安普索提高泰能对肺组织穿透作用的研究

STUDY OF INFLUENCE OF AMBROHEXEL ON THE ACTION OF IMIPENEM/CILASTATIN TO PENETRATE LUNG TISSUE

采用双盲对照法将１６例行纤支镜检查的志愿患者随机分为两组：一组单用泰能５０ｍｇ静滴，ｂｉｄ；另一组泰能５００ｍｇ静滴，ｂｉｄ，合用安普索６０ｍｇ，ｐｏ，ｔｉｄ。连续３ｄ后测定支气管灌洗（ＢＡＬ）液及同期血浆中泰能浓度。结果表明：单用泰能组输完泰能１．５ｈ后ＢＡＬ液中泰能浓度为１．３１±０．１６ｍｇ／Ｌ或６．６２±１．４９ｍｇ／ｇ，且与血浆泰能浓度呈显著正相关（Ｐ＜０．０１），提示泰能对肺组织具有良好的渗透作用，其渗透是一个正相扩散的过程。泰能合用安普索组输完泰能１．５ｈ后ＢＡＬ液中泰能浓度显著高于单用泰能组（Ｐ＜０．０１），其浓度为２．１１±０．２９ｍｇ／Ｌ或１１．６７±２．３９ｍｇ／ｇ，与血浆泰能浓度无明显相关（Ｐ＞０．０５），提示安普索能增强泰能对肺组织的穿透能力。同时证明纤支镜肺泡灌洗是研究药物肺内动力学的好方法。

The double blind placebo controlled study was conducted on 16 patients.They were randomized and equally divided to receive imipenem/cilastatin 500 mg bid by infusion and imipenem/cilastatin 500 mg bid by infusion+ambrohexel 60 mg tid by oral,for a period of 3 days in both groups.Results showed that the BAL fluid concentration of imipenem/cilastatin in single drug group was 1.31±0.16 mg/L(or 6.62±1.49 mg/g).The plasma and BAL fluid drug concentrations are positively corelated;and that the imipenem/cilastatin concentration in BAL fluid in combination drug group was 2.11±0.29 mg/L(or 11.67±2.39 mg/g)that was significantly higher than that in single drug group(P<0.01)but not corelated with plasma concentration(P>0.05).From this study it is suggested that the action of imipenem/cilastatin to penetrate lung tissue can be increased by ambrohexel.