Following results were obtained from intravenous administration of T-1982 (cefbuperazone) 1g by measuring its concentrations in uterine arterial serum, cubital venous serum, oviduct, ovary and several sites in uterine tissue.
1. Endometrium showed the highest concentration among various uterine tissues by any administration (bolus injection, dripping infusion for 1 or 2 hours).
2. Transfer concentrations about 1 hour after the end of 1 hour drip infusion proved to be almost the same as 2 hours drip infusion.
3. In the field of obstetrics and gynecology, it was conside, ed that T-1982 has good efficacy in infections especially caused by E. colt, Klebsiella and Proteus.

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Clinical studies on T-1982 (cefbuperazone) were performed in 20 patients of obstetrics and gynecology, and the following results were obtained.
1. Clinical effect: The effectiveness was 100% (excellent in 5 cases, good in 4 cases) in intrauterine infection, 75% in adnexitis (excellent in 1 case, good in 2 cases, poor in 1 case), 100% in pelveoperitonitis (excellent in 2 cases, good in 2 cases), 0% in parametritis (boor in 1 case) and 100% in BARTHOLIN'S abscess (good in 2 cases), with the overall effectiveness rate of 90% (excellent in 8 cases, good in 10 cases, poor in 2 ases).
2. Bacteriological effect: A total of 17 strains was isolated from 12 out of 20 cases. Fourteen out of 17 strains were aerobic organisms (7 of E. coli, 4 of Klebsiella, 2 of S. aecalis and 1 of S. epidermidis) and 3 out of 17 strains were anaerobes (each 1 strain of B. fragilis, P. prevotii and P. anaerobius) and all of them were eliminated.
3. No side effects due to this drug were noted.

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Fundamental and clinical studies on T-1982 (cefbuperazone) in the field of obstetrics and gynecology were carried out.
Transfer of T-1982 to various location in uterus tissue was more than 10μg/g over 2 hours after T-1982 1 g intravenous injection.
T-1982 was distributed in cervix uteri at the highest concentration followed by ovarium, oviduct, portio vaginalis, endometrium and myometrium. Mean transfer ratio of cervix uteri to uterus arterial blood was 67.6%.
Ten cases of gynecological infections receiving T-1982 demonstrated “good” results in 9 cases, except 1 case excluded from the evaluation of efficacy.
Neither side effect nor clinical test abnormality was observed.
Based on the results of basic and clinical studies, T-1982 is considered to have efficacy in the treatment of gynecological infections.

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T-1982 (cefbuperazone), a new cephamycin antibiotic, was studied for its MICs against clinical isolates, transfer into uterine tissues and clinical efficacy in the field of obstetrics and gynecology. The following results were obtained.
1. The MICs of T-1982 were measured against 397 strains of 13 species. In antibacterial activity, T-1982 was equal to CTT but inferior to CMZ against Gram-positive bacteria. Against Garm-negative bacteria, T-1982 was superior to CEZ and other cephamycin antibiotics, i. e. CMZ and CTT. The activity of T-1982 was almost equal to that of CMZ and superior to that of CTT against B. fragilis.
2. T-1982 concentrations in various uterine tissues attained the peaks of 16.8-35.9 μg/g at 34 minutes after intravenous dministration of 1g, the tissue/serum ratios being 34-72%. The tissue concentrations were about 3-4 μ/g even at 5-5.5 hours after administraion.
3. T-1982 was intravenously administered at a dose of 1g twice daily to 5 cases with obstetrical and gynecological infections. All the cases responded to the therapy.
4. Elevated GOT and GPT were observed in 1 case, but they returned to normal on 8 days after the therapy.

