Cefotiam (CTM) is a new cephem antibiotic which has potent activities against Gram-positive and Gram-negative bacteria.
We investigated the prophylactic treatment of CTM in orthopedic surgery and the concentrations of CTM Gram-negative in cerebrospinal fluid.
1. The mean serum concentration at 2 hours after the drip infusion of CTM (3g) was 28.28±5.48μg/ml, and the mean concentration of CTM in cerebrospinal fluid was 0.58±0.07μg/ml.
2. From the result of multi-regression analysis in group I (12 cases, over 40 years old) and group II (10 cases, below 39 years old), it was suggested that the factor of age had a marked effect on cerebrospinal fluid concentrations of CTM.(Group I>Group II)
3. High concentrations of CTM in cerebrospinal fluid after the 3g-administration, exceeding the MIC₈₀ for most causative organisms, suggested very useful prophylactic treatment of CTM in orthopedic surgery.

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Single doses of cefmenoxime (CMX), 1g intravenous drip infusion, were administrated to 5 patients with pleural effusion. The study group consisted of 3 men and 2 women, aged 38 to 69 years (mean 54.8 years); 4 had carcinoma with pleural effusion and 1 had SLE. Pleural fluid and serum samples were taken at intervals 1 to 24 hours for determination of CMX levels. The following results were obtained:
1. Intravenous drip infusion of 1g CMX yielded a peak pleural concentration of 4.5μg/ml after 2 hours and pleural levels over 3μg/ml were maintained for 5.5 hours after intravenous drip administration.
2. Ratio maximum pleural concentration to peak serum level reached 15.0±8.3% at 2 hours after intravenous drip administration.

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Penetration of lincomycin (LCM) in choledochal and cholecystic bile as well as in the gallbladder tissue and liver tissue was investigated together with bacteria detectable in the bile in order to evaluate basically usefulness of this antibiotic in the treatment of infections of the hepatocystic duct.
1. Intravenous drip infusion of LCM 1.5g (in 500ml of 5% glucose solution) over 1.5-2 hours resulted in mean drug concentrations of 33.9 and 10.1μg/ml in serum at 2 and 4 hours post start of infusion re-spectively; 215.5μg/ml in choledochal bile at 3 hours 15 minutes; 252.7μg/ml in cholecystic bile at 3 hours 36 minutes; 28.1μg/g in gallbladder tissue at 2 hours 55 minutes; and 15.4μg/g in liver tissue at 4 hours.
2. A cross-over study of LCM and cefazolin (CEZ) in 2 cases where T-tubes were employed demonstrat-ed evidently higher biliary levels of LCM than CEZ.
3. Bacteriological examination showed that Hafnia alvei plusStreptococcus faecalts were presented in choledochal bile from just 1 of 4 cases while in cholecystic bile from 9 of 15 cases were detected 22 strains of organisms includingKlebsiella pneumoniae (7 strains),Bacteroides fragilis (5), Escherichia coli (2), Citro-bacter freundii (2) and Serratia marcescens (2). A total of 7 strains of anaerobes including B. fragilis was isolated.
4. The above concentrations of LCM in the bile, gallbladder tissue and liver tissue sufficiently covered the MIC₉₀ of this antibiotic determined by us in 1980 for major species of anaerobes including clinical isolates of B. fragilis.
5. High penetration of LCM in the hepatocystic duct as well as its antibacterial spectrum and mode of action suggested usefulness of this antibiotic in the treatment of anaerobic infections of the hepatocystic duct. Also, LCM was thought very promising as an antibiotic to be used in combination with β-lactam antibiotics in treating mixed aerobic and anaerobic infections because it can eliminate antagonism to help cover a wider range of organisms and also can suppress β-lactamase activity.

