The pharmacokinetics of diethanolamine in Sprague–Dawley rats following intravenous administration

• Published in: Food and chemical toxicology Vol. 39; no. 9; pp. 931 - 939
• Main Authors: Mendrala, A.L, Waechter, J.M, Bormett, G.A, Bartels, M.J, Stott, W.T
• Format: Journal Article
• Language: English
• Published: Oxford Elsevier Ltd 01.09.2001; New York, NY Elsevier Science
• Subjects: Animals; Biological and medical sciences; Carbon Isotopes - urine; Chemical and industrial products toxicology. Toxic occupational diseases; Diethanolamine; Dose-Response Relationship, Drug; Erythrocytes - metabolism; Ethanolamines - administration & dosage; Ethanolamines - pharmacokinetics; Ethanolamines - toxicity; Female; Gas Chromatography-Mass Spectrometry; Injections, Intravenous; Kidney - metabolism; Liver - metabolism; Medical sciences; Models, Biological; Pharmacokinetics; Random Allocation; Rat; Rats; Rats, Sprague-Dawley; Tissue Distribution; Toxicology; Various organic compounds; DEA; RBC; Rat; ADME; Diethanolamine; Pharmacokinetics; LSC; PFBCl; GC/MS; AUC; MSD; Toxicokinetics; Vertebrata; Mammalia; Intravenous administration; Animal; Rodentia
• ISSN: 0278-6915; 1873-6351
• DOI: 10.1016/S0278-6915(01)00036-9

In order to better understand the potential toxicity of diethanolamine (DEA) and preparatory to physiologically-based pharmacokinetic model development, the pharmacokinetics of DEA at high and low internal dose through 96-h post-dosing were determined in female Sprague–Dawley rats administered 10 or 100 mg/kg uniformly labeled 14C-DEA via intravenous injection. Clearance of DEA from blood was calculated to be approximately 84 ml/h/kg at the low dose, increasing to approximately 242 ml/h/kg at the high dose. The primary route of excretion of administered radioactivity, approximately 25–36%, was via the urine as parent compound. A majority of the administered radioactivity was recovered in the tissues of treated rats, especially in the liver and kidneys, suggesting a propensity of DEA or its metabolites for bioaccumulation. An accumulation of radioactivity also occurred gradually in the red blood cells from about 6–96 h post-dosing. Some evidence of dose dependency in the fate of iv-administered DEA was observed, suggesting that saturation of the bioaccumulation process(es) occurred at a dose level of 100 mg/kg.