RT Journal Article
SR Electronic
T1 The pharmacokinetics of 1,3-di(4-imidazolino-2-methoxyphenoxy) propane.lactate (DMP.lactate), a new agent against opportunistic infections, in male beagle dogs.
JF Drug Metabolism and Disposition
JO Drug Metab Dispos
FD American Society for Pharmacology and Experimental Therapeutics
SP 233
OP 236
VO 22
IS 2
A1 I Bekersky
A1 R J Puhl
A1 G Hanson
A1 S Mong
YR 1994
UL http://dmd.aspetjournals.org/content/22/2/233.abstract
AB The pharmacokinetics and oral bioavailability of 1,3-di(4-imidazolino-2-methoxyphenoxy) propane.lactate (DMP) was determined in male dogs following iv and po administrations of DMP.lactate containing trace amounts of [14C]DMP.HCl. Following the iv administration of [14C]DMP.lactate (2.5 mg/kg), plasma concentrations of DMP declined in a biexponential manner and were measurable to 48 hr. The terminal elimination half-life was 37.7 hr. The mean AUC0-infinity of DMP was 1.58 micrograms.hr/ml. The volume of distribution was 89 liters/kg and the body clearance was 27 ml/min/kg. The disposition of total radioactivity was similar to that of DMP. Approximately 14% of the dose was eliminated in urine as DMP or total radioactivity. Renal clearance was 10% of the body clearance. Following the po administration of [14C]DMP.lactate (14 mg/kg) the mean Cmax of total radioactivity and DMP was 0.20 and 0.17 micrograms/ml, respectively. The respective mean AUC0-T was 0.37 and 0.21 micrograms.hr/ml. The mean oral bioavailability based on DMP plasma concentrations was 2.4%. The mean Cmax of DMP following a 100 mg/kg po dose of DMP.lactate was 14 micrograms/ml and the AUC0-T was 1.87 micrograms.ml/hr; the bioavailability was 3.2%. Approximately 1% of the orally administered dose was eliminated in urine as DMP.