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Fundamental and clinical studies were made on T-1982 (cefbuperazone) and the results were obtained as follows.
Serum and uterine tissue concentrations of T-1982 were determined at 26 minutes before and at 20 to 80 minutes after the completion of intravenous drip infusion of 1g.
The levels of T-1982 in the fallopian tube, ovarium, endometrium, myometrium and uterine cervix were 23.7, 19.5, 50.5, 10.9 μg/g and 17.5 μg/g at 20 minutes after the completion of infusion. The levels were sufficiently effective against major pathogens (Gram negative bacteria and anaerobic bacilli) isolated in the field of obstetrics and gynecology.
T-1982 was administered to 11 patients, including 7 of acute adnexitis, each one of pelveoperitonitis, pyometra, puerperal fever, and 1 of puerperal fever with sepsis, at a dose of 1-2g twice a day for a period of 5 to 9 days by intravenous injection or intravenous drip infusion. Clinical responses were excellent in 5, good in 3 and poor in 3. No adverse reactions nor marked changes in laboratory findings were observed in any of the cases treated with T-1982.

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Fundamental and clinical studies on T-1982 (cefbuperazone), a new cephamycin antibiotic, in the field of obstetrics and gynecology were carried out, and the following results were obtained.
The levels of T-1982 transferred to uterine artery, elbow vein and uterus were determined after intravenous drip infusion of 1.0g for 1 or 2 hours.
No difference of concentration between uterine artery and elbow vein was observed from 45 minutes to 5 hours after the end of administration.
The concentration of T-1982 in uterine artery ranged from 9.8 to 48 μg/ml after drug administration, and decreased slowly, but remained at about 10 μg/ml even 5 hours after the end of dministration.
Endometrium exhibited comparatively higher concentration of T-1982, but the difference of concentration was not observed among the other uterine tissues.
T-1982 concentraion ratios of various uterine tissues to elbow vein blood ranged from 172 to 10.2%, and mean ratio was 34.7%. Also, T-1982 concentration of more than 3 μ/g in each tissue was maintained for 2 hours after the end of administration.
Clinical results on abscess of BARTHOLIN'S gland (1) and adnexitis (1) were good, although bacteria were not detected.
No side effects caused by the drug were observed. These results indicate the usefulness of T-1982 in the treatment of infections in obstetrics and gynecology.

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T-1982 (cefbuperazone), a novel cephamycin antibiotic, was fundamentally and clinically studied in the field of obstetrics and gynecology.
The concentration of T-1982 in the maternal blood was highest and 135 μg/ml at the end of intravenous administration of 1.0g, then gradually decreased and was 10 μg/ml at 4 hours after administration. The half-life was 95.5 minutes. The concentration in the umbilical cord blood attained the peak of about 30 μg/ml at 30 minutes and was 10 μg/ml even at 4 hours, the half-life being 150 minutes.
Of 10 cases comprising 5 with endometritis, 3 with pelveoperitonitis, 1 with pyometra and 1 with vulvar abscess, 8 cases were with mixed infections. Thirteen strains of Gram-positive bacteria, 7 strains of Gram-negative bacteria and 9 strains of anaerobic bacteria were isolated. Of these bacteria, 24 strains excluding 4 of S. faecalis and 1 of S. epidermidis were eradicated. The MICs of T-1982 against Gram-positive bacteria (10 strains) were higher than those of CPZ, CMZ, CEZ and SBPC. Particularly against S. faecalis (4 strains), both T-1982 and CMZ demonstrated the MICs of > 100 μg/ml. The MICs of T-1982 against Gram-negative bacteria (6 strains) excluding P. aeruginosa were similar to those of CPZ but lower than those of CMZ, CEZ and SBPC. Against anaerobes (9 strains), T-1982, CPZ, CMZ, CEZ and SBPC showed low MICs with no remarkable difference.
Clinical response was observed in 8 (80%) of the 10 cases treated with T-1982. Two ineffective cases were with severe infections. No subjective and objective side effects nor abnormalities in hematology and hepatic and renal function were noted in any cases.
From the above results, it is indicated that T-1982 may be useful in preventing fetal infections due to premature rupture and treating gynecological infections.

