Abstract
Serum levels, urinary excretions, and tissue distributions of 3', 4'-dideoxykanamycin B (DKB) in rabbits and dogs were examined by cylinder-plate diffusion assay with Bacillus subtilis ATCC 6633 as test organism, comparing with those of gentamicin (GM).
The results obtained in the present study were summarized as follows:
(1) A mean peak serum level of 57.2 mcg (base)/ml was obtained in rabbits given single 20mg (base)/kg dose of DKB intramuscularly. Biological half-life calculated at linear two-compartment model was 1.389 hr. and amount recovered from 8-hour urine was accounted for about 75.0% of given dose. These properties were nearly equal to those obtained after intravenous administration.
(2) When 20 mg (base)/kg dose of DKB was administered to dogs intramuscularly, a mean peak serum level of 58.6 mcg (base)/ml was obtained. Absorption rate constant (3.1149 hr-1), elimination constant (0.4692 hr-1), volume of distribution (0.264 L/kg) and biological half-life (1.477 hr) were calculated at same analysis. Urinary excretion of DKB was also studied in same dosage. Amount recovered from 10-hour urine was accounted for about 64.0% of dose given. In comparison with GM, no significant difference in these pharmacodynamic properties was found between these two antibiotics.
(3) Tissue levels after single 50 mg (base) /kg dose of DKB and GM given intramuscularly were estimated in rabbits. Level of DKB in lung was obtained about two times higher than GM, but in the others (brain, thymus, heart, liver, spleen, kidney, muscle and liquid humor), DKB showed a similar tendency to GM.
(4) From these data, it may be suggested that 3', 4'-dideoxykanamycin B has similar pharmacodynamic properties as gentamicin.