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Thirty male patients with gonorrheal urethritis were treated with azthreonam at the urological ward of Tokyo Metropolitan Taito Hospital during the period from January to March, 1984, and clinically evaluated. Sixty-one strains of Neisseria gonorrhoeae isolated from the clinical specimens including those of the patients were bacteriologically studied.
Of the 61 strains, 9 (15%) were PPNG strains and the other 52 strains were non-PPNG strains.
MICs of PCG to the 9 PPNG strains were 3.13-50μg/ml and to the 52 non-PPNG strains were 0.024-3.13μg/ml. While MICs of azthreonam to the PPNG strains were 0.024-0.20μg/ml and to the non-PPNG strains were 0.0122-0.78μg/ml.
Those patients with gonorrheal urethritis were given a single 1g intramuscular dose of azthreonam.
The following clinical findings were obtained:
1. The clinical efficacy rate of 30 cases was 100%; excellent in 16, good in 14 cases.
2. All 2 patients with gonorrheal urethritis caused by PPNGs were cured with the treatment.
3. No subjective side effects were found.

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As part of preventive measures against postoperative infection following cardiac catheterization in infants with cardiac diseases, especially falling bacteria in X-ray room was studied. Moreover, a synthetic penicillin, ticarcillin (TIPC), was used as preventive antibiotic against postoperative infections due to falling bacteria which probably contaminate the air in the X-ray examination room, and the efficacy and side effects of the drug were observed. As result, coagulase-negative Staphylococcus was detected the most, followed by Micrococcus and then by fungus. The number of these 3 organisms corresponded to 90.3% of the total number of falling bacteria detected during operation. The number of falling bacteria during operation was 5.1 times larger than that before operation. Taking into account normal flora of skin, falling bacteria present in the X-ray room and causative organisms of bacterial endocarditis, TIPC was administered to 30 cases intravenously 5 times at a dose of 30mg/kg every 8 hours for the purpose of preventing possible postoperative infections following cardiac catheterization. The drug was effective to prevent such infec-tions in all cases. No side effects were noted in any case, in peripheral blood and hepatic function tests and other observations.

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Clinical studies on sulbactam/cefoperazone (SBT/CPZ) were carried out and the results were as follows: Eleven patients (pneumonia 8, acute purulent arthritis of the knee joint 1, urinary tract infection 2) were treated with SBT/CPZ, in doses of 30-67mg/kg divided 3 times per day for 3-6 1/3 days intravenously. The overall efficacy rate was 100%. As to adverse reaction, diarrhea was observed in 1 case. Abnormal laboratory data were noted in 2 cases (GPT elevation in 1, and eosinophilia and GPT elevation in 1).

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Approximately 20mg/kg/day of sulbactam/cefoperazone (SBT/CPZ) was given by one shot intravenous injection to 16 pediatric inpatients with respiratory tract infections (13 cases), urinary tract infection (1 case), skin infection (1 case) or gastrointestinal tract infection (1 case).
An excellent efficacy in 6 cases and a good efficacy in 10 cases were observed. Causative organisms were not identified in the respiratory tract infections, even though the efficacy was excellent or good.
Side effects were not noticed in particular and SBT/CPZ was judged as safe enough agent.
Concentrations of SBT/CPZ in the spinal fluid were determined in 3 patients. Their low concentrations suggested the poor transfer into the spinal fluid.
Finally, SBT/CPZ is a very useful agent since it is effective also against resistant organisms which produce penicillinase-type β-lactarnases.

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1. Sulbactam/cefoperazone (SBT/CPZ) was administered intravenously to 9 patients with respiratory infections (H. influenzae 6 cases, pathogens unknown 3 cases), 2 patients with urinary tract infection (E. coli and C. freundii; both cases had VUR), and 1 patient with staphylococcal bacteremia.
In these causative bacteria, 5 strains (H. influenzae 3, E. coil 1 and S. aureus 1) were beta-lactamase producers.
2. Bacteriological efficacy (eradication rate) was complete (9/9, 100%) and clinical efficacy was also complete (12/12, 100%).
3. In comparison with CPZ alone, MICs of SBT/CPZ against beta-lactamase producing bacteria were superior.
4. Although mild side effect was observed in 1 case (eosinophilia), no other severe form of adverse reaction were encountered.
5. It was concluded that SBT/CPZ was an useful antibiotic for the treatment of pediatric bacterial infections, especially caused by beta-lactamase (penicillinase) producing bacteria.

