[in Japanese]

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Cefsulodin (CFS), a new antipseudomonas cephalosporin, was clinically evaluated for treatment of the Pseudomonas aeruginosa infections in the surgical field to obtain the following results.
1. CFS was administered to total 11 cases of the surgical infections caused by P. aeruginosa, comprising of 5 cases with wound infections, 3 cases with infected burn and 1 case each with muscular abscess, decubitus and postoperative pneumonia in 0.5-1 g twice a day by intravenous bolus or drip infusion. Good clinical responses were obtained in 9 out of 11 cases (81.8%).
2. Bacteriological responses were observed in all cases. P. aeruginosawas eradicated in 9 cases and suppressed in 2 cases by CFS treatment. However, replacement of pathogens with the other organisms was observed in 6 out of 8 cases caused by P. aeruginosa only.
3. Neither objective and subjective side effects nor abnormalities of laboratory tests associated with CFS treatment were observed.
4. It can be, therefore, concluded that CFS is one of the useful drugs for treatment of the surgical infections caused by P. aeruginosa.

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Reproduction studies on ceftizoxime sodium (CZX-Na) were performed in JCL: SD strain rats according to the guidelines issued by the Japanese Ministry of Health and Welfare (1975). The does levels in each study were 100,320 and 1,000 mg/kg.
1. Fertility study
CZX-Na was given subcutaneously to males for 63 days and to females for 14 days before pairing the animals for mating. The dosing was continued for males until mating was observed, and for females throughout the mating period and until day 7 of gestation. All females were killed on day 21 of gestation to investigate litter parameters and abnormalities of fetuses. There were noabnormal signs in any treated males and females throughout the dosing period, except soft feces in a few animals given the largest does of 1,000 mg/kg. Body weight gain and food consumption of the treated males and females were almost the same as those of the control during the dosing period. Almost all the pairs mated within 6 days, and there were no intergroup differences in pregnancy rates.
At laparotomy on day 21 of gestation, there were no litter abnormalities, or external, internal or skeletal variants in fetuses of any treated animals.
2. Teratogenicity study
CZX-Na was given subcutaneously to pregnant animals from day 7 to day 17 of gestation. Two thirds of the females in each group were killed on day 21 of gestation to investigate litter parameters and abnormalities of fetuses. The remaining females were allowed to give birth, and the pups were examined for postnatal development.
There were no abnormal signs in any treated dams, except soft feces in a few animals of the treated groups during the dosing period. At laparotomy on day 21 of gestation, there were no litter abnormalities, or external, internal or skeletal variants of the fetuses. Gestation and delivery were normal in all treated dams allowed to give birth.
Mortality, growth, differentiation, behavior, and external and internal abnormalities of pups in the treated groups were almost the same as those in the control during lactation and after weaning. The reproductive performance in the F₁ generation was normal and there were no litter abnormalities, or external, internal or skeletal variants attributable to the treatment.
2. Peri-and post-natal study
CZX-Na was given subcutaneously to pregnant animals from day 17 of gestation to day 21 post partum. All pregnant dams were allowed to give birth, and the pups were examined for postnatal development.
There were no abnormal reactions to the treatment in any treated dams during gestation and lactation. The mean duration of gestation was 22 days in all the groups including the control, and labor and delivery were normal in all animals. Mortality, growth, differentiation, behavior, and external and internal abnormalities of pups in the treated groups were almost the same as those in the control during lactation and after weaning. The reproductive performance in the F₁ generation was normal and there were no litter abnormalities, or external, in ernal or skeletal variants.
The results in reproduction studies led to the conclusion that CZX-Na produced no adverse effects on fertility of fetal development, and the reproductive performance of the F₁ animals was normal even at the largest subcutaneous dose of 1,000 mg/kg.

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In vivo transfer and therapeutic efficacy of a new cephalosporin derivative, cefotaxime, which is stable against beta-lactamase hydrolysis, have studied in gynecology field.
The following results have been obtained.
(1) The level of cefotaxime transfered to uterus artery and to uterus was higher than its MIC against majority of Gram-negative bacilli, such as E. coli.
(2) Transfer of this drug to umbilical blood was also satisfactory.
(3) This drug as demonstrated its efficacy in treating 8 infection cases refractory to CET, CEZ and ABPC, out of which I had ‘excellent’ and 5 had ‘good’ results.
(4) No side effect was evidenced in any of our patients.
In conclusion, this drug has satisfactory tissue transfer as well as sufficient safety and excellent efficacy in treatment of gynecological infection cases.

