1984 Volume 32 Issue Supplement1 Pages 225-238
Bacteriological and clinical studies on DL-8280, a new synthetic antimicrobial agent of benzoxazine derivative, were performed and the following results were obtained.
MICs of DL-8280 against clinically isolated strains of E. coli, C. freundii, S. marcescens, P. aeruginosa were almost the same as those of NFLX and were significantly superior to those of NA, PPA and MLX.
DL-8280 was orally administered to healthy adult male volunteers at a dose of 200 mg. The maximum serum concentration of 2.83 μg/ml was obtained at 1 hour after administration. The half life of serum concentration was 3.13 hours. The maximum serum concentration of DL-8280 was higher than that of NFLX at the same dose level and bioavailability of DL-8280 was superior to that of NFLX. Serum concentration increased dose dependently. Urinary recovery of DL-8280 during 24 hours after administration was between 77.2 and 92.2%. In comparison with this high recovery rate of DL-8280, that of NFLX was only 35.4% during 24 hours after administration.
DL-8280 was administered to 21 patients with various infections in the field of internal medicine at daily doses of 150-600 mg for 5-21 days. The clinical result was “excellent” in 3, “good” in 16, “fair” in 2 and the efficacy rate was 90.5%. Twelve out of 13 bacterial strains were eradicated and the eradication rate was 92.3%.
Slight increase in serum alkaline-phosphatase was noted in one patient.
From these results, it is concluded that DL-8280 is the extremely useful synthetic antimicrobial agent for the treatment of the infections in the field of internal medicine.