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Sulbactam/cefoperazone (SBT/CPZ) was used in pediatric patients with acute infections, and the following results were obtained.
SBT/CPZ was administered to 18 pediatric patients with acute infections. Out of them, 14 patients, i.e., 3 with acute tonsillitis, 1 with acute laryngitis, 1 with acute bronchitis, 4 with acute pneumonia, 4 with bronchopneumonia, 1 with pyothorax, were adopted for the evaluation, and the other 4 were excluded because they were judged inadequate for clinical efficacy evaluation. The clinical efficacy of SBT/CPZ was assessed as excellent in 4, good in 9 and fair in 1. The effective rate was 92.9%.
In 6 cases causative organisms were detected, i.e., Haemophilus influenzae in 3, Klebsiella in 1 and Staphylococcus aureus in 2 cases. Eradication of these organisms was confirmed in all cases except for 1 patient with pyothorax caused by S. aureus. The doses used in 12 out of the evaluated 14 cases ranged from 58.4 to 80 mg/kg/day, 84.1 mg/kg/day was used in 1 case and 101.4 mg/kg/day was used in 1 case with pyothorax. Patients with severe infections were generally given large doses. The frequency of administration was 3 times per day except 1 case, and intravenous drip infusion was used in all cases. The duration of treatment was 2-<3 days for 7 cases, 3-5 days for 6 cases and 9 days for 1 case (pyothorax).
No clinical side effects were observed in any case. In laboratory examinations, a slight elevation of GOT was observed in 1 case, but no abnormal findings in the other cases.
From the above results, SBT/CPZ was considered to be a highly useful drug in the treatment of pediatric infections.

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Sulbactam, a new β-lactamase inhibitor, in combination with cefoperazone was administered to 18 pediatric patients, 7 months to 10 years 6 months of age, at a daily dose of 56-320 mg/kg divided into 4 times by intravenous bolus infusion for 3 to 11 days, and the sum of 2.6-74.0g of the drug was given.
A total of 18 cases comprised 8 with RTI, 1 with gastric tract infection, 4 with UTI and 5 with sepsis (suspected).
Clinical efficacy was excellent in 10 cases, good in 3 cases, fair in 1 case and poor in 4 cases, and efficacy rate was 72.2%.
Out of 8 strains (1 of S. aureus, 1 of P. aeruginosa, 1 of Salmonella subgenus I, 2 of E. colt, 2 of P. mirabilis and 1 of K. pneumoniae), possible causative organisms isolated before the treatment, 6 strains were disappeared, 1 strain of K. pneumoniae persisted, and 1 strain of P. aeruginosa was replaced by S. aureus.
Diarrhea was noted in 1 case as subjective side effect, and as abnormal laboratory findings, GOT and GPT elevations in 1 case, GPT elevation in 1 case and eosinophil elevation in 1 case were observed.

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Sulbactam/cefoperazone (SBT/CPZ), a fifty-fifty combination of a β-lactamase inhibitor, SBT, and an already marketed broad spectrum cephalosporin, CPZ, was evaluated for its efficacy and safety in 25 children. The diagnoses included purulent lymphadenitis, pneumonia, acute UTI, bacteremia and purulent meningitis. SBT/CPZ was effective in all the 20 cases with bacterial infections, but strains highly resistant to CPZ were not isolated in this study.
The serum and cerebrospinal-fluid levels of SBT were grossly parallel with those of CPZ, and the half-life of the serum SBT was 0.754 hour. Although severe adverse reactions were not encountered with SBT/CPZ therapy, loose stools in 20% and diarrhea in 16% of the cases were observed.

