Abstract |
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.
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Authors | I Bekersky, R J Puhl, G Hanson, S Mong |
Journal | Drug metabolism and disposition: the biological fate of chemicals
(Drug Metab Dispos)
1994 Mar-Apr
Vol. 22
Issue 2
Pg. 233-6
ISSN: 0090-9556 [Print] United States |
PMID | 8013279
(Publication Type: Journal Article)
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Chemical References |
- Anti-Infective Agents
- 1,3-di-(4-imidazolino-2-methoxyphenoxy)propane
- Pentamidine
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Topics |
- Administration, Oral
- Animals
- Anti-Infective Agents
(blood, pharmacokinetics, urine)
- Biological Availability
- Chromatography, High Pressure Liquid
- Dogs
- Half-Life
- Injections, Intravenous
- Male
- Opportunistic Infections
(drug therapy)
- Pentamidine
(analogs & derivatives, blood, pharmacokinetics, urine)
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