The Japanese Journal of Antibiotics
Online ISSN : 2186-5477
Print ISSN : 0368-2781
ISSN-L : 0368-2781
Virtual issue
Volume 43, Issue 4
Displaying 1-16 of 16 articles from this issue
  • KAORU SHIMADA
    1990 Volume 43 Issue 4 Pages 583-602
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
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  • TAKASHI MOTOHIRO, KEIKO ODA, MASAFUMI ARAMAKI, AKIRA KAWAKAMI, KOICHI ...
    1990 Volume 43 Issue 4 Pages 603-622
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Cefodizime (CDZM), a newly developed injectable cephem antibiotic, was given via bolus intravenous injection at each of 3 dose levels of 10, 20 and 40 mg/kg to each 3 children, and serum and urinary levels and urinary recovery rates were followed.
    A total of 57 patients received CDZM in the following regimen via bolus intravenous injection, and clinical efficacies, and microbial responses were evaluated. Mean dosage per application: 20.9 mg/kg, number of application per day: between 2 and 4 (2 times for 3 patients, 3 for 26 patients and 4 for 28 patients), mean duration of the therapy: 1 week. Patients consisted of 1 case of peritonsillar abscess, 2 acute bronchitis, 38 pneumonia, 8 urinary tract infection, 1 staphylococcal scalded skin syndrome, 2 cellulitis, 4 purulent lymphadenitis and 1 typhoid fever.In addition to the patients mentioned above 6 patients who dropped out were involved in the evaluation of adverse reactions and influence of the drug on laboratory test data, and the following results were obtained.
    1. Five minutes after bolus intravenous injection in doses of 10, 20 and 40 mg/kg, serum levels determined by the bioassay method were at their maxima, i.e. 114.0,264.6 and 461.6 μg/ml, respectively. Serum levels of drugs were dose-dependent throughout all the dosage levels tested. Mean serum half-lives of the drug were 1.757, 1.552 and 1.668 hours, respectively, for the 3 dose levels. Serum levels of the drug determined by the HPLC method were similar to those by the bioassay method: The maximum serum levels occurred at 5 minutes after administration, mean maximum concentrations were 105.5,264.0 and 461.7 μg/ml for the 3 dose levels, and a dose response was noted for the 3 dose levels. The half-lives were 1.755, 1.598 and 1.668 hours, respectively.
    2. Mean maximum concentrations in urine determined by bioassay for 2 of 3 cases received 10 mg/kg and 3 cases each given 20 and 40 mg/kg of CDZM were 884.3, 3,061 and 7,352 μg/ml, respectively, in the first 2 hours after administration. These levels were also dose-dependent. Mean recovery rates were 74.4, 78.4 and 71.5%, respectively, in the first 8 hours after administration. Mean maximum concentrations in urine measured by HPLC were similar to those determined by bioassay, i.e. 962.3, 3,404 and 7,899 μg/ml in the first 2 hours. They were, also, dose-dependent. Mean recovery rates were 82.1, 86.0 and 76.5%, respectively, in the first 8 hours after administration.
    The HPLC determinations gave slightly higher levels than the bioassay.
    3. Clinical efficacies were excellent or good in 93.0% (53 patients), thus the efficacy was generally good.
    4. Bacteriologically, 16 strains were followed and 15 of them (93.8%) were found to have been eliminated, giving a very high elimination rate.
    5. In the 63 cases including 6 dropped-out cases, 2 cases with adverse reactions, both diarrhea, were found.
    6. Abnormal findings in laboratory examinations were noted; 2 cases of thrombocytosis, 5 eosinophilia, 1 each of slight elevation of GOT or GPT, and 4 cases with simultaneously abnormal GOT and GPT.
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  • KOICHI DEGUCHI, NOZOMI YOKOTA, MASAMI KOGUCHI, YUTAKA NAKANE, YOSHIKO ...
    1990 Volume 43 Issue 4 Pages 623-635
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    MICs of 16 antimicrobial agents including a newly synthesized aminoglycoside antibiotic, arbekacin (HBK), were determined against methicillin-resistant Staphylococcus aureus (MRSA) strains which had been isolated since 1988 from patients with refractory infections.
    1. The proportion of highly methicillin-resistant strains was large, especially among those isolated from blood and respiratory tract.
    2. All the MRSA strains were resistant to all the β-lactam antibiotics tested.
    3. Most of the strains were also resistant to aminoglycosides. However, HBK inhibited the growth of 95% of the strains at 3.13 μg/ml or less, showing potent activities even against highly resistant MRSA strains.
    4. The MIC distribution of HBK against MRSA strains showed no change since 1986 when year to year data were compared.
    Based on our studies on the drug resistance pattern of MRSA since 1986, a large proportion of MRSA strains isolated from blood and respiratory tract appeared to be coagulase type II.
