PHARMACOKINETICS OF 7432-S, A NEW ORAL CEPHALOSPORIN, IN EXPERIMENTAL ANIMALS
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概要
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We administered 7432-S, a new oral cephalosporin antibiotics, to various experimental animals to compare its pharmacokinetics with those of cefaclor (CCL). After a 20mg/kg oral dose a 7432-S, the mean peak concentrations in plasma reached 16.7, 8.2, 1.6. 28.2 and 7.2μg/ml in mice, rats, rabbits, dogs and monkeys, respectively. The urinary recovery rates were 55.7, 41.8, 20.8, 62.5, and 20.2% of the administrated dose in abovementined species, respectively. 7432-S was well absorbed orally, and the areas under the plasma concentration time curves (AUCs) of 7432-S were higher than those of CCL in four animal species. The AUC ratio of 7432-S versus CCL was 1.9 (mice), 1.4 (rats), 1.5 (dogs) and 1.9 (monkeys), but less than 1/3 in rabbits. The urinary recovery percentages of 7432-S were also higher than those of CCL in the species other than rabbits and monkeys. In mice, rats and dogs, the plasma concentration of 7432-S reached a peak within 1 h after oral dosing, but at 3-4h in rabbits and monkeys. In mice and monkeys, its plasma levels or urinary recovery showed a linear increase in the amount absorbed with an increase in dose. 7432-S penetrated better than CCL in to the exudate of inflamed granuloma pouch in rats and into the cerebrospinal fluid in rat pups. In the tissue distribution in mice and rats, the ratio of the tissue levels versus the plasma concentrations kept constant, suggesting that there was no accumulation of antibiotics in specific tissues or organs. In the urine samples, 7432-S-trans was detected in trace in addition to 7432-S. As the antibacterial activity of the trans-isomer was 8 times lower than that of 7432-S, this trace metabolite made virtually no contribution to the activity in the body fluids.
- 公益社団法人 日本化学療法学会の論文
公益社団法人 日本化学療法学会 | 論文
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