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A clinical investigation on the efficacy of T-1982 (cefbuperazone), a new cephamycin antibiotic, was peformed in the field of obstetrics and gynecology.
T-1982 was administered to 17 cases: 6 cases of parametritis, 3 cases of endometritis after artificial abortion, 3 cases of puerperal fever, 2 cases of febrile abortion, 1 case of BARTHOLIN'S abscess, 1 case of adnexitis and 1 case of infection of vaginal hematoma.
Seventeen cases of these infections receiving in total 6 to 20g of T-1982 demonstrated excellent results in 8 cases and good in the remaining 9 cases.
Neither side effect nor clinical test abnormality was observed.
From the present study, T-1982 is considered to have excellent efficacy and safety.

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T-1982 (cefbuperazone) concentrations in antecubital venous blood and pelvic dead space exudate were examined in 4 patients who had received radical hysterectomy due to uterocervical cancer. Data analysis for the transfer of T-1982 into pelvic dead space exudate was performed with the simulation curves prepared from pharmacokinetic parameters by the three-compartment model.
When T-1982 was given at a dose of 1g, the peak level in the venous blood was 83.7μg/ml at 1 hour after the start of administration. With regards to T-1982 concentration in pelvic dead space exudate, the peak level of 19.3 μg/ml was observed at 2.24 hours after the start of administration and relatively high concentration of about 6.1 μg/ml was observed even at 8 hours after the start of administration.
From the above results, it is concluded that T-1982 is a useful drug for the treatment of infections in the field of obstetrics and gynecology.

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Experimental and clinical studies of T-1982 (cefbuperazone), a new cephamycin antibiotic, were performed in the field of obstetrics and gynecology, and the following results were observed.
1. T-1982 was determined for its in vitro activity against 180 recent clinical isolates in comparison with cefmetazole (CMZ) and cefazolin (CEZ). The activity of T-1982 was superior to that of CMZ against E. coli (101 strains) and B. fragilis (19 strains), and similar to that of CMZ and CEZ against Peptococcus (34 strains).
2. High concentrations of T-1982 exceeding the MIC values against various bacteria were maintained for a few hours in the female genital organs and postoperative retroperitoneal exudate after intravenous drip infusion of 2g.
3. T-1982 was administered to a total of 6 patients in daily dose of 2-3g for 2-10 days. The clinical results were excellent or good in 5 cases. Drug eruption was observed in 1 case.
These results suggest that T-1982 is highly effective for the treatment of bacterial infections in this field.

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T-1982 (cefbuperazone), a new cephamycin antibiotic with broad spectrum against Gram-positive, negative aerobic and anaerobic organisms, was clinically and bacteriologically evaluated on the gynecologic infectious diseases.
Fourteen cases hospitalized at Kanazawa Medical University Hospital and the affiliated hospitals from October 1981 to July 1982 were treated with T-1982.
By clinical symptoms, signs and bacteriological examinations the patients were diagnosed as pelveoperitonitis (1), intrauterine infection (3), adnexitis (3), infectious diseases of external genitalia (4), infectious abortion (1), vulvar hematoma (1), and rectovaginal fistula (1).
T-1982 was administered intravenously or by drip infusion at a dose of 0.5-2.0g twice a day after dissolved in a saline solution or a 5% glucose solution.
Based on the improvement of clinical findings and antibacterial effect of T-1982, results were evaluated as excellent, good, poor and unknown. Clinical effects more than good were shown in 9 of 11 cases which could be followed up exactly on the therapeutic of T-1982.
Two cases showing poor response were pelveoperitonitis and pyometra under carcinoma colli uteri stage IIIb, respectively.
In 8 of 11 cases, antibacterial effect of T-1982 could be evaluated.
Thirteen strains of aerobic and anaerobic bacteria were disappeared by T-1982 therapy, while no effect was seen on 5 strains.
On the side effect of T-1982, exanthema was observed in 1 case but disappeared soon after the cessation of administration.