    5. Netilmicin-resistant MRSAs have increased since 1986, and MRSA resistant to fosfomycin, minocycline, ofloxacin and norfloxacin have also increased in 1989 compared to 1988.
    6. The drug resistance pattern of MRSA has been changing every year and they are acquiring multi-drug resistance.
    Thus, in the treatment of MRSA infections, it is very important to identify the drug susceptibility of MRSA quickly and accurately.
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  • EFFECT OF SULBACTAM AGAINST β-LACTAMS RESISTANT STRAINS AND IN VITRO COMBINED EFFECT OF SULBACTAM/CEFOPERAZONE WITH EACH OF PIPERACILLIN, LATAMOXEF, CEFTAZIDIME, FOSFOMYCIN AND DOXYCYCLINE
    MASAKAZU KOUDA, IKUKO KUMAGAI, JUN-ICHI KOBAYASHI, RYOKO SUGAI, HIROKO ...
    1990 Volume 43 Issue 4 Pages 636-658
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    We evaluated relationships between production of β-lactamase and their resistances to β-lactams, effect of sulbactam (SBT), a β-lactamase inhibitor, against β-lactam resistant strains, and combined effect of sulbactam/cefoperazone (SBT/CPZ) with other antibiotics against multiresistantstrains.
    Through these studies, we obtained the following results.
    1. Most of the strains resistant to β-lactams were β-lactamase producers.
    2. Relationships between the production of β-lactamase and their resistances to β-lactams indicate that their resistances generally were the highest in producers of both penicillinase (PCase) and cephalosporinase (CEPase), moderate in producers of either PCase or CEPase, and the lowest in β-lactamase non-producers. Most of highly-resistant strains of MRSA appeared to be β-lactamase non-producers though some exceptions were observed among methicillinresistant Staphylococcus aureus (MRSA), Serratia marcescens and Pseudomonas aeruginosa.
    3. SBT showed good effect against PCase producers, moderate effect against producers of both PCase and CEPase, little effect against CEPase producers, and no effect against β-lactamase non-producers.
    4. Results of combined effect of SBT/CPZ with other antibiotics indicated that good synergism was obtained by combining SBT/CPZ with fosfomycin (FOM) or piperacillin against multi-resistant strains of Proteus spp., Enterobacter cloacae, and S. marcescens, by combining SBT/CPZ with ceftazidime (CAZ) or FOM in methicillin-sensitive S. aureus and by combining SBT/CPZ with CAZ in P. aeruginosa.
    5. Better synergism was obtained with the higher concentrations of antibiotics.
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  • JUN IGARI, MASATO SHITARA, MASAJI SHITARA, KAYOKO YOSHIMOTO, YASUYUKI ...
    1990 Volume 43 Issue 4 Pages 659-669
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    A nationwide susceptibility survey of clinical isolates of Escherichia coli and Klebsiella pneumoniae initiated in 1980 was continued for the 8th consecutive year. A total of 4,421 strains of E. coli and 2,825 strains of K. pneumoniae isolated mainly from urine, sputum and pus, were obtained from 69 hospitals throughout Japan during the 2 years (1986-1987). MICs were determined using the agar plate dilution method (MUELLER-HINTON agar, BBL) with inoculation of 108CFU/ml bacteria. Antibiotics tested in this survey were 2 penicillins, 7 cephems and 2 aminoglycosides.
    Most of the strains of the two species of bacteria were susceptible to ceftizoxime (CZX), cefotetan (CTT), latamoxef (LMOX), cefotiam (CTM) and cefmetazole (CMZ) and also gentamicin (GM) and netilmicin (NTL) were active against both species of bacteria. About 90% of the E. coli strains were inhibited at a concentration of 0.20 μg/ml of CZX, 0.39 μg/ml of LMOX, 0.78 μg/ml of CTT, 1.56 μg/ml of CTM or NTL, or 3.13 μg/ml of CMZ or GM. Most of the strains were resistant to ampicillin (ABPC) and piperacillin. For the strains of K. pneumoniae, similar results were obtained.
    Yearly changes in susceptibility of E. coli and K. pneumoniae were not obvious with ABPC, cefazolin, CMZ or GM.
    No significant differences were observed during 1986-1987 in susceptibilities of the isolates of both species of bacteria due to different clinical specimens.
    These results suggest that the 2nd and the 3rd generation cephems and aminoglycosides, alone or in combination, may be efficacious in treating infections due to E. coli and K.pneumoniae.
