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(jiān)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(qū)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(jié)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(jié)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(nèi)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(jiān)護雜志, 2008, 08(2): 88-92. doi: 復制
| 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. |
- 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.