Title: Disposition, bioavailability, and serum protein binding of pentachlorophenol in the B6C3F1 mouse.

Authors: Reigner, B G; Rigod, J F; Tozer, T N

Published In Pharm Res, (1992 Aug)

Abstract: The toxicokinetics of pentachlorophenol (PCP) were studied in B6C3F1 mice, a strain in which PCP was previously found to be carcinogenic. In a crossover design, doses of 15 mg/kg were given intravenously (bolus) and orally (gastric intubation) to six animals. Concentrations of PCP in blood, urine, and feces were measured by capillary gas chromatography with electron-capture detection. After intravenous administration, the values of clearance and volume of distribution were 0.057 +/- 0.007 L/hr/kg and 0.43 +/- 0.06 L/kg, respectively. These two parameters exhibited low intermouse variability (coefficients of variation less than 14%). The elimination half-life was 5.2 +/- 0.6 hr. After oral administration, the PCP peak plasma concentration (28 +/- 7 micrograms/ml) occurred at 1.5 +/- 0.5 hr and absorption was complete (bioavailability = 1.06 +/- 0.09). The elimination half-life was 5.8 +/- 0.6 hr. Only 8% of the PCP dose was excreted unchanged by the kidney. PCP was primarily recovered in urine as conjugates. A portion of the dose was recovered in urine as the mutagen, tetrachlorohydroquinone (5%) (TCHQ), and its conjugates (15%). For both PCP and TCHQ, sulfates accounted for 90% or more of the total conjugates (glucuronides and sulfates).

PubMed ID: 1409377

MeSH Terms: Administration, Oral; Animals; Blood Proteins/metabolism*; Data Interpretation, Statistical; Half-Life; Hydroquinones/urine; Injections, Intravenous; Male; Mice; Pentachlorophenol/administration & dosage; Pentachlorophenol/metabolism; Pentachlorophenol/pharmacokinetics*; Pentachlorophenol/toxicity; Protein Binding