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  • CEFUROXIME AXETIL
    TAKEFUMI MORIHANA, KAZUYA INOSHITA
    1990 Volume 43 Issue 4 Pages 670-676
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The distribution of cefuroxime (CXM) was examined in NZW rabbits after oral administration at a dose of 20 mg/kg of cefuroxime axetil. CXM was detected in blood, oral tissues (tongue, gingiva, parotid gland, submandiblar gland, cervical lymphonodi and lower jaw bone), liver and kidney.
    The results were analyzed through pharmacokinetic calculation. Ratio of pharmacokinetic parameters in the tissues and those in the serum (free) were as follows:
    Cmax: 0.26 to 0.62, AUC: 0.70 to 1.53, MRT: 2.6 to 3.0, VRT: 7.7 to 12.2
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  • TADAHIRO MATSUSHITA, OSAMU KASUGA, TOUTARO YAMAGUCHI
    1990 Volume 43 Issue 4 Pages 677-685
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Combined actions of aspoxicillin (ASPC) with several aminoglycosides (AGs) against various Pseudomonas aeruginosa strains were examined using the checker board method and experimental infection of mice, and the actions were compared with those of piperacillin (PIPC) and mezlo-cillin (MZPC).
    1. The combination of ASPC with gentamicin, amikacin (AMK) or tobramycin showed synergistic activities against 81.9-95.5% of the test strains. These frequencies were higherthan those of reference penicillins (PCs). Mean values of FIC index for combinations between ASPC and AGs were smaller than 0.5, thus, the combinations showed the strongest synergism among the PCs tested.
    2. ASPC combined with AGs showed synergistic actions on experimental mouse infectionscaused by strains of P. aeruginosa. The potency of ASPC was the same as that of PIPC, but MZPC had a weaker activity than ASPC or PIPC.
    3. Schedule of administration of ASPC and AMK was examined using experimental infection in mice caused by P. aeruginosa. When AMK was administered first, a synergism was clearly observed when ASPC was administered within 1 hour of the AMK administration. When ASPC was administered first, a synergism was observed when AMK was administered within 4 hours of the ASPC administration.
    4. Influences of AMK and ASPC or reference PCs on growth of P. aeruginosa 22 were examined at lower concentrations than MIC. AMK showed a bacteriostatic action on the test strain at 1/4 MIC. But no influence was observed at lower concentrations than 1/4 MIC of AMK. ASPC and reference PCs showed slight effects on growth of the test strain at concentrations of 1/32 MIC of PIPC, 1/128 MIC of MZPC and 1/256 MIC of ASPC. The PCs showed bactericidal action against the test strain at these concentrations when combined with 1/4 MIC of AMK.
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  • KAZUO SENGOKU, TETSUYA SHIMIZU, HIROMITSU HAGA, RYOICHI INOUE, TOMOFUM ...
    1990 Volume 43 Issue 4 Pages 686-691
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Pharmacokinetic and clinical studies were carried out on aztreonam (AZT), a monobactam antibiotic with a high activity against Gram-negative bacteria.
    The results obtained are summarized as follows:
    1. Following 2g bolus intravenous injection, transfers of AZT to umbilical cord serum and amniotic fluid were found to be satisfactory. AZT level in amniotic fluid was higher than μg/ml at 40 minutes after administration and it was at 3.7 μg/ml in 23.5 hours.
    2. In the treatment of 9 patients with perinatal infections, clinical efficacies of AZT were judged excellent in 3 cases and good in 6 cases.
    3. No side effects and abnormal laboratory findings due to the drug were observed in any case.
    These results indicate that AZT may be a useful antibiotic for the treatment of perinatal infections.
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  • SATORU MAKINODA, HIROAKI NEGISHI, TOSHIHIRO OHKOHCHI, KAORU HANATANI, ...
    1990 Volume 43 Issue 4 Pages 692-695
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    The basic and clinical efficacies of aztreonam (AZT) were evaluated in obstetric and gynecologicinfections during the perinatal period. The results obtained are summarized below.
    1. Concentrations of AZT in umbilical venous blood and amniotic fluid showed a good placental transfer of AZT. The rate of placental transfer of AZT was very similar to rates for cephalosporins.
    2. Since the clinical efficacy rate of AZT in the treatment of Gram-negative bacterial infections was 80.0%, AZT appears to be a useful drug against Gram-negative bacterial infections.
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  • TETSURO CHIMURA, NOBUYUKI MORISAKI, TORU FUNAYAMA, MASAKI MATSUO
    1990 Volume 43 Issue 4 Pages 696-699
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Clinical effects of aztreonam (AZT), a monobactam antibiotic, on perinatal infections were studied with the following results:
    1. Efficacy rate of AZT in the clinical application to 12 cases of perinatal infections via 2-4g/day drip infusion (total dosage 8, -24 g) was 91.7% (11/12). Breakdown of the effects according to diseases were “excellent” for mastitis (n = 3), pyelonephritis (n =1) and urinary tract infection (n=1), and “good” for a total of 6 cases, i.e, amnionitis (n=2), amniotic fluid infections (n=3) and external genital infection (n=1).
