鹽酸莫西沙星的全身和肺部藥代動力學比較研究_《中國呼吸與危重監護雜志》

作者：

王小均 ,  劉春濤 , 余勤 , 黃琳 , 馮萍 , 梁茂植 , 向瑾

四川大學華西醫院臨床藥理研究所（四川成都 610041）;

關鍵詞：

鹽酸莫西沙星肺部感染藥代動力學

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目的比較鹽酸莫西沙星全身和肺部藥代動力學特點，探討藥物濃度監測和療效評估的實用性技術，以指導臨床合理進行抗感染治療。方法選擇10例肺部感染（慢性阻塞性肺疾病急性加重6例、社區獲得性肺炎4例）患者，服用400 mg單劑量的鹽酸莫西沙星。于服藥前及服藥后1、2、3、4、8及24 h采集血液，于服藥前及服藥后1、2、4、8、20及24 h采集痰液，用高效液相色譜法測定血清和痰液中鹽酸莫西沙星達峰濃度（Cmax）及24 h藥時曲線下面積（AUC0-24 h）。結果單次口服鹽酸莫西沙星后約2 h在血中達峰濃度，Cmax為（5.95±1.35）mg/L，AUC0-24 h為（58.72±8.11）mg·h-1·L-1；約3 h在痰液中達峰濃度，Cmax為（16.18±6.47）mg/L，藥時曲線下面積（AUC0-24 h）為（138.04±78.29）mg·h-1·L-1。口服鹽酸莫西沙星后痰中Cmax和AUC0-24 h顯著高于血清Cmax和AUC0-24 h（P均 lt;0.05）。結論單次口服鹽酸莫西沙星后，藥物迅速分布于肺部，在24 h內肺部濃度高于血清濃度1倍以上。測定痰液藥物濃度可反映肺部藥代動力學特征。

引用本文： 王小均,劉春濤,余勤,黃琳,馮萍,梁茂植,向瑾. 鹽酸莫西沙星的全身和肺部藥代動力學比較研究. 中國呼吸與危重監護雜志, 2008, 08(2): 88-92. doi: 復制

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2.	Breilh D,Jougon J,Djabarouti S,et al.Diffusion of oral and intravenous 400 mg once-daily moxifloxacin into lung tissue at pharmacokinetic steady-state.J Chemother,2003,15:558-562.
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6.	Lemoine T,Breilh D,Ducint D,et al.Determination of moxifloxacin (BAY 12-8039) in plasma and lung tissue by high-performance liquid chromatography with ultraviolet detection using a fully automated extraction method with a new polymeric cartridge.J Chromatogr B Biomed Sci Appl,2000,742:247-254.
7.	Ehrlich M,Daschner FD,Kümmerer K.Rapid antibiotic drug monitoring: meropenem and ceftazidime determination in serum and bronchial secretions by high-performance liquid chromatography-integrated sample preparation.J Chromatogr B Biomed Sci Appl,2001,751:357-363.
8.	Woodcock JM，Andrews JM，Boswell FJ，et al.In-vitro activity of BAY 12-8039，a new fluoroquinolone. Antimicrob Agents Chemother，1997，41:101-106.
9.	John TS,Marilyn W,John L,et al.Pharmacokinetics of a Once-Daily Oral Dose of Moxifloxacin (Bay 12-8039),a New Enantiomerically Pure 8-Methoxy quinolone.Antimicrobial Agents and Chemotherapy,1999,43:2793–2797.
10.	Leone M, Albanèse J,Sampol-Manos E,et al.Moxifloxacin penetration in bronchial secretions of mechanically ventilated patients with pneumonia.Antimicrob Agents Chemother,2004,48:638-640.
11.	Soman A,Honeybourne D,Andrews J,et al.Concentrations of moxifloxacin in serum and pulmonary compartments following a single 400 mg oral dose in patients undergoing fibre-optic bronchoscopy.J Antimicrob Chemother,1999,44:835-838.
12.	Zhanel GG,Noreddin AM.Pharmacokinetics and pharmacodynamics of the new fluoroquinolones: focus on respiratory infections.Curr Opin Pharmacol,2001,1:459-463.
13.	Wise R.A Review of the Clinical Pharmacology of Moxifloxacin, a New 8-Methoxyquinolone, and its Potential Relation to Therapeutic Efficacy.Clinical Drug Investigation,1999,17:365-387.
14.	Aminimanizani A,Beringer P,Jelliffe R. Comparative pharmacokinetics and pharmacodynamics of the newer fluoroquinolone antibacterials.Clin Pharmacokinet,2001,40:169-187.
15.	Tsang KW,Roberts P,Read RC,et al.The concentrations of clarithromycin and its 14-hydroxy metabolite in sputum of patients with bronchiectasis following single dose oral administration.J Antimicrob Chemother,1994,33:289-297.
16.	Baldwin DR,Honeybourne D,Wise R.Pulmonary disposition of antimicrobial agents: methodological considerations.Antimicrob Agents Chemother,1992,36:1171-1175.

