The netilmicin (NTL), which is an aminoglycoside antibiotic, was determined by high-performance liquid chromatography (HPLC) using the post-column derivatization with ο-phthalaldehyde and β-mercaptopropionic acid (OPA/MP) for the sensitive and stable analysis.
The OPA/MP gave the good stability for a long time more than OPA and 2-mercaptoethanol (ME)(OPA/ME), and also its fluorescent derivative of NTL was stable. The reaction of OPA/MP and NTL was almost independent on both the reaction temperature and the time. So, the OPA/MP was the more useful reagent for HPLC analysis using auto-sampler. The fluorescent intensity of the derivative of NTL with OPA/MP was about twice as much as that of the OPA/ME [the limits of detection in human plasma were 0.2 μg/ml (OPA/MP) and 0.5 μg/ml (OPA/ME), respectively].
For an application to the clinical sample, the serum concentrations after intramuscular administration of NTL in man were measured by the three method (HPLC with OPA/MP, HPLC with OPA/ME and SLFIA). The good correlation between both HPLC methods and SLFIA method was obtained, and the SLFIA method gave a little higher results. The results of both HPLC methods were almost the same. In the view of the stability and the sensitivity, therefore, the use of OPA/MP in HPLC analysis of the aminoglycoside antibiotics may be recommended than the OPA/ME.

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Two-hundred and thirty-four bacteria isolated from urine of patients with acute cystitis were compared with 386 bacteria isolated from patients with complicated urinary tract infection. E. coli was isolated from 81.2% of patients with acute cystitis. In complicated urinary tract infection, the frequencies of Klebsiella, Proteus, Serratia and Pseudomonas increased, and the incidence of E. coli decreased to 37.0%. Minimal inhibitory concentration (MIC) of cinoxacin for isolates from complicated urinary tract infection was lower than that of the same species isolated from acute cystitis. Oral cinoxacin administration in a daily dose of 800 mg eradicated all bacteria from patients with acute cystitis. No relationship was found between MIC and clinical effects of the drug.

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Five-hundred and sixteen adult patients with acute cystitis were treated with cinoxacin, 400 mg twice daily for a week. Two-hundred and thirty-three cases who passed the criteria of acute simple cystitis which was decided by UTI Committee Members, showed a high cure rate of 98.7%. The rate was 94.6% with atypical cases who were excluded from above calculation because they were either older than 69 years or male, or had a history longer than 2 weeks. Patients infected with S.epidermidis less responded to the treatment.

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The incidence of pre-and post-operative infections among 52 patients who underwent transurethral prostatectomy (TUR) was studied. Cefotetan was used to prevent pen-operative complications caused by bacteria; twice on the day of TUR and the succeeding day, and once the succeeding two days in a dose of 1 gram. No case suffered such active infection as septicemia, epididymitis and pyelonephritis. Nineteen out of 22 cases (86.4%) with significant pre-operative bacteriuria (>1×10⁴/ml) had not significant bacteriuria after the TUR. Twenty-six out of 30 cases (86.7%) without significant pre-TUR bacteriuria were aseptic after the TUR. The organisms found after TUR were, with one exception, either P.aeruginosa or E. faecalis which are resistant to the drug.

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Effectiveness of antibiotics against respiratory infection can be achieved when it is inhibitory for offending microorganism and its distribution is sufficient in the affected tissue. For evaluation of cefbuperazone, 100 mg per kg was intravenously injected to albino rabbits, and bronchoalveolar lavage was conducted repeatedly. Cefbuperazone was detected in the bronchoalveolar lavage fluid from 30 minutes to 6 hours, with maximum concentration of 1.7 μg/ml from one rabbit and 1.0 μg/ml in average of 4 rabbits. Comparring these value to venous blood maximum concentrations of cefbuperazone, namely 216.5 μg/ml from one rabbit and 144.6 μg/ml in average of 4 rabbits, ratio was one to 127 and one to 145 each, and the data indicated low distribution of cefbuperazone in bronchoalveolar tissue.
Concentration of cefbuperazone in the bronchoalveolar lavage fluid increased proportionally relating to the amount intravenously injected.
Bronchoalveolar lavage space was filled with saline to death, and cefbuperazone concentration of the saline was measured. Cefbuperazone concentration at the time filled and that of 30 minutes later showed the ratio of 1 to 4.5 which result indicate the drug diffused from the wall to fluid filling the lumen in 30 minutes. This data suggest that the concentrations of cefbuperazone in the bronchoalveolar lavage fluid reflect that of the tissue but express several times lower.

