Interspecies scaling of excretory amounts using allometry – retrospective analysis with rifapentine, aztreonam, carumonam, pefloxacin, miloxacin, trovafloxacin, doripenem, imipenem, cefozopran, ceftazidime, linezolid for urinary excretion and rifapentine, cabotegravir, and dolutegravir for fecal excretion

4区 · 医学

Article

作者: Srinivas, Nuggehally R.

1. Interspecies allometry scaling for prediction of human excretory amounts in urine or feces was performed for numerous antibacterials. Antibacterials used for urinary scaling were: rifapentine, pefloxacin, trovafloxacin (Gr1/low; <10%); miloxacin, linezolid, PNU-142300 (Gr2/medium; 10-40%); aztreonam, carumonam, cefozopran, doripenem, imipenem, and ceftazidime (Gr3/high; >50%). Rifapentine, cabotegravir, and dolutegravir was used for fecal scaling (high; >50%). 2. The employment of allometry equation: Y = aW(b) enabled scaling of urine/fecal amounts from animal species. Corresponding predicted amounts were converted into % recovery by considering the respective human dose. Comparison of predicted/observed values enabled fold difference and error calculations (mean absolute error [MAE] and root mean square error [RMSE]). Comparisons were made for urinary/fecal data; and qualitative assessment was made amongst Gr1/Gr2/Gr3 for urine. 3. Average correlation coefficient for the allometry scaling was >0.995. Excretory amount predictions were largely within 0.75- to 1.5-fold differences. Average MAE and RMSE were within ±22% and 23%, respectively. Although robust predictions were achieved for higher urinary/fecal excretion (>50%), interspecies scaling was applicable for low/medium excretory drugs. 4. Based on the data, interspecies scaling of urine or fecal excretory amounts may be potentially used as a tool to understand the significance of either urinary or fecal routes of elimination in humans in early development.

1996-06-01·Journal of Chromatography B: Biomedical Sciences and Applications

High-performance liquid chromatographic method for the rapid and simultaneous determination of sulfamonomethoxine, miloxacin and oxolinic acid in serum and muscle of cultured fish

Article

作者: Takahiko Aoki ; Ryuji Ueno

A rapid method for the simultaneous determination of sulfamonomethoxine (SMM), miloxacin (MLX) and oxolinic acid (OA) in serum and muscle of cultured fish by high-performance liquid chromatography has been developed. A Hisep shielded hydrophobic phase column (15 cm x 4.6 mm I.D.) and a mobile phase of 0.05 M citric acid-0.2 M disodium hydrogenphosphate buffer, pH 2.5 in 10 mM tetra-n-butyl ammonium bromide-acetonitrile (85:15) with ultraviolet detection at 265 nm were used. The recoveries of SMM, MLX and OA from serum and muscle samples were 72-101%. The detection limits of the three drugs were 0.05-0.1 microgram/ml or g of sample.

1981-09-01·The Japanese journal of antibiotics

[Chemotherapy on the biliary tract infections. XIII. Miloxacin, a novel chemotherapeutic agent, its excretion into bile and clinical effect on the biliary tract infections (author's transl)].

Article

Miloxacin, a novel chemotherapeutic agent, has been reported to have very potent antibacterial activity to E. coli, Klebsiella, Proteus and other Gram-negative rods and be excreted into bile at high levels. Therefore, the effectiveness of miloxacin against biliary tract infections and its excretion into bile in patients were investigated. The results were as follows: i) Comparative studies on the excretion of miloxacin, nalidixic acid (NA) and cephalexin (CEX) into bile of patients operated in gallbladder were performed by a crossover method. The maximum concentration of miloxacin after oral administration of 500 mg ranged from 18.2 to 24.0 micrograms/ml and were much higher than those of NA (5.3 micrograms/ml) and CEX (3.4 micrograms/ml). The mean recovery of miloxacin within 6 hours was 0.256% and much greater than those of NA (0.075%) and CEX (0.027%). ii) Into bile, intact miloxacin and its metabolites (the glucuronides of miloxacin and M-2) were excreted but M-1 was scarcely excreted. Regression analysis of the concentrations by the bioassay compared with those intact miloxacin by the HPLC method gave a good correlation with r = 0.96. iii) The clinical effectiveness against the biliary tract infections was investigated in 29 cases. Miloxacin showed the excellent effect in 8 cases and the good effect in 17 cases, giving an effective ratio of 86.2%. Especially, all of the cases dosed with miloxacin over 34 mg/kg in a day showed excellent or good results. iv) The rates of clinical effectiveness were 85.7, 80.0% and 71.4% in E. coli, Klebsiella and Proteus infections, respectively. The antibacterial activity of miloxacin against 27 strains isolated in this test was more potent than those of NA and CEX. v) During the clinical tests, none of any side effect with miloxacin was observed in both of subjective and objective symptoms. These results show that miloxacin is expected to be fully applicable on the therapy of biliary tract infections.

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