1. Mouton JW,Dudley MN,Cars O,et al.Standardization of pharmacokinetic/pharmacodynamic (PK/PD) terminology for anti-infective drugs: an update.J Antimicrob Chemother,2005,55:601-607.
2. Breilh D,Jougon J,Djabarouti S,et al.Diffusion of oral and intravenous 400 mg once-daily moxifloxacin into lung tissue at pharmacokinetic steady-state.J Chemother,2003,15:558-562.
3. Krasemann C,Meyer J,Tillotson G,et al.Evaluation of the clinical microbiology profile of moxifloxacin.Clin Infect Dis,2001,32::S51-63.
4. Cazzola M,Matera MG, Donnarumma G,et al.Pharmacodynamics of levofloxacin in patients with acute exacerbation of chronic bronchitis.Chest,2005,128:2093-2098.
5. Tatar Ulu S.High-performance liquid chromatography assay for moxifloxacin: pharmacokinetics in human plasma.J Pharm Biomed Anal,2007,43:320-324.
6. Lemoine T,Breilh D,Ducint D,et al.Determination of moxifloxacin (BAY 12-8039) in plasma and lung tissue by high-performance liquid chromatography with ultraviolet detection using a fully automated extraction method with a new polymeric cartridge.J Chromatogr B Biomed Sci Appl,2000,742:247-254.
7. Ehrlich M,Daschner FD,Kümmerer K.Rapid antibiotic drug monitoring: meropenem and ceftazidime determination in serum and bronchial secretions by high-performance liquid chromatography-integrated sample preparation.J Chromatogr B Biomed Sci Appl,2001,751:357-363.
8. Woodcock JM，Andrews JM，Boswell FJ，et al.In-vitro activity of BAY 12-8039，a new fluoroquinolone. Antimicrob Agents Chemother，1997，41:101-106.
9. John TS,Marilyn W,John L,et al.Pharmacokinetics of a Once-Daily Oral Dose of Moxifloxacin (Bay 12-8039),a New Enantiomerically Pure 8-Methoxy quinolone.Antimicrobial Agents and Chemotherapy,1999,43:2793–2797.
10. Leone M, Albanèse J,Sampol-Manos E,et al.Moxifloxacin penetration in bronchial secretions of mechanically ventilated patients with pneumonia.Antimicrob Agents Chemother,2004,48:638-640.
11. Soman A,Honeybourne D,Andrews J,et al.Concentrations of moxifloxacin in serum and pulmonary compartments following a single 400 mg oral dose in patients undergoing fibre-optic bronchoscopy.J Antimicrob Chemother,1999,44:835-838.
12. Zhanel GG,Noreddin AM.Pharmacokinetics and pharmacodynamics of the new fluoroquinolones: focus on respiratory infections.Curr Opin Pharmacol,2001,1:459-463.
13. Wise R.A Review of the Clinical Pharmacology of Moxifloxacin, a New 8-Methoxyquinolone, and its Potential Relation to Therapeutic Efficacy.Clinical Drug Investigation,1999,17:365-387.
14. Aminimanizani A,Beringer P,Jelliffe R. Comparative pharmacokinetics and pharmacodynamics of the newer fluoroquinolone antibacterials.Clin Pharmacokinet,2001,40:169-187.
15. Tsang KW,Roberts P,Read RC,et al.The concentrations of clarithromycin and its 14-hydroxy metabolite in sputum of patients with bronchiectasis following single dose oral administration.J Antimicrob Chemother,1994,33:289-297.
16. Baldwin DR,Honeybourne D,Wise R.Pulmonary disposition of antimicrobial agents: methodological considerations.Antimicrob Agents Chemother,1992,36:1171-1175.

《中國呼吸與危重監護雜志》

鹽酸莫西沙星的全身和肺部藥代動力學比較研究

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《中國呼吸與危重監護雜志》

鹽酸莫西沙星的全身和肺部藥代動力學比較研究

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