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Fundamental and clinical studies were carried out on sulbactam/cefoperazone (SBT/CPZ) in the field of pediatrics. The following results were obtained:
1. A total of 185 clinical isolates that had been stocked at our department was employed to determine the minimum inhibitory concentrations (MICs) of SBT/CPZ against various bacterial species. SBT/CPZ showed strong antibacterial potency against E. coli, Salmonella, Klebsiella and P. mirabilis, and relatively strong potency against S. marcescens, P. aeruginosa and S. aureus.
2. Antibacterial potency of SBT/CPZ was stronger than that of CPZ alone against E. coli, and it also showed strong activity against strains of Salmonella, S. marcescens and S. aureus, moderately or highly resistant to CPZ.
3. SBT/CPZ was administered by intravenous bolus infusion to pediatric patients to determine the serum concentrations of SBT and CPZ. At a dose of 10mg/kg the mean serum levels of SBT and CPZ were as follows; 17.8 μg/ml, 40.7μg/ml at 15 minutes and 0.3μg/ml, 3.0μg/ml at 6 hours, respectively. The half-lives of SBT and CPZ in the serum were 1.05 hours and 1.76 hours, respectively.
Similarly, at a dose of 20mg/kg the mean serum levels of SBT and CPZ were; 31.9μg/ml, 81.0μg/ml at 15 minutes and 0.5μg/ml, 6.1μg/ml at 6 hours, and the half-lives were 1.00 hour and 1.72 hours, respectively.
At a dose of 40mg/kg, only 1 case was determined. The serum levels of SBT and CPZ were 34.4μg/ml, 74.8μg/ml at 30 minutes and 0.2μg/ml, 3.7μg/ml at 6 hours, and the half-lives were 0.78 hour and 1.38 hours, respectively.
4. SBT/CPZ was drip-infused intravenously over a period of 1 hour, and the serum concentrations of SBT and CPZ were determined.
At the dose of 10mg/kg or 20mg/kg, the peak serum levels of SBT and CPZ were observed at 1 hour or at the end of drip infusion.
At a dose of 10mg/kg the mean serum levels of SBT and CPZ were 14.4μg/ml, 33.7μg/ml at 1 hour and 1.4μg/ml, 4.6μg/ml at 7 hours, respectively. The half-lives was 1.86 hours for SBT and 2.23 hours for CPZ, respectively. Similarly at a dose of 20mg/kg, the mean serum levels of SBT and CPZ were, 22.2μg/ml, 34.6μg/ml at 1 hour and 0.5μg/ml, 2.8μg/ml at 7 hours, and the half-lives was 1.17 hours and 1.75 hours, respectively.
5. The urinary recovery rate was determined for the 6 hours period after admistration. The urinary recovery rate were approximately 30-60% for SBT and 10-20% for CPZ.
6. SBT/CPZ was administered to 11 cases with bacterial infections. A good or excellent clinical effectwas seen in the 10 cases (91%).
7. The bacteriological effect of SBT/CPZ was investigated in 7 strains of 4 cases.
All strains were eradicated, a 100% bacteriological eradicated rate. A total of 7 strains comprized 1 of E. coli, 1 of P. mirabilis, 1 of P. vulgaris, 1 of P. aeruginosa, 1 of H. influenzae and 2 of S. aureus. Each one of E. coil, P. vulgaris, H. influenzae and S. aureus was β-lactamase producing organism.
8. The following side effects to the SBT/CPZ therapy were recorded; 2 cases of diarrhea, 1 case of eosinophilia and 1 case of prolongation of PT and APTT.

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Clinical trials were carried out with sulbactam/cefoperazone (SBT/CPZ)(combination ratio of 1:1) in pediatric infections. Results were as follows.
1. The mean half-lives of SBT and CPZ in the serum following intravenous injection of SBT/CPZ were about 0.7 and 1.2 hours, respectively.
2. Urinary excretions of SBT and CPZ within 6 hours after intravenous injection of SBT/CPZ were 81.9% and 28.1%, respectively.
3. SBT/CPZ was administered to 33 pediatric patients with various infection; 18 respiratory tract infections, 12 urinary tract infections and 3 Salmonella enterocolitises. The overall efficacy rate was 87.9%. In particular, 7 of 8 urinary tract infections caused by,β-lactamase producing organisms were improved after administration of SBT/CPZ.
4. Diarrhea in 8 and soft stool in 3 of 33 patients occurred, and slight elevation of GOT/GPT was observed in 2 patients.

