研究的目的是确定氟康唑在人类免疫缺陷病毒(HIV)感染儿童口服给药后的药代动力学。禁食过夜后,以混悬液形式给予单剂量2mg/kg或8mg/kg;5名儿童接受2mg/kg,4名儿童接受8mg/kg(年龄5 - 13岁)。在给药后第1天的不同时间以及第2 - 7天每天采集一次血样。通过气相色谱法测定氟康唑血清浓度。在2mg/kg剂量下,Cmax、AUC(0 - ∞)和t1/2分别为2.3 - 4.4μg/ml、84.9 - 136μg·h/ml和19.8 - 34.8小时。在8mg/kg剂量下,Cmax、AUC(0 - ∞)和t1/2分别为5.4 - 12.1μg/ml、330 - 684μg·h/ml和25.6 - 42.3小时。与健康成人已发表的数据相比,氟康唑在本组儿童中达到了相似的血清浓度,表明吸收程度几乎完全。