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Biomedical subjects

A Yoshitake

Publications and source records attributed to A Yoshitake.

At least 73 records · Page 4Linked to original sources
PubMed1985

Application of gas chromatograph-mass spectrometer-computer system to evaluation of 14C-labelled compounds.

Usefulness of gas chromatograph-mass spectrometer-computer system (GC-MS-CPU) not only for measurement of specific activities of 14C-labelled compounds in a mixture but also for evaluation of 14C-labelled compounds in terms of examining their purities and elucidating chemical structures of the impurities was proved. A sample of methyl 2-(p-chlorophenyl-14Cn)-3-methylbutylate (III) synthesized from p-chlorophenyl-14Cn-acetonitrile (VI) was analyzed by GC-MS-CPU, and it was found that the labelled compound was contaminated with a small amount of the corresponding m-isomer (IV) having a very high specific activity. Further examination suggested that the contaminating m-isomer (IV) originated from m-chlorophenyl-14Cn-acetonitrile (IX) which had already contaminated in the starting material (VI), and also that cyanomethylation of p-dichlorobenzene-14Cn (VIII) by benzene-type reaction resulted in producing a mixture of p- and m-chlorophenyl-14Cn-acetonitriles (VI, IX).

Carbon Radioisotopes↗
PubMed1980

Absorption and excretion of miloxacin in mice, rats, and dogs.

Miloxacin, a synthetic antibacterial agent structurally related to oxolinic acid, has a broad spectrum of activity in vitro against gram-negative bacteria and considerable activity in vivo against infections with these bacteria. These observations led to studies on the absorption and excretion of miloxacin in mice, rats, and dogs after administration of a single oral dose. Studies on oxolinic acid have been included for comparison. Peak serum levels of miloxacin, attained 1 h after administration of 20, 50, and 100 mg/kg to rats and dogs, were approximately 20, 40, and 60 micrograms/ml, respectively. Peak levels in mice receiving the same dose were 15, 60, and 80 micrograms/ml at 0.5 h. Peak serum levels of oxolinic acid were attained 0.5 to 1 h later than the above times at comparable doses and were one-half to one-fourth those of miloxacin. Urinary recovery of miloxacin at the above doses ranged from 3.2 to 6.5% during the 24-h posttreatment period. Recoveries of oxolinic acid were one-half to one-fifth those of miloxacin. At a 50-mg/kg dose, rats excreted 4.6% of the miloxacin in bile in the 20-h posttreatment period.

4-Quinolones↗
PubMed1980

Determination of miloxacin and metabolites in human serum and urine by high-pressure liquid chromatography.

A sensitive and reliable high-pressure liquid chromatography (HPLC) assay for miloxacin and its two principal metabolites, 5,8-dihydro-8-oxo-2H-1,3-dioxolo[4,5-g]quinoline-7-carboxylic acid (M-1) and 1,4-dihydro-1,6-dimethoxy-7-hydroxy-4-oxoquinoline-3-carboxylic acid (M-2), in human serum and urine was developed. A strong anion-exchange Zipax SAX column using a mobile phase of 0.01 M citric acid solution containing 0.03 M sodium nitrate with pH 5.0 was used to achieve separation of the three compounds. The retention times of miloxacin, M-1, and M-2 were 3.8, 9.3, and 5.9 min, respectively. Serum and urine concentrations of these compounds as low as 10 ng/ml were measured. When results from the HPLC assay were compared with those from the microbiological assay of serum and urine samples from human subjects receiving miloxacin orally, the correlation coefficients were 0.94 for the serum and 0.99 for the urine. The HPLC assay method presents an alternative to the microbiological assay and permits future pharmacokinetic investigations of miloxacin.

4-Quinolones↗
PubMed1980

[Absorption, distribution, excretion, and metabolism of 14C-miloxacin in female rats (author's transl)].

Absorption, distribution, excretion, and metabolism of 5,8-dihydro-5-methoxy-8-oxo-2H-1, 3-dioxolo[4,5-g]quinoline-7-carboxylic acid(miloxacin), a new antimicrobial agent, were studied in female rats by using 14C-miloxacin which was administered orally to the animals in a dose of 50 mg/kg. 14C-Miloxacin was absorbed rather fast and the radioactivity of 14C distributed widely in a variety of tissues. Peak concentrations of 14C in serum and tissues occurred 1 to 2 hr after dosing, and were approximately 60 micrograms equivalent of miloxacin per ml or g in serum, liver and kidney. Excretion of 14C in urine and feces was fast, and recoveries of 14C during 48 hr period were approximately 30% in urine and 60% in feces. Concentrations of intact 14C-miloxacin were higher in serum and kidney while lower in liver. Major metabolites in excreta were the demethoxy derivative (M-1) and the glucuronide of miloxacin; and as minor metabolites five other metabolites were identified. As sex differences, the following facts were observed; concentrations of 14C in serum and tissues were generally 1.2 to 1.6 times higher in female rats those in male rats, and the capacity to metabolize miloxacin, especially in the glucuronic acid conjugation, was rather lower in female rats than that in male rats.

4-Quinolones↗
PubMed1979

[Metabolism of 14C-miloxacin in rats--metabolites in urine, bile and feces (author's transl)].

Isolation and characterization of metabolites of miloxacin, a new antimicrobial agent, were undertaken with rats. 14C-Miloxacin was orally administered to Sprague-Dawley rats at a dose of 50 mg/kg, and urine, bile and feces were collected. The metabolites extracted from the biological samples were isolated by column and thin-layer chromatographies. Characterization of the isolated metabolites was carried out by comparison with the authentic materials in various physicochemical analyses. Eight metabolites together with intact miloxacin were identified; containing the metabolites of N-demethoxy (M-1), catechol (M-3) and 6-methoxy (M-2 and M-4) types and their conjugates with glucuronic acid.

Animals↗