PHARMACOKINETICS OF CIPROFLOXACIN .1. COMMUNICATION - ABSORPTION, CONCENTRATIONS IN PLASMA, METABOLISM AND EXCRETION AFTER A SINGLE ADMINISTRATION OF [C-14] CIPROFLOXACIN IN ALBINO-RATS AND RHESUS-MONKEYS

  • 1 January 1986
    • journal article
    • research article
    • Vol. 36-2  (10) , 1496-1502
Abstract
The absorption, disposition, metabolism and excretion of 1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-[U-14C]piperazinyl)-3-quinoline carboxylic acid (ciprofloxacin, Bay o 9867; designated tradename: Ciprobay) were studied following a single intraduodenal (rat), oral and intravenous (rat, monkey) administration, respectively, in the dose range 5 to 30 mg/kg body weight. Ciprofloxacin was absorbed partially (30 to 40%) in both species. Peak plasma concentrations of radioactivity were measured approximately 1 h (rat) or 2 h (monkey) after oral dosing. Terminal half-lives ranging from 26 to 44 h were determined for the elimination of radioactivity from the plasma (observation time up to 48 h after dosing). Nearly identical concentrations of the unchanged drug and total radioactivity were found during the first 7 or 8 h for the monkey after intravenous injection and for the rat also after oral administration, respectively. After reaching maximum concentration of 0.25 .mu.g/ml after administration of 5 mg/kg to rats and 0.88 .mu.g/ml after dosing with 30 mg/kg to a rhesus monkey, the unchanged drug was eliminated from plasma corresponding to half-lives ranging from 3 h (rat) and 4.4 h (monkey). The radioactivity was rapidly and completely excreted in both species. After intravenous administration about 51% (rat) and and 61% (monkey), respectively, was excreted via the kidney. After oral dosing renal excretion amounted to 6-14% rate and 30% (monkey), respectively. Maximum residues in the body (exclusive gastrointestinal tract) of 1% of dose occurred in both species. In urine and feces of rats predominantly the unchanged drug and a conjugate were detected. The monkey urine and feces contained predominantly the unchanged drug. Two metabolites occurring in small amounts were identified and characterized, respectively. After intraduodenal administration to rats 17% of the dose was excreted with the bile, a small amount of it was reabsorbed. After oral dosage ciprofloxacin was secreted into the milk of lactating rats predominantly as the unchanged drug. Binding of [14C]ciprofloxacin to plasma proteins was 33% (rat) and 23% (monkey), respectively.

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