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Laboratory and clinical investigation of T-1982 (cefbuperazone) in the field of obstetrics and gynecology were carried out and the following results were obtained.
1. The peak concentrations of 18.1-36.0 μg/ml were noted in pelvic cavity fluid at 1-3 hours after intravenous injection or drip infusion of 1 g of T-1982 in 3 cases after total hysterectomy for diffuse uterine cancer, then the concentrations decreased very slowly and were over 10μg/ml at 6 hours after administration. Transfer rate of the drug into pelvic cavity fluid was 33-66% of the serum concentrations.
2. In clinical trial, a total of 5 cases including 4 cases of external genital infections and 1 case of pelvic infection were treated with T-1982, and the results were evaluated as good in 3 cases, poor in 1 case and unknown in 1 case. Side effects were observed in 1 case who showed slight increase of GOT and GPT.

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Fundamental and clinical studies were carried out on T-1982 (cefbuperazone) a new cephamycin antibiotic, with the following result.
1. Following a single intravenous administration of 1.0g of T-1982, the transfer of T-1982 to the internal genital organs was found to be good. The transfer of T-1982 to retroperitoneal fluid was also good.
2. In clinical trial, T-1982 was administered to 10 patients with obstetrical and gynecological infection. Efficacy was excellent in 4 cases and good in 6 cases.
No side effects were observed. In laboratory findings, a transient elevation of alkaline phosphatase was noted in 1 case.

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T-1982 (cefbuperazone), a new cephamycin antibiotic, was fundamentally and clinically studied. The following results were obtained.
1. Serum and internal genital tissue levels of T-1982 were measured following intravenous injection or intravenous drip infusion of 1 g.
High serum levels of more than 10 μg/ml and tissue levels of more than 5 μg/g were maintained for 3 hours after intravenous administration.
Favourable transfer of T-1982 into the pelvic dead space exudate was observed. The exudate level attained its peak at 2 hours and was 14.6 μg/ml on average even at 8 hours after intravenous infusion.
With its MIC values, T-1982 was considered to be bactericidal against many Gram-negative bacteria except Pseudomonas sp.
2. A total of 4 cases comprising 2 with pyometra, 1 with pelveoperitonitis and 1 with endometritis complicated with pelveoperitonitis was treated with T-1982 at a dose of 1-2g twice daily by intravenous drip infusion.
The clinical response was excellent in 1 case and good in 2 cases. A case with pyometra due to S. faecalis did not respond to the therapy.
Side effects and abnormal laboratory findings due to the drug were not noted.

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1. Tissue concentrations of T-1982 (cefbuperazone) at 100-220 minutes after the completion of 1g/60 minutes dripping infusion were 8.9-10.6μg/g in the uterus, ovary and oviduct. These concentrations were higher than 80% MIC of the causative organisms, including E. coli, K. pneumoniae, P. mirabilis, Bacteroides and Peptococcus isolated from infections in the field of obstetrics and gynecology.
2. The T-1982 concentration in the retroperitoneal space exudate reached a peak value of 19.6μg/ml at 2 hours after the completion of 1g/60 minutes dripping infusion and decreased at a constant rate.
3. We administered T-1982 at 2 g per day for a period of 7-9 days to 3 patients with gynecological infectious diseases. All cases proved to respond effectively. No side effects and abnormal laboratory findings were observed.

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One gram of T-1982 (cefbuperazone), a new cephamycin antibiotic, was given intravenously to a total of 28 patients prior to abdominal total hysterectomy for uterine myoma or benign ovarian tumor.
Bilateral uterine arteries were clamped at 0.25, 0.5, 1, 2, 4 hours or 6 hours after administration, and serum samples and uterine tissues were taken for the measurement of T-1982 concentration by bioassay method.
A little difference was found in the serum concentration between cubital venous and uterine arterial serum, the half lives being 1.88 hours and 1.74 hours, respectively. The initial concentrations were estimated to be 99.9 μg/ml and 103.2 μg/ml, respectively. The peak concentrations were obtained at 30 minutes in the endometrium, myometrium, oviduct and ovary, and at 1 hour in the cervix uteri and portio vaginalis. These were 45.2μg/g, 22.4 μg/g, 36.1 μg/g, 19.9 μg/g, 27.6μg/g and 23.4μg/g, respectively. The tissue concentrations thereafter decreased in the same manner as the serum concentrations.
Judging from its favorable transfer into the uterine tissues and MICs against clinical isolates often seen in the field of obstetrics and gynecology, T-1982 was evaluated to be clinically useful in the treatment of obstetrical and gynecological infections.

