THE PHARMACOKINETIC STUDIES ON ASTROMICIN IN RATS: INTRAMUSCULAR, INTRAVENOUS OR DRIP INTRAVENOUS ADMINISTRATION

• Published in: Japanese journal of antibiotics 1984/07/25, Vol.37(7), pp.1263-1271
• Main Authors: KURIMOTO, TSUKASA, KOBAYASHI, HIROYUKI, INOUE, AKINOBU, OKACHI, RYO
• Format: Article
• Language: Japanese
• Subjects: Aminoglycosides - administration & dosage; Aminoglycosides - metabolism; Animals; Anti-Bacterial Agents - administration & dosage; Anti-Bacterial Agents - metabolism; Infusions, Parenteral; Injections, Intramuscular; Injections, Intravenous; Kidney - metabolism; Kinetics; Male; Rats
• ISSN: 0368-2781; 2186-5477
• DOI: 10.11553/antibiotics1968b.37.1263

Absorption, tissue distribution and excretion of astromicin (ASTM) were studied in rats after intramuscular (i. m.), intravenous (i. v.) or drip intravenous (d. i. v.; for 15, 30min. or 60min.) administration at a dose of 20mg/kg. The pharmacokinetic studies of ASTM were carried out using one-compartment open model (i. m.) or two-compartment open model (i. v. and d. i. v.). 1. The peak values of ASTM observed in serum were 48.6μg/ml (i. m.), 255.3μg/ml (i. v.), 57.5μg/ml (15min. d. i. v.), 45.9μg/ml (30min. d. i. v.) and 39.1μg/ml (60min. d. i. v.). 2. The pharmacokinetic parameters of ASTM after 15min. d. i. v. administration were calculated as follows: Kel 0.110min-1 T1/2 21.4min., Vdβ 0.310L/kg, Tmax. 15.0min., Cmax 58.6μg/ml AUC 1,991μg·min/ml. 3. ASTM was rapidly distributed into the kidneys and lungs. The peak values of ASTM in the kidneys were 156.8μg/g (i. m.), 185.2μg/g (i. v.), 132.9μg/g (15min. d. i. v.), 135.3μg/g (30min. d. i. v.) and 117.3μg/g (60min. d. i. v.). 4. Urinary recovery rates of ASTM amounted to 85.5% (i. m.), 99.5% (i. v.) or 87.9% (30min. d. i. v.). 5. After i. m. or 30min. d. i. v. administration of ASTM, no active metabolite was found in urine of rats.