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Microbioligical, pharmacokinetic and clinical studies on sulbactam/cefoperazone (SBT/CPZ) were carried out in the field of pediatrics.
1. Antimicrobial activity
The MIC80 of SBT/CPZ was 6.25μg/ml for clinically isolated 24 strains of S. aureus (24β-lactamase producing strains), 0.39μg/ml for 17 strains of S. pyogenes, 3.13μg/ml for 24 strains of E. coli (22 p-lacta-mase producing strains), 3.13μg/ml for 22 strains of K. pneumoniae (22 β-lactamase producing strains), 1.56μg/ml for 22 strains of P. mirabilis and 0.20μg/ml for 15 strains of H. influenzae (13 β-lactamase producing strains). In comparison with CPZ in respect to the MIC, SBT/CPZ exhibited synergistic effect on 31 strains out of 81 g-lactamase producing strains (included 6 strains of S. aureus, 9 of E. coli, 5 of K. pneumoniae and 11 of H. influenzae) which was scarcely observed against 43 non-β-lactamase producing strains.
2. Absorption and excretion
Serum levels and urinary excretion of SBT/CPZ were studied in 7 children aged 5 to 12 years.
The mean serum concentration of SBT at 15 minutes following a single intravenous injection of 10mg/kg of SBT/CPZ was 14.2μg/ml and that of CPZ was 30.4μg/ml. The mean urinary recovery rates at 6 hours following the intravenous injection were 57.8% and 18.3%, respectively. The mean serum concentrations of SBT and CPZ after 1-hour infusion of 10mg/kg of SBT/CPZ were 10.9μg/ml and 17.6μg/ml, respectively. The urinary recovery rates of SBT and CPZ at 7 hours after the infusion were 100.0% and 27.7% on average, respectively. The mean serum levels of SBT and CPZ at 15 minutes after a single intravenous injection of 20mg/kg of SBT/CPZ were 25.6μg/ml and 66.0μg/ml, respectively and urinary elimination until up to 6 hours were 72.5% on average for SBT and 21.1% for CPZ.
3. Clinical study
SBT/CPZ was used for the treatment of a total of 20 pediatric patients aged 1 month to 14 years to evaluate its clinical effectiveness, bacteriological efficacy and adverse effects.
The clinical efficacy in 6 patients with acute pneumonia, 3 with staphylococcal scalded skin syndrome, 2 each with acute purulent tonsillitis and acute pyelonephritis, 1 each with acute purulent lymphadenitis, acute sinusitis, acute bronchitis, peritonitis and acute enteritis was judged to be excellent in 15 cases and good in 3 cases with an efficacy ratio of 100%. The clinical efficacy in 6 patients whose infections were caused by β-lactamase producing strains was judged to be excellent in all the cases.
The bacteriological efficacy of SBT/CPZ was assessed on 5 strains of S. aureus (5 p-lactamase producing strains), 5 strains of H. influenzae (5 non-β-lactamase producing strains), 1 non-β-lactamase producing strain of H. parainfluensae, 2 strains of E. coli (1 β-lactamase producing strains) and 1 non-β-lactamase producing strain of S. thompson. All strains except for 1 strain each of S. aureus and S. thompson which decreased in number or reappeared after once eradicated were eradicated with a bacteriological eradication rate of 85.7%.
Only a patient complained of fever which is suspected to be related to the drug. No other side effect was reported. An elevation of GOT and GPT was observed in 3 patients and eosinophilia in 2 but all returned to normal after withdrawal of the drug or with continued therapy.

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The authors have carried out the laboratory and clinical studies of sulbactam/cefoperazone (SBT/CPZ) and obtained the following results.
The antibacterial activities of SBT/CPZ against the clinical isolates of S. aureus, E. coli, K. pneumoniae, E. cloacae, E. aerogenes, S. marcescens, P. aeruginosa were measured by the plate dilution method with inoculum size of 106 cells/ml.
The susceptibility distribution of S. aureus to SBT/CPZ ranged from 0.39 to 6.25μg/ml, and the peak of distribution was 1.56μg/ml.
The peak of susceptibility distribution of K. pneurnonlae was 0.20μg/ml, and the distribution of E. coli and E. aerogenes ranged from 0.10 to 12.5μg/ml and that of S. marcescens, from 0.2 to 25μg/ml
The growth of 80.8% of P. aeruginosa was inhibited at the concentration of 12.5μg/ml.
The distribution of E. cloacae ranged from 0.1 to 50μg/ml.
For pharmacokinetic study, SBT/CPZ was given in a single dose of 20mg/kg by drip infusion for 1 hour in 2 children and 40mg/kg by drip infusion for 1 hour in 1 children.
With drip infusion of SBT/CPZ, the peak serum level were 17.8/43.9μg/ml, 21.8/75.5μg/ml on completion of the infusion, respectively.
SBT/CPZ was effective in 14 cases out of 16 cases with clinical effect.
No side effect was observed except for eosinophilia in 1 case.