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Fundamental and clinical studies on T-1982 (cefbuperazone), a new cephamycin antibiotic, were carried out, and the following results were obtained.
1. When T-1982 was administered at a dose of 1 g by intravenous drip infusion for 30 minutes or 1 hour, the concentration in serum showed as high as 23.0 μg/ml or 25.0 μg/ml even 2 hours after administration. The concentrations in the genital tissues about 5 hours after administration ranged 1.2-45.6 μg/g for 30 minutes drip infusion and 0.9-26.8 μg/g for 1 hour drip infusion.
From these results, T-1982 was supposed to maintain the in vivo concentration to inhibit 80-100% the growth of bacteria such as S. aureus, E. coli, Klebsiella, Proteus, S. marcescens and Gram-negative anaerobic bacteria, B. fragilis which were often isolated clinically in the field of obstetrics and gynecology.
2. When T-1982 was administered at a dose of 1-2g twice a day to 14 patients with female genital infection; 2 intrauterine infection, 2 pyometra, 7 pelveoperitonitis, 1 adnexitis, 1 adnexal abscess and 1 vaginal cuff abscess, the clinical results were excellent in 9, effective in 4 and poor in 1. The efficacy rate was 92.9%.
3. No side effects nor abnormalities in laboratory findings were observed in any of the 14 cases.
These results suggest that T-1982 has efficacy for the treatment of obstetrical and gynecological infections.

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Human pharmacokinetics and clinical studies of T-1982 (cefbuperazone) were carried out and the following results were obtained.
1. Transference into pelvic cavity fluid T-1982 level in pelvic cavity fluid showed the peak level of 48.0 μg/ml at 30 minutes after 2 hours drip infusion of 1 g in 1 case. The concentration tended to be more sustained than that of venous blood.
2. Clinical study
T-1982 was administered to 2 cases with pelveoperitonitis, 2 cases with puerperal fever and 1 case with adnexitis at a dose of 1 g twice a day for a period of 4 or 5 days. The clinical effect was excellent in 3 and good in 2 cases.
Neither side effects nor abnormalities of laboratory findings were observed.

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T-1982 (cefbuperazone), a new cephamycin antibiotic, was fundamentally and clinically studied in the field of obstetrics and gynecology.
The following results were obtained.
1. The concentrations of T-1982 in arterial and venous blood and genitalia following intravenous injection were measured. The results demonstrated favourable transfer of the drug into various internal genital organs.
2. T-1982 was administered to 12 patients. The efficacy rate was 75.0%, that is to say, good in 9 cases. No side effects were noted in any cases.
It is, therefore, presumed that T-1982 is a useful drug for the infectious diseases in the field of obstetrics and gynecology although the number of subjects was not so large in this study.

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T-1982 (cefbuperazone), a new cephamycin antibiotic, was basically and clinically studied in the field of obstetrics and gynecology. The following results were obtained.
1. The pelvic dead space exudate and serum levels of T-1982 were measured in patients with radical hysterectomy with pelvic lymphadenectomy for uterine cervical cancer after 1 hour drip infusion of 1 g. At the end of infusion, the serum level was 87.2 μg/ml on average and thereafter declined rapidly. The pelvic dead space exudate level attained the peak of 25.1μg/ml at 2 hours and thereafter declined gradually but was 3.2 μg/ml even at 8 hours after infusion.
2. A total of 10 cases comprising 1 with intrauterine infection, 2 with pelveoperitonitis, 2 with adnexitis and 5 with external genital organ infection were intravenously treated with T-1982 at a dose of 1 g twice daily for 5-7 days. The clinical results were excellent in 1 case, good in 8 cases and poor in 1 case. Eruption and elevated GOT and GPT were noted in 1 case.

