In an in vitro combination study norfloxacin was compared with gentamicin in combination with four β-lactams (piperacillin, ceftazidime, cefsulodin, and ceftriaxone) against ten strains of clinically isolated Pseudomonas aeruginosa by microtitre checkerboard technique. Synergy was found in 30-70% of the tested strains with gentamicin-β-lactam combinations and 0-40% with norfloxacin-β-lactam combinations.
One strain highly resistant to β-lactams was selected for studying the combined effect of three drugs (gentamicin, norfloxacin, β-lactams) in comparison with two drug combinations. Three drug combinations were found to be superior to two-drug as shown by a further reduction in a Fractional Inhibitory Concentration (FIC) index. The best result was obtained from the combination of norfloxacin, gentamicin, and piperacillin. No antagonism was found in any of the combinations tested.

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Two hundred and nine strains of Staphylococcus aureus isolated from clinical specimens were tested for drug-susceptibility to 16 antibiotics and coagulase typing.
Comparing the MIC ₈₀ of the 16 drugs, we found that cephaloridine, gentamicin, minocycline, cefazolin, methicillin, and cefmetazole were effective against S. aureus. The isolation frequency of methicillin-resistant strains (MRSA) was 12.4%, and almost all MRSA were multiple-resistant. The isolation frequency of drug-resistant strains to other antibiotics was between 2.6%(chloramphenicol) and 25.8%(erythromycin). The percentage of β-lactamase-producing strains was 72.2%. We found no relation between the MIC of ampicillin and β-lactamase production. Though minocycline is effective against MRSA, 9.1% of strains were resistant.
We also examined the coagulase typing of S. aureus. Type VII strains were predominantly isolated (33.0%), followed by type II (30.7%) and type IV (17.3%). Correlation between coagulase type and drug susceptibility was noted. Almost all drug-resistant strains belonged to coagulase type IV and most of the coagulase type VII strains were sensitive to all 16 antibiotics.

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The distribution of cefmetazole to broncho-alveolar space after i. v. administration was studied in rabbits with unilateral acid aspiration pneumonia. Penetration to the side with pneumonia and the opposite intact side were compared. The effect of gravitational blood flow on drug distribution was also evaluated. The following results were obtained.
1) Concentrations of CMZ in lung tissue and broncho-alveolar lavage fluid were significantly higher on the pneumonia side than on the intact side.
2) Penetration to broncho-alveolar space was closely related to the drug concentration in serum.
3) Distribution of CMZ in the lung was proportional to the gravitational blood flow.
These findings indicate that the penetration of CMZ to broncho-alveolar space is mainly due to a passive diffusion mechanism; and that when inflammation is present, this mechanism is probably facilitated by the breakdown of the “ blood-broncho-alveolar barrier ”.

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The pharmacokinetics and therapeutic effect of cefbuperazone (CBPZ) were studied using rabbits with an experimental biliary infection caused by E. coli. The animals were divided into three groups; control group: normal rabbits, CBPZ (-) group: infected rabbits without CBPZ, CBPZ (+) group: infected rabbits with CBPZ administration. The following resultswere obtained.
1. Bile color in the CBPZ (-) group changed from green to pale brown, but no changes were found in the CBPZ (+) group.
2. The number of viable E. coli in bile did not decrease even 48 hr later in the CBPZ (-) group; but in the CBPZ (+) group, it decreased progmessively until it was less than 10 cells/ml after 24 hr.
3. White blood cells in the CBPZ (+) group were significantly less than in the CBPZ (-) group.
4. Liver dysfunction in the CBPZ (+) group was not serious compared to that of the CBPZ (-) group.
5. CBPZ level in bile was much higher than that in blood.
6. CBPZ in the gallbladder and bile duct showed high levels even after 6 hr.
7. From the microscopic findings, inflammatory changes in the gallbladder and bile duct in the CBPZ (+) group were not so serious as those in the CBPZ (-) group.
From these results, we concluded that CBPZ has a high degree of biliary excretion and excellent tissue penetration, and that it should be useful in the treatment of biliary infection.

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The cephalosporin group of antimicrobials has gained general acceptance for surgical prophylaxis. However, the number and variety of cephalosporins now available have complicated the process of choosing the most effective agent. In our previous studies we produced evidence that thirdgeneration cephalosporins resulted in postoperative infection rates lower than with second-generation cephalosporins. In this study, clinical isolates from patients with postoperative infections after prophylaxis with second-or third-generation cephalosporins were sensitive mainly to penicillins and/or aminoglycosides. There were no problems in the treatment of postoperative infections following abdominal surgery after prophylaxis with third-generation cephalosporins. It is advisable, however, that the newer antibiotics should not be given for prophylaxis, but reserved for the treatment of postoperative infections.

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Urinary tract infection before transurethral prostatectomy is thought to increase post-operative morbidity including sepsis. In this study, 14 of 37 patients undergoing transurethral prostatectomy had bacteriuria before surgery. No sepsis developed and all infections disappeared after surgery. Further analysis revealed that both lenkocytosis and the fever index were lower in the eight patients to whom antibiotics were administered just before prostatectomy than in the other six patients.

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We conducted a double blind study to evaluate the efficacy of norfioxacin (NFLX) and the recurrence of female uncomplicated cystitis after treatment. Patients were given 400, 200 or 100 mg of NFLX orally b. i. d. for seven days. Clinical efficacy was evaluated at the third and seventh day of treatment. It for the recurrence of cystitis was done at the seventh day after the end of treatment.
1) E. coli was found in 80.4% of the strains isolated as ausative organisms. The MICs of NFLX were less than 0.2μg/ml against 92% of E. coli. Of the causative organisms, 10.5% consisted of Gram-positive cocci. The MICs against 87.5% of these were greater than 6.25μg/ml.
2) Overall clinical efficacy at the third day of treatment was 100% in the 400 mg group (46 patients), 200 mg (53) and 100 mg group (40). Likewise, it was 100% for all groups at the seventh day of treatment. No significant difference between the groups was observed in the evaluation of overall clinical efficacy, effects on symptoms, pyuria and bacteriuria.
3) Recurrence of cystitis was evaluated in 82 patients; namely, in 25, 29 and 28 patients from the 400, 200 and 100 mg group, respectively. Recurrence was observed in two patients after treatment with 400 or 200 mg. The overall recurrence rate was only 2.4%(2/82).
From the present study we have concluded that 100-400 mg/day of NFLX is effective in the treatment of female acute uncomplicated cystitis, and that the incidence of recurrence is possibly lower than that after treatment with other chemotherapeutic agents.

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Influences of OK-432 and/or bone marrow transplantation (BMT) on the suppression of bone marrow cells proliferation by mitomycin C (MMC) were observed with CFU-C, CFU-S and CFU-F in mice.
The suppression of CFU-C, CFU-S and CFU-F by MMC was restored by the administration of OK-432 (50 KE/kg) at day 1 after the treatment with MMC, but not before the MMC treatment.
An administration of OK-432 (10 KE/kg) five times at day 1, 3, 5, 7 and 9 after the MMC treatment was more effective than single dosage of 50 KE/kg 1 day after the MMC treatment.
The bone marrow suppression by MMC was restored by BMT alone.
From the results of the present experiments, we suggest that the administration of OK-432 in purpose of restoration of the suppressed bone marrow cells proliferation by MMC should be done after the treatment with MMC. In addition, a stimulatory effect of OK-432 on the proliferation of the transplanted bone marrow cells was also suggested.

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