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We conducted several studies using a combination of sulbactam (SBT) and cefoperazone (CPZ) in a ratio of 1:1 with the following results.
1. Serum and cerebrospinal fluid (CSF) concentrations of the drugs were determined in 2 rabbits with meningitis caused by S. aureus.
Following intravenous injection, serum concentrations of CPZ were higher than those of SBT in both rabbits whereas CSF concentrations were much higher with sulbactam than with CPZ indicating good penetrability of SBT into CSF.
2. The serum concentration of SBT at 1/2, 1, 2 and 4 hours after an intravenous administration of 9.8mg/kg of the combination to a child were 3.5, 1.4, 0.3 and 0.1μg/ml and those of CPZ 19.0, 13.0, 6.7 and 2.9μg/ml, respectively. The half-lives were 0.705 hours for SBT and 1.31 hours for CPZ.
3. An intravenous dose of this combination (19.6mg/kg) was given 3 times a day to 13-year-old girl with decreased neutrocyte chemotaxis due to periblepharal abscess caused by S. aureus. The therapeutic effect was excellent. Though very slight transient eosinophilia was noted, no adverse reaction was found. The susceptibility of the isolated organism to this drug was not determined, but it was found to be resistant to the CTX using the disc method.

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To 6 cases of children in 2 groups of 3 each, newly developed sulbactam/cefoperazone (SBT/CPZ) was given at 20 and 40mg/kg by intravenous bolus injection, respectively, and the serum and urinary concentrations and recoveries of SBT and CPZ were determined. To 1 case of purulent meningitis, this drug was given at 40mg/kg by intravenous bolus injection, and the cerebrospinal fluid and serum concentrations of SBT and CPZ were determined. Susceptibility tests to SBT/CPZ and CPZ of total 289 strains were conducted; Gram-positive cocci tested consisted of 26 S. aureus strains, 20 S. pyogenes strains and 21 S. pneumoniae strains, and Gram-negative bacilli consisted of 24 H. influenzae strains, 22 E. coli strains, 26 K. pneumonlae strains, 24 E. cloacae strains, 21 E. aerogenes strains, 19 Citrobacter sp. strains, 20 S. marcescens strains, 23 P. mirabilis strains, 23 indole-positive Proteus sp. strains and 20 P. aeruginosa strains. SBT/CPZ was given to total 43 cases at a mean daily dosage of 80.4mg/kg, in 3 or 4 divided doses (6 cases in 3 and 37 cases in 4), 1 case receiving the drug by drip infusion over 30 minutes (in 3 divided doses) and all the other 42 cases by intravenous bolus injection, for 7 days on an average. They consisted of 2 cases of tonsillitis, 1 case of otitis media, 1 case of otitis media associated with mastoiditis, 30 cases of pneumonia, 1 case of suspected septicemia, 1 case of purulent meningitis, 5 cases of urinary tract infection, 1 case of purulent lymphadenitis and 1 case of submaxillaritis. And the clinical and bacteriological effects were evaluated. Also, side reactions and laboratory examinations for abnormal values due to administration of this drug were made on 47 cases including 4 drop-outs. The following results were obtained:
1. After administration of this drug to 2 groups of 3 children each at 20 and 40mg/kg by intravenous bolus injection, mean serum concentrations of both SBT and CPZ reached the peaks in 5 minutes; SBT levels were 60.9 and 124.7μg/ml for the 2 groups and CPZ levels were 105.0 and 214.1μg/ml, respectively. In either group, CPZ levels were 1.7 times as high as SBT levels, and there was observed a dose-response in both. In the 20mg/kg group, mean half-lives of SBT and CPZ were 0.96 and 1.24 hours, respectively, and in the 40mg/kg group, they were 1.01 and 1.32 hours, CPZ values tending to be longer.
2. In the above 2 groups given SBT/CPZ by intravenous bolus injection, mean urinary SBT and CPZ concentrations reached the peaks in 0-2 hours after administration. The 20mg/kg group showed 1,583.3μg/ml for SBT and 323.4μg/ml for CPZ, while the 40mg/kg group did 4, 103.3 and 1, 178.1μg/ml, respectively. In the 20mg/kg group, recovery rates of SBT and CPZ up to 6 hours were 62.1 and 14.3%, respectively, and in the 40mg/kg group these figures were 73.4 and 26.4%. The recovery rates of CPZ were lower than those of SBT in both groups.
3. To 1 case of purulent meningitis, SBT/CPZ was given at 40mg/kg by intravenous bolus injection on 7, 12 and 19 sick-days. And the cerebrospinal fluid and serum concentrations were determined at 1 hour after administration on each day. The cerebrospinal fluid levels of SBT were 3.2, 0.8 and 0.5μg/ml and those of CPZ 2.1, 1.6 and 1.3μg/ml on 7, 12 and 19 days of illness, respectively. That is, the levels of both drugs decreased in the cerebrospinal fluid coincided with the improvements and thus the cerebrospinal fluid-serum ratios of SBT stood at 23.4, 5.7 and 2.2% and those of CPZ at 6.2, 4.2 and 1.5%, respectively.
4. Susceptibility tests to CPZ and SBT/CPZ of 289 clinically isolated strains revealed that MICs of SBT/CPZ against 26 S. aureus strains were inferior overall to those of CPZ, but none of the strains tested gave more than 100μg/ml as some did to CPZ. MICs of SBT/CPZ against 20 S. pyogenes strains and 21 S. pneumoniae strains were two-fold higher to those of CPZ.