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T-1982 (cefbuperazone), a new cephem antibiotic, was fundamentally and clinically studied in the field of obstetrics and gynecology. The following results were obtained.
1. The concentrations of the drug in arterial and venous blood, and genitalia following intravenous drip infusion were measured. The results demonstrated favourable transfer of the drug into various internal genital organs.
2. Eleven patients with bacterial infections were treated with T-1982. The therapeutic results were markedly effective in 2 and good in 9 cases, therefore the effective rate was 100%. No side effects were noted in any cases.
It is therefore, presumed, that T-1982 is a useful drug for infectious diseases in the field of obstetrics and gynecology although the number of subjects was not so large in this study.

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T-1982 (cefbuperazone), a new cephamycin antibiotic, was fundamentally and clinically studied in the field of obstetrics and gynecology. The following results were obtained.
1. The concentrations of T-1982 in arterial and venous blood and genitalia were measured. The results demonstrated favourable transfer of drug into various internal genital organs.
2. T-1982 was administered to 13 patients. The effectiveness rate was 92.3%, that is to say, excellent in 4 cases, good in 8 cases and poor in 1 case.
3. As for side effect, any noteworthy effect was not observed.

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Fundamental and clinical studies on T-1982 (cefbuperazone), a new cephamycin antibiotic, were carried out in the field of obstetrics and gynecology, and the following results were obtained.
In a fundamental study, T-1982 was given to 7 patients with postpanhysterectomy at a dose of 1 g by intravenous drip infusion, and T-1982 concentrations in uterine artery and elbow vein serum and each uterine tissue (fallopian tube, ovary, endometrium, corpus uteri, cervix uteri and portio) were serially determined. The concentration in the endometrium (though the range of values was wide) was found higher than that in the other tissues.
In a clinical study, T-1982 was given to 5 patients; 2 patients with parametritis and each one patient with right salpingitis, pyometra and metroendometritis. The efficacy rate was 80%.
No side effects nor remarkable abnormalities in hematology, urinalysis and renal and hepatic function were observed during the therapy.

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Susceptibility of 100 clinical isolates of H. influenzae (84β-lactamase non-producing strains and 16 β-lacta-mase producing strains) to 5 cephamycin antibiotics was studied in comparison with 3 reference antibiotics.
In MIC₉₀ against β-lactamase non-producing strains, LMOX and ABPC were the most excellent, followed by T-1982, CTT, CTM, CMZ, CFX and CEZ.
Against 8-lactamase producing strains, all the cephamycin antibiotics were as active as against 8-lactamase non-producing strains, whereas ABPC was extremely less active with the MIC₉₀, of >100 μg/ml. CTM and CEZ were about 1 tube less active than against β-lactamase non-producing strains.
Thus, it was confirmed that the cephamycin antibiotics were stable to β-lactamase.

