Penetration of clofoctol into human lung.
The disposition of clofoctol was determined in plasma and lung tissue from 34 patients undergoing pulmonary resection for lung cancer. Clofoctol 1.5 g was given as a rectal suppository; samples of plasma and pulmonary tissue were collected between 15 and 270 min post-dose. Plasma and lung peak concentrations of the drug were 38.07 +/- 0.73 mg/l and 93.13 +/- 6.68 mg/kg at 30 and 90 min, respectively. Mean values for areas under the concentration-time curve and half-life for plasma and lung were 80.91 mg/l/h, 229.65 mg/h, and 1.18 h and 1.21 h, respectively. Tissue to plasma ratios were 0.85 +/- 0.06, 3.82 +/- 0.21 and 6.19 +/- 0.63 at 30, 90 and 180 min post-dose, respectively. Clofoctol is well absorbed from the rectum and accumulates in lung tissue. This may explain its efficacy in bacterial respiratory infections.
D000368:Aged; D002722:Chlorobenzenes; D003408:Cresols / Q000097:blood / Q000378:metabolism; D005260:Female; D006207:Half-Life; D006801:Humans; D007700:Kinetics; D008168:Lung / Q000378:metabolism*; D008175:Lung Neoplasms / Q000378:metabolism; D008297:Male; D014018:Tissue Distribution
D002722:Chlorobenzenes; D003408:Cresols; C018874:clofoctol