The authors have carried out the laboratory and clinical studies of cefuroxime(CXM). The results were as follows:
The sensitivity was measured by plate dilution method on 26 strains ofS. aureus, 22 strains ofE. coiland 24 strains ofK. pneumoniaeisolated from patients. The distribution of sensitivity ofS. aureus was 0.78-3.13μg/ml and the peak of distribution was 1.56μg/ml. The distribution of sensitivity of E. coliwas 1.56-50μg/ml and the peak was 6.25μg/ml. The growth of 79.2%K. pneumoniaewas inhibited in concentration of less than 3.13μg/ml.
CXM was given intravenously for 30 minutes at a single dose of 20 mg/kg to 3 children.
The serum mean levels of CXM were 99.0±10.6μg/ml at 30 minutes, 18.0±10.7μg/ml at 1 hour, 7.0±2.0, 2.2±0.6, 0.79±0.2μg/ml at 2, 4 and 6 hours after drip infusion for 30 minutes, respectively. Mean half life was 48 minutes.
The mean urinary recovery rate was 96.2% up to 8 hours after administration.
CXM was effective in 9 of 10 cases of bacterial infections. No side effect was observed except for 1 case with elevation of serum transaminase.

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Fundamental and clinical studies were made on cefuroxime, a new cephalosporin, and the following results were obtained.
(1) Antibacterial activity of the drug against 15 strains of Staphylococcus aureus was almost equal to that of cefazolin. Although cefazolin was superior against 33 strains of E. coli to cefuroxime, the latter tended to have a higher antibacterial activity against the strains with higher MIC to cefazolin. Based on the studies with 6 strains of Klebsiella pneumoniae, 43 of Klebsiella oxytoca and 12 of Proteus, it was suggested that cefuroxime was more stable to β-lactamase than cefazolin. Both cefuroxime and cefazolin had MICs of more than 100μg/ml against 3 strains of Enterobacter, 2 of Citrobacter and 9 of Pseudomonas aeruginosa.
(2) Passage of the drug into the cerebrospinal fluid (CSF) was evaluated in experimental staphylococcal meningitis in rabbits. The average maximal CSF concentration of the drug in 4 rabbits was 2.90±0.75μg/ml (45 minutes after a one-shot intravenous injection of 100mg/kg). The area under the curve (AUC) of the CSF concentration up to 3 hours was 282.08 min ·μg/ml, CSF/serum ratio of the AUC 12.6%, and T1/2 of the CSF concentration 69.1 minutes which was 3.31 times as high as that of the blood, respectively. The longer T1/2 of the CSF appeared to be the merit of cefuroxime.
(3) Two children received a single intravenous drip infusion of the drug, 26.8 mg/kg and 29.1 mg/kg, respectively, over a30-minute period and the blood concentrations determined. They were highest at the end of the infusion, i.e., 55μg/ml and 105μg/ml, declined rapidly thereafter, and were 0.82μg/ml and 1.45μg/ml 4 hours after the end of the infusion, T1/2 being 41.1 minutes and 41.7 minutes, respectively.
(4) Four children, each two of pneumonia and empyema, were treated with71.4-87.2 mg/kg of the drug by a 30-minute drip infusion divided in three doses. An overallefficacy rate was 75%, i.e., excellent in two cases of pneumonia, good in one case of empyema and failure in another case of empyema.
(5) One patient with empyema initially complained of a vascular pain by one-shot intravenous injection but offered no complaints when it was switched to a 30-minute drip infusion. Except for this, no adverse reactions related to cefuroxime injection were recognized.
(6) Based on the above results, it was concluded that cefuroxime is a potent new antibiotic in the treatment of respiratory tract infection in children. Pharmacokinetic studies also suggested its usefulness in urinary tract infection. Based on the studies on experimental meningitis in rabbits, cefuroxime was expected to be a potent antibiotic in the treatment of ampicillin-resistant Haemophilus influenzae meningitis but further investigations will be required to establish its indication.

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The general pharmacological properties of cefadroxil which is a new semisynthetized cephalosporin were examined and following results were obtained.
1) Cefadroxil had no appreciable influences on the central nervous system in mice and the EEG in cats.
2) Cefadroxil had no effects on the isolated smooth muscle organs.
3) Cefadroxil had no effects on the passage of charcoal meal in mice and the motility of the stomach in situ in rabbits.
4) Cefadroxil inhibited the gastric secretion in pylorus-ligated rats.
5) Cefadroxil induced no marked changes in the respiration, blood pressure, heart rate, electrocardiogram and femoral blood flow in anesthetized dogs. Cefadroxil had no effects on the isolated hearts and ear vessels of rabbits.
6) Cefadroxil decreased the urine volume and the excretion of electrolytes (Na⁺, K⁺ and Cl^-) in first three hours in rats.
7) Cefadroxil increased the biliary secretion in rats.
No significant effects of cefadroxil were found in the other pharmacological experiments.

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Cefoxitin was given to the 7 patients of infections in the field of obstetrics and gynecology, and the following results were obtained:
1) The clinical response was excellent in 2 patients, good in 4 and poor in 1 patient with the efficacy rate of 85.7%. Out of the 4 patients resistant to the previous therapy with other antibiotics, 3 patients responded to cefoxitin, and all the 3 patients of anaerobic infections responded satisfactorily to cefoxitin.
2) Microorganisms isolated were 2 strains each of E. coli and Staphylococcus aureus, 3 strains of Peptococcus and 1 strain of Eubacterium lentum. All the 8 strains isolated were sensitive to cefoxitin. As to bacteriological response, all the strains isolated were eradicated except 1 strain of Staphylococcus aureus whichrecurred on the 9th day after completion of the therapy with the eradication rate of 87.5%.
3) No subjective nor objective side effects were noted. Especially, the elevated GOT and GPT observed on a patient complicated with hepatitis prior to the initiation of cefoxitin treatment were found to be normal upon completion of the treatment.

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Using 6 healthy adult male volunteers, who were devided in halves, the serum and urinary levels of cephaloridine were determined during and after 2-hour constant drip infusion of 2 g cephaloridine dissolved in 500 ml physiological saline solution (=Group I) and 1-hour constant drip infusion of 1.5g solution (=Group II); besides, pharmacokinetic analysis was made for one-compartment and twocompartment models.
On the basis of the values of serum levels obtained from this trial, pharmacokinetic parameters were calculated and simulation curves of serum levels for various doses (0.5-2g) and duration (1-4 hours) of cephaloridine drip infusion were drawn.

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