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The combined antibiotics, sulbactam/cefoperazone (SBT/CPZ), was administrated intravenously to 10 patients with various kinds of gynecological infectious diseases and the efficiency of the drug was investigated clinically or bacteriologically. The results obtained were as follows.
1. The clinical and bacteriological efficiency rate of SBT/CPZ on gynecological infectious diseases was determined as about 100 per cent and 75 per cent.
2. Three species out of 11 isolated bacteria produced β-lactamase. Two cases out of 3 β-lactamase positive bacteria were disappeared in the materials obtained from the patients after the treatment of the drug.
3. No remarkable side effect except for 1 buccal exanthema and 1 genital candidasis was detected during the administration course of the drug.

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Sulbactam (SBT)/cefoperazone (CPZ) is the combined drug of SBT (β-lactamase inhibitor) and CPZ by 1 to 1 to get spectrum covering much wider range than CPZ only.
SBT/CPZ was used in 6 cases of female intrauterine and intrapelvic infections and 3 cases of external genital infections.
The clinical efficiency was almost good excluding adnexitis. There were neither subjective and objective side effects nor abnormal laboratory findings.

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A daily dose of 2 or 4 grams of sulbactam/cefoperazone (SBT/CPZ) by drip infusion was given to 12 patients with gynecoobstetrical infections and the results were followings:
The clinical effect was judged excellent in 2 cases, good in 9 cases and poor in 1 case, and the effective rate was 91.7%.
Except for Streptococcus faecalis, the bacteriological effect was sufficient. A good effect was also seen in Pseudomonas cepacia resistant organism to other cephem antibiotics.
Diarrhea was observed in 1 patient, and increases of GOT and GPT, possibly attributable to concomitantly used anticancer agent, were detected in another patient.
In conclusion, SBT/CPZ with a 91.7% of efficacy rate, was useful in infections caused by β-lactamase producing organisms and, thus, a useful agent for gynecoobstetrical infections.

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Sulbactam/cefoperazone (SBT/CPZ) was studied for clinical efficacy in the field of obstetrics and gyneco-logy, and following results were obtained:
1. In the treatment of 6 cases of gynecological infection, the clinical efficacy of SBT/CPZ was assessed as excellent in 1 case and effective in 5 cases.
2. Neither adverse effects nor abnormalities in laboratory findings due to SBT/CPZ were observed.
Based on these results, SBT/CPZ is considered to be a highly effective antibiotic with clinical efficacy in obstetric and gynecological infections in the daily dosage of 2 g given in two divided doses.

