摘要
目的研究莫西沙星在人体肺内药动学。方法20例行支气管镜检查的病人,术前给予莫西沙星400mg口服,分为4组,分别在2、4、12、24h采集支气管肺泡灌洗液和血样,通过反相高效液相色谱分析以及尿素稀释法,得出血浆、气管上皮细胞衬液(ELF)、肺泡巨噬细胞(AM)中药物浓度及肺内药动学主要参数。结果莫西沙星在血浆、ELF、AM中的ρmax分别为(2.1±s0.8)、(51±45)、(603±425)mg·L-1,在血浆、ELF、AM中AUC比值为1∶20∶235。结论支气管肺泡灌洗结合反相高效液相色谱法研究药物肺内药动学是一种方便、安全、可靠的研究方法。给药24h内,莫西沙星在人体肺组织内的药物浓度可达血浆数十倍甚至数百倍。
AIM To investigate the intrapulmonary pharmacokinetics of moxifloxacin in human. METHODS Twenty patients underwent bronchoscopy at different timed intervals （2, 4, 12, and 24 h） after drug administration and bronchoalveolar lavage （BAL） samples were taken. Drug concentrations in plasma, BAL fluid, and alveolar macrophages （AM） were determined by high-pressure liquid chromatography. The concentrations in epithelial lining fluid （ELF） were calculated by the urea diffusion method and the pharma- cokinetic parameters in plasma, ELF, and AM were compared. RESULTS The maximal concentrations in plasma, ELF, and AM were （2.1 ± s 0.8） , （51 ± 45） , （603 ± 425） mg·L^-1. The ratio of drug AUC in plsasma, ELF, and AM,were 1 ： 20 ： 235. CONCLUSION BAL associated with HPLC is an efficient and safe method to study the intrapulmonary pharmacokineties of moxifloxaein in human. During the period of 24 h after drug administration, moxifloxacin achieved much more higher concentrations in ELF and AM than those in plasma.
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2009年第1期11-14,共4页
Chinese Journal of New Drugs and Clinical Remedies
关键词
支气管肺泡灌洗
色谱法
高压液相
莫西沙星
巨噬细胞
肺泡
上皮细胞衬液
bronchoalveolar lavage
chromatography, high-pressure liquid
moxifloxacin
macrophages, alveolar
epithelial lining fluid
