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Pharmacokinetics and bioavailability of 2‐mercaptopropionylglycine administered intravenously and orally in dogs
Author(s) -
HOPPE A.,
DENNEBERG T.,
EMANUELSSON B.M.,
KÅGEDAL B.,
LINDGREN S.
Publication year - 1991
Publication title -
journal of veterinary pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.527
H-Index - 60
eISSN - 1365-2885
pISSN - 0140-7783
DOI - 10.1111/j.1365-2885.1991.tb00851.x
Subject(s) - pharmacokinetics , bioavailability , urine , oral administration , pharmacology , body weight , renal physiology , medicine , excretion , drug , distribution (mathematics) , chemistry , renal function , mathematical analysis , mathematics
The pharmacokinetic disposition of 2‐mercaptopropionylglycine (2‐MPG) given as a single intravenous injection and/or as a single oral dose was studied in 9 normal and 13 cystinuric dogs. After intravenous injection of approximately 10 or 20mg/kg body weight the pharmacokinetics were best described by a three‐exponential function. The first phase involved a distribution process apparently including establishment of drug‐plasma protein and drug‐tissue binding. The second phase involved rapid renal elimination and 60% of the drug was excreted within 3h of administration. There was also a slow terminal third phase with a long half‐life after both intravenous (t 1‐2 =23h) and oral (t 1/2 =22h) administration. No dose dependency was observed. A deep pool of reversibly tissue‐bound 2‐MPG was indicated by a V ss of 3.3±0.9l/kg body weight and the long terminal elimination phase. Total clearance was estimated as 4.1±0.9ml/min/kg body weight. 2‐MPG was eliminated mainly by renal excretion, but there was a difference in recovery of dose between normal and cystinuric dogs. During the first 24h after intravenous and oral administration, 69% and 54%, respectively, of the drug was recovered in the urine of normal dogs. The corresponding figures in cystinuric dogs were 44% and 29%, respectively. The absolute bioavailability (F AUC ) was 88±20% in normal dogs.