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Following results were obtained from intravenous single administration of cefotaxime 2 g by measuring its levels in uterine arterial blood, elbow venous blood, ovary, oviduct, several sites in uterine tissue, and in the fluid excreted in the dead space formed by radical hysterectomy.
(1) Uterine artery and elbow vein blood levels revealed marked increase immediately after administration followed by gradual reduction at slow rate.
(2) Peak levels in female internal genital organ tissue were achieved 12-19 minutes after cefotaxime administration, and ranged between 5 to 8 mcg/g independently from measurement site. In cervix uteri, portio vaginalis high concentration of 4.9-5.7 mcg/g was achieved within ten minutes after drug administration.
(3) In the fluid excreted in the dead space formed by radical hysterectomy cefotaxime levels were maintained around 15 mcg/ml level throughout 5-6 hours following its administration, and gradually decreased at slow rate later.

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Ten cases of gynecological infection were treated successfully by a new cephalosporin derivative, cefotaxime (HR 756, CTX), which proved excellent in 4 cases and good in 6 cases. No adverse reaction was found to be induced by administration of this drug. Post-administration results were all normal for both renal and hepatic function tests.
It is extremely difficult to accurately assess bacteriological efficacy of a drug in treatment of female genital infections. Nevertheless, we determined its MICs for a few number of strains we could isolate from clinical cases. Its MIC against 4 strains of B. fragilis inoculated at 10⁸ cells/ml was 25-50 mcg/ml and was 1.56-3.13 mcg/ml at 10⁸ cells/ml inoculation. Its MIC against 2 strains of Ps. cepacia was 12.5 mcg/ml at 10⁸ cells/ml inoculation and 6.25 mcg/ml at 10⁸ cells/ml inoculation. These MICs suggest that this drug is a very promising antimicrobial agent for treatment of gynecological infections, as been already indicated by clinical results of this drug.

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The following results have been obtained in our basic and clinical studies to examine a new cephalosporin derivative, cefotaxime (CTX).
For basic study purpose, we injected 1g of CTX to 6 patients who had received simple total hysterectomy and measured its level in elbow vein, uterine artery, corpus uteri, cervix uteri, endometrium, oviduct and ovary.
Any definitive conclusion should not be drawn from these results, since they have too big variation. However, slightly higher levels were achieved cervix uteri and oviduct than in other organs in a same patient.
For clinical evaluation, we tried this drug to 12 cases of female genital infections and 91.7% response rate was obtained.
Our studied population includes 8 cases of adnexitis, 2 with pelveoperitonitis, 1 with panperitonitis, and 1 patient with BARTHOLIN abscess. Organisms were detected only in 3 cases, including S. aureus in one patient, Micrococcus sp. in one, and mixture of Klebsiella sp. and B. fragilis in 1. Puncture of DOUGLAS pouch was performed in 3 cases after the completion of therapy and all had negative results.
No side effect was observed, and no significant difference was noted between pre-and post-therapy examinations of peripheral blood, hepatic function and renal function.

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Therapeutic efficacy and safety of a new cephalosporin for injection, cefotaxime (CTX) have been examined in gynecological infection cases.
CTX has demonstrated in this study excellent therapeutic efficacy in infections with aerobes only, sanerobes only and with mixture of aerobes and anerobes.
No side effect has been observed in our patients who had been administered total dose of 8-28g during the period of 4-7 days.

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Fundamental and clinical studies of cefotaxime (CTX), a new semisynthetic cephalosporin antibiotic were carried out in the field of obstetrics and gynecology. The following results were obtained.
1. CTX was almost equally active to SCE-1365 and less active than cefotiam (CTM) and cefazolin (CEZ) against S. aureus, much more active than these 3 antibiotics against E. coli, more active than the 3 antibiotics against Enterobacter, equally active to SCE-1365 and a little weaker than CEZ against anaerobic Gram positive cocci, and superior to SCE-1365 and CEZ against Bacteroides.
2. CTX was more stable to B. fragilis-producing β-lactamase than CET, CEZ and cefoperazone (CPZ).
3. The concentrations of CTX transfered to the female genital organs after CTX 1g d. i. were sufficiently effective against facultative or strict anaerobic bacteria mainly isolated from obstetrical and gynecological infections.
4. CTX was administered to 10 patients with genital infections. CTX was excellent in 1 case, good in 8 cases and poor in 1 case. The response rate of CTX was 90%. Bacteria, isolated in 5 cases before CTX treatment, were eradicated in 4 cases. The bacteriological effectiveness of CTX was thus 80%.
5. No side effect attributable to CTX was observed.