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Clinical efficacy of netilmicin (NTL) was clinically evaluated against 34 cases with surgical infections, obtaining the following results.
1. The evaluation of the overall clinical efficacy by the physicians in charge revealed 3 markedly effective cases, 21 moderately effective cases, and 1 fairly effective case with efficacy rate of 96% in group A (the group of treatment with NTL from the beginning), and 3 markedly effective cases, 4 moderately effective cases and 2 fairly effective cases with efficacy rate of 77.8% in group B (the group of treatment with no efficacy using other antibiotics).
2. The evaluation of the overall clinical efficacy by the integrated evaluation standards revealed 1 markedly effective case, 22 moderately effective cases, and 2 poorly effective cases with total efficacy of 92%. in group A, and 7 moderately effective cases, and 2 poorly effective cases with efficacy rate of 77.8% in group B.
3. The evaluation of the clinical efficacy by isolated bacteria revealed 9 moderately effective cases and 2 poorly effective cases in 11 cases with single infection of Gram-positive bacteria with efficacy rate of 81.8%, 6 moderately effective cases out of total 6 cases with single infection of Gram-negative bacteria with efficacy rate of 100%, and 1 markedly effective case, and 5 moderately effective cases in total of 6 cases with mixed infection of bacteria with efficacy rate of 100%.
The overall efficacy in group A was 1 markedly effective case, 20 moderately effective cases and 2 poorly effective cases out of total 23 cases with efficacy rate of 91.3%.
The evaluation of efficacy in group B revealed 4 moderately effective cases in total 4 cases with single infection of Gram-negative bacteria with efficacy rate of 100% and 1 moderately effective case and 2 poorly effective cases in total 3 cases with mixed infection of bacteria with efficacy rate of 33.3%. The overall efficacy in group B was 5 moderately effective cases and 2 poorly effective cases in total 7 cases with efficacy rate of 71.4%.
4. The bacteriological efficacy of NTL by types of isolated bacteria revealed 11 cases with elimination of bacteria, 4 cases with retention of the original bacteria and 7 cases with alteration of bacteria in total 22 cases of group A.
The bacteriological efficacy in group B was 4 cases with elimination of bacteria and 3 cases with retention of the original bacteria, but without any case with alteration of bacteria.
5. Side effects were evaluated with 36 cases including 2 cases excluded from efficacy evaluation. Neither subjective nor objective findings revealed any adverse symptoms.
In the laboratory tests, a case demonstrated the elevation in GPT, but without specific problem in treatment with NTL.

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Thirteen patients who were performed radical lobectomy for the disease of the chest, were administered of cefotiam (CTM) 1.0g for an hour by intravenous drip infusion during their operation. The concentration of CTM in serum and lung tissue were determined.
CTM showed very high concentration in lung tissue and very high concentration ratio of lung tissue to serum cencentration for several hours.
These results suggested that CTM will be useful agent for the prevention and treatment of pulmonary infection, since CTMsh owed also very potent antibacterial activity against Gram-positive and Gram-negative bacteria.

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A clinical investigation of a long-acting amoxicillin preparation (L-AMPC) in 82 patients (81 with skin and soft-tissue infections and 1 with osteomyelitis) gave the following results.
1. Staphylococcus aureus and Staphylococcus epidermidis were most frequently detected organisms. With an inoculum of 10⁶ cells/ml, the respective MICs for S. aureus and S. epidermidis were 1.56 μg/ml and 0.2 μg/ml.
2. When evaluated by the doctors in charge, the overall effect was excellent in 23 patients, good in 46, fair in 7 and poor in 6, with an efficacy rate of 84.1%.
The efficacy rate was as high as 75.0-95.5% in considerable numbers of patients with furuncle, felon, infectious sebaceous cyst, subcutaneous abscess, phlegmon or periproctic abscess. The effectiveness rate was 92.3% (12/13) in patients who did not respond to treatment with other antibiotics such as cephalexin.
The standard criteria of overall effectiveness were newly established by the committee under the consideration of the clinical course of symptoms and absence or present of surgical procedure. When evaluated by the standard criteria, the overall effectiveness was excellent in 27 patients, good in 42, fair in 4 and poor in 9, with an efficacy rate of 84.1%. There were no significant differences between the evaluation by the doctors in charge and that by the standard criteria.
3. The eradication rate of the organisms detected was 94.1% (64/68 patients); 85.7% for S. aureus (24/28 strains) and 100% for S. epidermidis (27/27 strains).
4. No significant differences were noted between the patients with and without surgical procedure in clinical effectiveness or bacteriological efficacy.
5. One patient had diarrhea of unknown cause.
6. No abnormal changes due to L-AMPC were noted in any laboratory test.
7. The usefulness rate was 76.8%.
These findings indicate that L-AMPC in b.i.d. doses is safe and effective in skin and soft-tissue infections in surgery.

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