From experiments in which cefradine (CED) was orally administered to healthy volunteers in doses of 1,000mg, 500mg and successive 250mg after meal and 500mg in fasting condition, the following results were obtained.
1) Absorption of CED was rapid in fasting volunteers with peak serum levels at about one hour after administration. On the other hand, the absorption was delayed in non-fasting volunteers with peak serum levels at about 2-3 hours after administration. Absorbed amounts of CED were proportional to the doses with no effect of meal.
2) Maximum urinary excretion of CED was observed in 0-2 hour-urine of fasting volunteers and 2-4 hour-urine of non-fasting volunteers. Total urinary recovery of CED was about 85% in either experiment, showing no effect of meal.

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[in Japanese]

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We estimated the minimum inhibitory concentrations of following twenty-one antimicrobial agents against 161 strains of Pseudomonas aeruginosaisolated from clinical specimens during 1979. Antimicrobial agents were 5 penicillins (carbenicillin, sulbenicillin, piperacillin, apalcillin and ticarcillin), 3 cephalosporins (cefsulodin, cefoperazone and ceftizoxime), 5 aminoglycosides (gentamicin, tobramycin, dibekacin, amikacin and kanamycin), 3 tetracyclines (tetracycline, doxycycline and minocycline), chloramphenicol, colistin, polymyxin B, nalidixic acid and pipemidic acid.
Among penicillins piperacillin and apalcillin showed strongest antibacterial activity and the activity of carbenicillin was weakest. Highly resistant strains against carbenicillin increased rapidly until 1975.
Among cephalosporins cefsulodin showed strongest antibacterial activity and its activity was stronger than piperacillin. Antibacterial activity of cefoperazone and ceftizoxime were weaker than cefsulodin, but stronger than carbenicillin and sulbenicillin.
Among aminoglycosides kanamycin showed very weak antibacterial activity, but another four drugs showed very strong activity. But resistant strains against these four drugs increased gradually and over 20% of strains was resistant to gentamicin. Among gentamicin, tobramycin and dibekacin cross-resistance was observed, but not between amikacin and these three drugs. Recently the number of strains resistant to both amikacin and gentamicin increased.
Tetracyclines, chloramphenicol and nalidixic acid showed rather weak activity, but colistin and polymyxin B showed very strong activity and resistant strains against these drugs were very few. Pipemidic acid showed rather stronger activity than nalidixic acid, but its activity was weaker than aminoglycosides excluding kanamycin.

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The competitive effect of ceftizoxime, a new cephalosporin, on in vitro binding of bilirubin to human serum albumin was investigated and compared with that of other β-lactam antibiotics. At the normal range of the albumin (3.48g/dl) and bilirubin (0.936mg/dl) concentrations in the serum of healthy infants, free bilirubin concentration was not increased by adding ceftizoxime and the other,βlactam antibiotic concentrations tested (up to 640μg/ml). The same results were obtained even under the same condition except that the bilirubin concentration was increased to 10mg/dl. Under the condition that the albumin concentration decreased to one fifth of the normal concentration, bilirubin was competitively displaced to some extent by adding dicloxacillin (MDIPC), cefazolin (CEZ) and cefmetazole (CMZ) but not by adding ceftizoxime at the concentration of 640μg/ml.

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The mechanism of renal excretion of ceftizoxime was investigated by renal clearance test and stop flow analysis in rabbits and dogs.
The serum half life of ceftizoxime after dosing of probenecid and ceftizoxime in combination was about twice longer in rabbits than and almost the same in dogs as that after dosing of ceftizoxime alone.
Renal clearance test and stop flow analysis were performed with the following results:
(1) Renal clearance of ceftizoxime was about 3.2 times higher in rabbits than and almost the same in dogs as creatinine clearance.
(2) Ceftizoxime was scarcely excreted and reabsorbed in the proximal and distal areas of dogs.
(3) Ceftizoxime was excreted in the proximal area and not reabsorbed in the distal area of rabbits.
These findings indicate that 60% of the urinary excretion of ceftizoxime was obtained through proximal tubule and remaining amount by glomerular filtration in rabbits, and most of the urinary excretion was obtained by glomerular filtration in dogs.

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Ocular tissue levels of dibekacin (DKB) were studied in rabbits after instillation of 0.3% DKB eye-drops five times every 5 minutes.
(1) In normal eyes, DKB levels were determined in all of the outer parts of eye and some of inner parts such as aqueous humor and vitreous body. Such levels were relatively higher than those of gentamicin.
(2) In cauterized eyes by NaOH tissue levels were several times higher than those obtained in normal eyes.
(3) Considering these results and MIC levels against both Gram-positive and Gram-negative bacteria such as Pseudomonas aeruginosa or Staphylococcus aureus, it is suggested that 0.3% DKB eye-drops will show effectiveness in clinical use.

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A daily dose of 1.0-1.5g of amoxicillin, a synthetic penicillin, was tried as an antiluetic in 9 cases of syphilis. Oral administration for 4 weeks makes up one course of treatment. One of the patients was given two courses of treatment.
Amoxicillin showed effect in 6 patients out of 9 (66.7%).
Constipation and diarrhoea were observed in two cases and one case as side effects, and they were controlled easily.
Amoxicillin could be a very effective and safe antiluetic.

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