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Fundamental and clinical studies were made on cefotaxime (HR-756, CTX), a new cephalosporin antibiotic, with the following esults.
1. Cefotaxime was given to 22 patients. Efficacy was excellent in 3 cases, good in 17 cases and poor in 2 cases. No side effects were observed in any cases.
2. Following a single intravenous injection of 1.0 or 2.0g, the transfer of CTX to the internal genital organs was found to be good. The transfer of CTX to exudate of the dead space of pelvis was also good.
3. The above data demonstrated that CTX is a safe and effective drug.

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Fundamental and clinical studies were made on cefotaxime (CTX), a new cephalosporin antibiotic, The following results were obtained.
1. Antibacterial activity:
At a concentration of 3.13mcg/ml, CTX inhibited the growth of 90.2% of 92 strains of Gram-negative rods and 80.0% of 15 strains of Gram-positive cocci.
2. Concentrations of CTX in body fluids and genital organs after 2g i. v.:
(1) CTX level in pus reached the peak (5.6mcg/ml) at 2 hours after administration.
(2) Mean CTX levels in the pelvic space exudate reached the peak (28.0mcg/ml) at 2 hours after administration.
(3) CTX levels in the uterine appendages and uterus reached the peak (8.9 and 4.5mcg/g, respectively) at 110 to 280 minutes after administration.
3. Clinical results:
CTX was excellent in 7 of 13 cases and good in the remaining 6 cases. The response rate to CTX was 100%.
4. The bacteriological effect: The bacteriological effect of CTX was also 100%. Bacteria were eradicated in 7 of the 10 cases where organisms were demonstrated before CTX treatment. Partial reduction bacteria was observed in the remaining 3 cases.
5. No side effect attributable to CTX was observed.

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The new antibiotic cefotaxime (HR 756, CTX) has been proved to be clinically effective against infections observed in the field of obstetrics and gynecology. The present study was intended to investigate the transfer of CTX to the internal genital organs and the dead pelvic space. Theresults were obtained as follows:
1. The concentrations of CTX transferred to the uteri and its appendages after CTX 1g in-travenous injection were sufficiently effective againt the major pathogens (Gram-negative and anaerobic bacteria) demonstrated in the field of obstetrics and gynecology.
2. The concentrations of CTX transferred to the dead space of the pelvis were effective against almost all of the Gram-negative bacteria for 6 to 12 hours after CTX 1g or 2g intravenous injection. CTX was thus proved to be very effective for the prevention and treatment of infections of the dead pelvic space.

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We have conducted basic and clinical examination of a new cephalosporin derivative, cefotaxime (CTX).
The average level of transfer measured at various locations in uterus tissue and adnexa 15 to 105 minutes (53.4 minutes in average) after intravenous administration of this drug ranged from 1.5mcg/g (myometrium) to 3.3mcg/g (portio vaginalis). It was distributed in cervix uteri and portio vaginalis at highest concentration, followed by oviduct, tunica serosa and ovary, and to myometrium at lowest concentration. The same pattern of distribution was observed in transfer ratio of various location in uterus tissue to uterus arterial blood.
The drug was transfered at very high level in pelvic cavity fluid after total hysterectomy throughout 3 postoperative hours.
Five cases of gynecological infections receiving in total 10 to 42g of CTX demonstrated ‘excellent’results in 2 cases, and ‘good’ in 3 cases. Out of these, 3 cases did not respond to other antibiotic.
Neither side effect nor clinical test abnormality was observed, except for one case, in which mild increase of GOT and GPT occured.
Based on the results of basic and clinical studies as discribed above, this drug is considered to have excellent efficacy and safety.

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6059-S, a new injectious oxacephem antibiotic, has been investigated to give following results.
1. Clinical results
Twenty patients were administrated intravenously 20-124mg/kg/day of 6059-S for 2-14 days. Clinical effect was excellent in 5 cases, good in 7, fair in 3, poor in 1, unknown in 3 and except in 1, and efficacy rate was 75%.
Side effect was observed only 1 case of discomfort and chill of hand and foot immediately after intravenous injection and no adverse value in laboratory findings was seen.
2. Pharmacokinetics
Blood level and urinary excretion of 6059-S single administration were measured in 4 patients with normal renal function and a patient with renal failure.
Half life was 1.27-1.76 hours in 4 patients with normal renal function and 4.33 hours in a patient with renal failure.
Urinary excretion was 43.4-50.9% up to 4 hours in 2 patients with normal renal function, and it was delayed to 1.0% up to 12.5 hours in a patient with renal failure.