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A combination of sulbactam, a β-lactamase inhibitor, plus cefoperazone (SBT/CPZ=1/1) was studied in the field of obstetrics and gynecology, and the results were followings:
1. Absorption and transfer into genital organ tissues were good. With the 1 g intravenous injection the maximum serum concentrations in the uterine artery were 88. 6ug/ml for CPZ and 50. 0ug/ml for SBT, and the maximum tissue concentrations were 12. 2-17. 4ug/g for CPZ and 9. 8-21. 4ug/g for SBT. When the 2g was administered, the maximum tissue concentrations were 11. 9-26. 7ug/g for CPZ and 6. 0-8. 0ug/g for SBT. These elimination showed the similar trend as their serum levels, and their tissue levels were higher than MIC₈₀ for the main organisms.
2. Their penetration into the intrapelvic dead space exudate was also good and showed that the peak levels were 30. 1ug/ml for CPZ and 17. 4ug/ml for SBT at 2 hours after the 2 g intravenous injection. The peak levels of 34. 4ug/ml for CPZ and 8. 8ug/ml for SBT at 6 hours after 2g intravenous drip infusion were obtained. Their elimination was slow, and the concentration higher than MIC₈₀ for main organisms was maintained for a long period of time.
3. For gynecoobstetrical infections such as adnexitis, intrauterine, intrapelvic and external genital organ infections, a daily dose of 2-4g of SBT/CPZ produced a 100% clinical efficacy in 10 patients and a 88. 9% bacteriological effect. The eradication ratio was more than 80% against β-lactamase producing organisms. Side effects were few.
4. The above results indicated that SBT/CPZ was useful in the field of obstetrics and gynecology.

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The tissue penetration of sulbactam/cefoperazone (SBT/CPZ) was studied. The drug was also used in the treatment of 3 patients with gynecoobstetrical infection. The results of these studies are summarized as follows.
1. The elbow venous blood concentration and uterine arterial blood concentration were in about the same level and diminution curve of their concentrations took also a similar pattern.
2. The tissue levels of the uterus and uterine appendices were determined and found to be high in the portio vaginalis, myometrium and oviduct.
3. Each of the 3 patients with whom the dead space fluid concentration was determined showed her own concentration curve.
4. SBT/CPZ was administered to 2 patients with adnexitis and 1 patient with pelvic peritonitis, and was markedly effective in 2 patients and moderately effective in other 1 patient.

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Sulbactam/cefoperazone (SBT/CPZ) was administered to 19 patients with various infections in the field of obstetrics and gynecology. The clinical efficacy was judged as excellent in 1 case and as good in 16 cases; hence, the efficacy rate was 89.5%. SBT/CPZ was not effective in a patient with end-stage carcinomatous peritonitis and nor in a patient with pyosalpinx caused by E. coli and Peptococcus magnus.
Except a case by E. coli, SBT/CPZ was highly effective for pyosalpinx and pelvic peritonitis where E. coli or K. pneumoniae was the causative organism.
No side effects were observed.

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One or 2 grams of sulbactam/cefoperazone (SBT/CPZ) in 250ml of 5% glucose solution was administered twice daily by drip infusion to 10 patients with female genital organ infections.
The clinical effectiveness was seen in 8 patients but not in 2 patients associated with emergence of replaced organism or non-eradicated causative organism.
Antibacterial activity of SBT/CPZ vs. CPZ in the 20 clinical isolates revealed that SBT/CPZ was 1 or 3 tubes superior to CPZ alone in the β-lactamase producing organisms, but, 1 or 2 tubes inferior to CPZ in the β-lactamase non-producing organisms.
In 1 case increases in GOT and GPT, and in another increases in GOT and GPT, and a decrease in platelets were observed even though their degrees were mild.

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Sulbactam (SBT), a new β-lactamase inhibitor, in combination with cefoperazone (CPZ) was studied for the clinical evaluation in the field of obstetrics and gynecology.
SBT/CPZ was given to 6 cases with the following infections; 4 of pyometra, 1 of Doumws-abscess and 1 of pelvic cellulitis. Five cases were old patients accompanied by cancers, and 2 cases were refractory to other antibiotics therapy.
The clinical efficacy was excellent in 1 case, good in 3 cases, poor in 2 cases.
No side effects nor abnormal laboratory findings associate with the agent were observed.

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