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A study was made to assess the clinical efficacy of norfloxacin (NFLX), a member of the 3 rd generation quinolones, on bacterial prostatitis.
Prior to the treatment, the diffusion of NFLX into human prostatic fluids (PF) was assayed in using expressed prostatic secretions (EPS). When administering 200 mg of the drug, an average concentration after one hour was 0.16 μg/ml (n=6).
The clinical study involved 15 patients with 10 acute and 5 chronic bacterial prostatitis. The isolates from EPS totally consisted of gram-negative bacilli (GNB) i. e., 13 of E. coli, 1 of K. pneumoniae and 1 of E. cloacae. The MIC of NFLX on the strains of E. coli was sensitive in a range from 0.025 to 0.1 μg/ml.
NFLX was administered at a dosage of 600 mg a day for 12-51 days depending on the clinical courses. The bacteriological eradication was obtained in 14 out of 15 isolates throughout the treatment. The overall clinical efficacy was evaluated as excellent in 46.7%, good in 40.0% and poor in 13.3%, effectiveness rate being 86.7% in total.
There were no side effects and no abnormal laboratory findings throughout the treatment in all cases.
From the result obtained, NFLX was considered to be a successful and safe antimicrobial drug in the treatment of bacterial prostatitis.

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A double blind comparison of L-105, a new parenteral cephalosporin and cefmenoxime was carried out in the treatment of complicated urinary tract infections. Patients received either 1g of L-105 or cefmenoxime twice a day for 5 days by intravenous drip infusion.
All patients had pyuria of at least 5 WBCs per high power field, bacteriuria of at least 104 bacteria per ml of urine and underlying urinary tract disease. The overall clinical efficacy of the treatment was evaluated by the criteria proposed by the UTI Committee in Japan as excellent, moderate or poor based on the combination of changes in pyuria and bacteriuria.
Of the 183 patients evaluated for the clinical efficacy, 93 patients received L-105 and 90 received cefmenoxime. No significant difference in background characteristics was observed between the two treatment groups. Excellent and moderate responses were obtained in 63. 4% of the patients receiving L-105 and in 56. 7% of the patients receiving cefmenoxime. This difference was not statistically significant. The overall bacteriological eradication rates obtained were 85.2% of 149 strains in the L-105 group and 84.1% of 151 strains in the cefmenoxime group. The eradication rates for P. aeruginosa were low in both groups.
Clinical adverse reactions were observed in each one patient in both groups. Drug related laboratory adverse reactions were observed in each 5 patients in both groups. There were no significant differences between the two treatment groups regarding the incidences of clinical and laboratory adverse reactions and L-105 appeared to be as well tolerated as cefmenoxime.
From the results obtained in this study, we concluded that L-105 was as useful as cefmenoxime in the treatment of complicated urinary tract infections, except for those due to P. aeruginosa.

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The clinical effectiveness and safety of BAY o 9867 (Ciprofloxacin, CPFX) in the treatment of the patients with bacterial pneumonia were compared with those of bacampicillin (BAPC) by a double-dummy fashion.
Patients over 18 years old with apparent clinical signs and symptoms of pneumonia were administered with CPFX at a daily dose of 600 mg or BAPC at a daily dose of 1 g orally for 14 days in principle.
The following results were obtained.
1) On the basis of committee judgement, the clinical efficacy rate in the total cases including non-bacterial pneumonia was 85.3%(58/68) in CPFX group and 90.5%(57/63) in BAPC group, respectively. In bacterial pneumonia, the rate was 83.3%(45/54) in CPFX group and 88.9%(40/45) in BAPC group, respectively. The differences between the two groups in both analyses were statistically not significant.
2) The clinical efficacy rate by doctors in charge in the total cases was 87.7%(57/65) in CPFX group and 86.9%(53/61) in BAPC group, respectively. In bacterial pneumonia, the rate was 86.8%(46/53) for CPFX group and 87. 2%(41/47) for BAPC group, respectively. In both analyses, the differences between the two groups were statistically not significant.
3) As for the bacteriological response, the eradication rate in the total cases was 85.7%(18/21) in CPFX group and 65.0%(13/20) in BAPC group, respectively. In bacterial pneumonia, the eradication rate was 83.3%(15/18) in CPFX group and 56.3%(9/16) in BAPC group, respectively. In both analyses, the rates of CPFX were higher than those of BAPC, but statistically, the differences between the two groups were not significant.
4) Side effects were noted in 7 of 83 cases (8.4%) treated with CPFX and 8 of 84 cases (9.5%) with BAPC, and abnormal changes in laboratory findings were noted in 12 of 80 cases (15.0%) with CPFX and 18 of 77 cases (23.4%) with BAPC. The differences between the two groups were not significant statistically. Neither serious side effect nor remarkable abnormal change in laboratory findings was noted.
5) The utility rates judged by the committee members and by doctors in charge were not significantly different between the two groups.
From these results, it is considered that the clinical efficacy and safety of CPFX at a daily dose of 600 mg are equal to those of BAPC at a daily dose of 1 g in the treatment of the patients with bacterial pneumonia.

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