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6059-S was administered to 32 children with various acute bacterial infections (bronchopneumonia 11, bronchitis 1, pyelonephritis 5, acute enteritis 6, purulent infection 4, secondary infection due to agranulocytosis 5) at the dose of 21 to 190mg/kg/day for 2 to 12days.
The clinical response of 6059-S was very satisfactory in all 17 cases with the injection of respiratory tract or urinary tract infection, but it was not so favourable in 5 cases of secondary infection due to agranulocytosis.
The overall clinical response was excellent in 5, good in 20, fair in 4, and failure in 3 with effective rate of 78%. As to side effect, each one case diarrhea and elevation of GOT and GPT was noted.

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[in Japanese]

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Fundamental and clinical studies in the pediatric field on 6059-S, a newly synthesized oxacephem antibiotics, were carried out, and following results were obtained.
1) MIC of 6059-S for K. oxytoca(40 strains), recently isolated from patients, were almostly more less than 0.2 mcg/ml, and that for H. influenzae was 0.05 mcg/ml, but that for non-group A-β-Streptococcus(2 strains) were 12.5 mcg/ml.
2) In 9 infants, the serum concentration of 6059-S in a dose of 10-37.5 mg/kg/day with intravenous drip infusion method was measured. The peak serum concentration were 32.8-241 mcg/ml at end of injection, and serum concentration were 0.6-3.19 mcg/ml 7 hours after administration.
The excretion rates in urine for 12 hours after administration were distributed between 55.8-89.6%.
3) Clinical evaluation of 6059-S was performed in evaluated 29 cases: 24 cases of respiratory tract infection, 2 cases of cervical lymphadenitis, 2 cases of urinary tract infection, 1 case of enteritis. The ove all efficacy rate was 96.6%.
4) Side effects observed during this therapy were 1 case of diarrhea, 2 cases of adverse effect (eosinophilia, elevation of GOT, GPT).

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1. MIC of 6095-S against 92 strains of clinically isolated bacteria were measured. The compound was active against most of Gram-negative rods, but was not active against Staphylococcus aureus.
2. 20 mg/kg of 6059-S (newly synthesized oxacephem antibiotics) was administered to the pediatric patients and its blood concentration was measured by agar well method using E. coli 7437 as a test organism.
3. The mean blood concentrations were maximum at 15 minutes after intravenous one-bolus injection. Maximum levels were 94.5 mcg/ml in the patients of below 5 years old and 98.7 mcg/ml above 6 years old. Their half-life of the blood levels were 95.4 and 110.6 minutes respectively.
4. The mean blood concentrations were highest at the end of the infusion in the cases of 60 minutes drip injection. Maximum levels were 85.0 mcg/ml in the patients of below 5 years old and 64.8 mcg/ml above 6 years old.
5. Clinical efficacy of 6059-S in 6 cases pyelonephritis, 2 cases of sepsis, 1 case of meningitis, 1 case of intraperitoneal abscess, 9 cases pneumonia and 1 case of tonsillitis was 100%. In the case of urinary tract infection, 4 patients were treated successfully by the administration of 20 mg/kg/day of 6059-S. Other bacterial infections were treated with 55 to 200 mg/kg/day.
6. 100% of the causative organisms were eliminated by 6059-S. They were E. coli, Klebsiella pneumoniae, Serratia marcescens, H. influenzae and β-Streptococcus.
7. No remarkable side effect was noticed during administration.

