Abstract | PURPOSE: METHOD: The aerosol formulation (0.2 mg/kg) was administered to rat lungs using a Liquid MicroSprayer. RESULTS AND DISCUSSION: The time courses of the concentration of TEL in lung epithelial lining fluid (ELF) and alveolar macrophages (AMs) following administration of an aerosol formulation to rat lungs were markedly higher than that following the administration of an oral formulation (50 mg/kg). The time course of the concentrations of TEL in plasma following administration of the aerosol formulation was markedly lower than that in ELF and AMs. These results indicate that the aerosol formulation is more effective in delivering TEL to ELF and AMs, compared to the oral formulation, despite a low dose and it avoids distribution of TEL to the blood. In addition, the antibacterial effects of TEL in ELF and AMs following administration of the aerosol formulation were estimated by pharmacokinetics/pharmacodynamics analysis. The concentrations of TEL in ELF and the AMs time curve/minimum inhibitory concentration of TEL ratio were markedly higher than the effective values. CONCLUSION:
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Authors | Kohei Togami, Sumio Chono, Toshinobu Seki, Kazuhiro Morimoto |
Journal | Drug development and industrial pharmacy
(Drug Dev Ind Pharm)
Vol. 36
Issue 7
Pg. 861-6
(Jul 2010)
ISSN: 1520-5762 [Electronic] England |
PMID | 20515406
(Publication Type: Comparative Study, Journal Article, Research Support, Non-U.S. Gov't)
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Chemical References |
- Anti-Bacterial Agents
- Ketolides
- telithromycin
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Topics |
- Administration, Inhalation
- Animals
- Anti-Bacterial Agents
(administration & dosage, pharmacokinetics, pharmacology)
- Epithelial Cells
(metabolism)
- Extracellular Fluid
(metabolism)
- Haemophilus influenzae
(drug effects)
- Ketolides
(administration & dosage, pharmacokinetics, pharmacology)
- Lung
(metabolism)
- Macrophages, Alveolar
(metabolism)
- Rats
- Rats, Sprague-Dawley
- Respiratory Tract Infections
(drug therapy)
- Streptococcus pneumoniae
(drug effects)
- Technology, Pharmaceutical
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