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Clinical efficacy was evaluated in children, particularly in the treatment of bacterial meningitis, and the following results were obtained.
1. Eleven children with the following bacterial infections were treated with 6059-S: 4 patients with bacterial meningitis (causative organism:H. influenzae in 3 and E. coli in 1), 2 with subcutaneous abscess (causative organism: each one case caused by S. aureus and P. aeruginosa), 1 with empyema thoracis (H. influenzae), 2 with suspected sepsis (causative organisms unknown), 1 with sepsis complicated with urinary tract infection (E. coli) and 1 with urinary tract infection (E. coli). Each two patients with subcutaneous abscess and suspected sepsis had leukemia and malignant tumor as the underlying disorder, respectively. Patients with bacterial meningitis were given intravenously about 200mg/kg/day of 6059-S divided in four doses, and other patients were treated either with an intravenous or a 1-hour intravenous drip infusion of 66.1-108.3 mg/kg/day divided in 2 to 3 doses. An overall efficacy rate was 90.9%, excellent or good in 10 patients and failure in one patient with suspected sepsis.
2) Neurological sequelae in bacterial meningitis were paresis of the right upper extremity in one patient (H. influenzae) and hydrocephalus in another (E. coli). When we take into consideration the fact that the causative organisms.were negative on the next day following the start of the antibiotic treatment in three patients other than case 1 whose causative organism was negative already when 6059-S started and that an improvement of the cerebrospinal fluid findings was satisfactory, an occurrence of neurological sequelae was considered not due to a lack of therapeutic efficacy but to a delay of the start of the antibiotic treatment.
3) Adverse reactions were noted in 3 patients, i.e., skin eruption in 1, neutropenia in 1, and eosinophilia, elevation of GOT and GPT in 2, respectively. They were all temporary and recorded in patients who were given either large doses or for longer periods.
4. Two patients received about 50 mg/kg of 6059-S by a 1-hour intravenous drip infusion, and the serum concentrations of the drug were determined. They were maximum at the end of the infusion, i.e., 158μg/ml and 214μg/ml, and 18μg/ml and 12μg/ml at 4 hours after the infusion; T 1/2 being 76.6 min. and 57.7 min., respectively. Serum concentrations in a 34-day-old premature infant who was given intravenously 45.5 mg/kg were 94μg/ml (1/2 hour), 59μg/ml (1hour), 49μg/ml (2 hours), 28.8μg/ml (4 hours) and 20μg/ml (6 hours), T 1/2 being 160 min.
5. Concentrations of the drug in the cerebrospinal fluid in 4 patients with bacterial meningitis following an intravenous injection of about 50 mg/kg appeared to be influenced by the time interval after the injection, the day of an illness and the disease activity, but was expected to give a level higher than 3μg/ml, which was 30 to 60 times higher that the MICs of each causative organism.
6. The above results indicate that 6059-S is a very effective antibiotic in the treatment of bacterial infections in children and the optimal dosage is to give about 20 mg/kg 2 to 3 times daily by an intravenous injection or by an intravenous drip infusion except for bacterial meningitis. In cases with bacterial meningitis, the drug is indicated for those caused by Gram-negative rods and should be given intravenously 50 mg/kg four times daily. However, it remains to be solved whether the dose will be able to be reduced.

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A new semisynthetic 1-oxa-β-lactam derivative, 6059-S, was evaluated for its safety and efficacy in children. Twenty-five patients were treated with 10 to 274 mg/kg per day of6059-S by intravenous administrations. The diagnosis of the patients were acute pharyngitis (2), acute bronchitis (2), pneumonia (4), pertussis (4), acute enterocolitis (2), recurrent urinary tract infection (2), suspected septicemia (3), and acute purulent meningitis(1); and the remaining 5 patients were considered to have nonbacterial infections. The pathogens recovered were Streptococcus pneumoniae(1),Haemophilus influenzae(4),Haemophilus parainfluenzae(1),Enterobacter cloacae(1), Enterobacter aerogenes(1),Proteus morganii(1),Pseudomonas aeruginosa(2) and Salmonella typhimurium(1). All the patients of bacterial infections were cured after the 6059-S therapy. However, Pseudomonas aeruginosa and Salmonella typhimurium were not erradicated after the 6059-S therapy, and the rate of bacterial disappearance was 75%.
Diarrhea (3), precordial pain (2, only in cases with high-dose therapy), transient elevation of GOT and GPT (2), and transient eosinophilia (2) were found to be associated with the 6059-S therapy. However, no severe adverse reactions were encountered.
Half life of the serum 6059-S level was1.34±0.16 hours. CSF concentrationsin a case with Haemophilus influenzae meningitis ranged 4.0 to 9.7mcg/ml after an intravenous injection of 34.3 to 75mg/kg of 6059-S.
From the present study, 6059-S appears to be a safe and effective antibiotic when used in children with susceptible bacterial infections. It remains to be further determined whether 6059-S is superior toABPC in the treatment of Haemophilus influenzae meningitis.

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[in Japanese]

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6059-S, a new oxacephem antibiotic was applied in the clinical use of gynecological and obstetrical infection.
1. In obstetrical field, attention should be paid on choice of antibiotics in the case of maternal infection. Especially in the trimester of pregnancy, such drugs as ampicillin (ABPC) has been reported apparent unfavourable effects by decreasing the estriol (E₃) level.
2. The comparative study between 6059-S, SBPC and ABPC was performed by various hormone level, including E₃ (blood and urine), blood progesterone, α-fetoprotein, human chorionic gonadotropin (HCG), cortisol and human placental lactogen (HPL). 9 cases of intrauterine fetal growth retardation (IUGR)(ranging from 28-36 weeks of pregnancy) was selected, including toxemia of pregnancy or complicated pregnancy of myoma of uterus and diabetes mellitus. The determination of hormone level, one drug (2g) out of three test drug was chosen at random and administered by intravenous infusion on 3-4 days after admission. After 5 days of interval, another test dosis was given, and the evaluation between the drug effects was performed on the hormonal level.
3. Following the single administration of ABPC (2g) by intravenous infusion, the decrease of urinary E₃ reached 26% on the 2 days after injection. As for SBPC the decrease was 21%, while in cases 6059-S, no apparent change was determined. Statistical difference between 6059-S and ABPC 5% by x² determination was found. On the other hormonal level, there was relatively great individual difference, and the apparent day by day change was undeterminable.
4. Clinical estimation of 6095-S on the gynecological infection was also performed on the 7 cases of patients. The overall efficacy rate was 85.7%. No adverse reaction was observed except one case elevation of S-GPT.

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A new antibiotic drug of oxacephem, with marked resistance to β-lactamase, 6059-S for parenteral use was tested in 10 patients with acute peritonitis. In 4 cases with appendicitis, 6059-S in a dose of 500 mg was given intramusculary before operation. In 2 cases with perforate MECKEL'S diverticulitis and intestinal obstruction for right femoral hernia, 6059-S in a dose of 1 g was given by intravenous injection or intravenous drip infusion before or during operation. And in a case with peritonitis after gastrectomy for gastric cancer, 6059-S in a dose of 2 g was given by intravenous drip infusion. Tissue specimens of different sites or body fluids were taken during the operation and from the removed organs. The materials of purulent ascites were subsequently taken at intervals. Determination of 6059-S concentration was performed according to plate agar well bioassay method with Escherichia coli 7437 strain.
The peak of 6059-S concentration in purulent ascites of patient with peritonitis for perforate MECKEL'S diverticulitis was 30.5 mcg/ml at 50 min. after 1 g intravenous administration. Concentration of 6059-S in drained pus was 8.38 mcg/ml soon after intravenous drip infusion (2 g, for 2 hrs.).
In 10 patients with peritonitis, 6 patients were given 6059-S in a dose of 500 mg by intramuscular administration twice a day, and the serious 4 patients were given in a dose of 1 to 2g by intravenous drip infusion 1 to 2 times a day. Clinical responce was excellent in 6 cases, good in 3 cases, fair in 1 case and poor was none. Any clinical adverse effect was not recognized.
On the 6059-S concentration in patients with peritonitis, the concentration in purulent ascites, drained pus and infected tissues were observed higher than the MIC of 6059-S against Escherichia coli and Klebsiella pneumoniae.
Therefore, 6059-S will be a very useful drug when used for chemotherapy of acute or subacute peritonitis.

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A new antibiotic drug of oxacephem, with marked resistance to β-lactamase, 6059-S for parenteral use was used in 12 patients with acute cholecystitis and cholangitis. 6059-S was given by intramuscular, intravenous or drip intravenus administration at a daily dose of 500mg to 2g. Clinical response was excellent in 1 case, good in 10 cases, fair in 1 case and poor in none. Any clinical adverse effect was not recognized.
6059-S is a dose of 500mg was given by intramuscular administration before the operation to 9 patients. Tissue specimens of different sites were taken from removed organs. The materials of A-bile and B-bile were subsequently taken at intervals.
6059-S concentrations in the A-bile increased after injection and reached to peak from 2 hours to 2.5 hours, then declined very slowly. 6059-S concentration in the B-bile reached to high level of theconcentration comparative quickly after intramuscular administration, and it was thought to be excreted through the wall of the gallbladder. 6059-S concentration in the gallbladder wall was directly proportional to the degree of pathological changes of inflammation.
On the 6059-S concentration in patients with acute cholecystitis and cholangitis, the concentration in A-bile, B-bile and gallbladder wall were observed higher than the MIC of 6059-S for Escherichia coli and Klebsiella pneumoniae.
Therefore 6059-S will be a very useful drug when used for chemotherapy of the infectious diseases of the biliary tract.

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