    2. Results of bacteriological studies were “eradicated” (n=1), “replaced” (n=4), “appeared” (n=2) and “unknown” (n=5). MIC values of AZT (106 cells/ml) were in a range of25->100 μg/ml in 1 case of cervicitis (complicated with amnionitis) in the 13th week of pregnancy where AZT was found noneffective.
    3. Neither subjective nor objective side effects nor abnormal clinical values were observed during the treatment with AZT.
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  • SEIJI MATSUDA, KINKI OH, HIROAKI HIRAYAMA
    1990 Volume 43 Issue 4 Pages 700-705
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Preclinical and clinical studies on aztreonam (AZT) in the perinatal period were carried out and the results are summarized below.
    1. Concentrations of AZT in maternal serum, umbilical cord serum and amniotic fluid were measured after intravenous injection of AZT 1 g and 2 g, and intravenous drip infusion of AZT 1 g. As results, the transfer of AZT into umbilical cord serum started to increase in 1 to 2 hours, and the transfer of AZT into amniotic fluid started to increase after an elapse of 2 hours. Upon the intravenous injection of 2 g, AZT concentration in amniotic fluid was as high as 27.1 μg/ml even at 10 hours 30 minutes after the injection, and it was still 6.9 μg/ml at 20 hours or more after the injection.
    2. AZT 2 g/day (b.i.d.) was administered by intravenous drip infusion to 1 perinatal infection case with pyelonephritis. It was clinically effective and neither side effect nor abnormal laboratory test value was observed.
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  • NANKUN CHO, KANGO FUKUNAGA, KATSUAKI KUNII, INTETSU KOBAYASHI
    1990 Volume 43 Issue 4 Pages 706-718
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Pharmacokinetic, bacteriological and clinical studies on aztreonam (AZT) in the perinatal period were carried out with the following summary of the results.
    Antibacterial effects of AZT on bacterial growth of Escherichia coli (MIC 12.5 μg/ml) and Pseudomonas aeruginosa (MIC 50 μg/ml) in amniotic fluid were determined and it was found that the activity of AZT is enhanced in amniotic fluid.
    AZT repidly penetrated into tissues and sera of pregnant women upon intravenous (i.v.) injection and its maternal serum concentrations reached their peak levels shortly after the injection. Placental penetration of AZT to the fetus was good and, after single i.v. injection of 1 g, the concentrations of AZT in the umbilical cord serum and amniotic fluid exceeded MICs against major Gram-negative bacilli. These results indicate that single i.v. injection of AZT 1 g twice a day is effective for the treatment and prophylaxis of perinatal infections.
    Injection of AZT for the treatment of puerperal infections showed excellent clinical effectiveness with 100% eradication of aerobic Gram-negative rods. No side-effect was observed in any case.
    All of these results suggested clinical usefulness of AZT in the perinatal period.
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  • KUNIHIKO ITO, REIKO HIROSE, TERUHIKO TAMAYA, YOSHITAKA YAMADA, KOJI IZ ...
    1990 Volume 43 Issue 4 Pages 719-726
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Pharmacokinetic and clinical studies of aztreonam (AZT) in perinatal infections in the field of obstetrics and gynecology were performed with the following results.
    1. At one shot intravenous injection, 1 g AZT showed rapid distribution to the umbilicalcord serum with concentrations higher than 15 μg/ml in 1 hour 36 minutes after injection and higher 10 μg/ml even in 4 hours 30 minutes after injection.Significant difference in concentrations was not observed between arterial serum sample and venous serum sample of the umbilical-cord in a single subject. The concentration in the amniotic fluid reached a level higher 10 μg/ml in 3 hours 37 minutes after injection.
    2. Distribution into milk reached a concentration between <0.4 μg/ml to 1.0 μg/ml by 6 hours after administration.
    3. AZT 1 g × 2/day was given by intravenous drip infusion to 4 cases of perinatal infection in obstetrics and gynecology for 5 to 9 days. Clinically, AZT was effective for all the cases. Neither side effect nor abnormal laboratory value was observed.
    Consequently, AZT was considered to be highly effective and safe for its clinical use in the parturition and the puerperium.
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  • TAKAO YAMAMOTO, JINSUKE YASUDA, HIROJI OKADA, KAZUHIRO IWASAKU
    1990 Volume 43 Issue 4 Pages 727-735
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Pharmacokinetic and clinical studies on aztreonam (AZT) in the perinatal period in obstetrics and gynecology were performed with the following results.
    1. Concentrations of AZT in maternal serum, umbilical cord serum, amniotic fluid and neonatal serum were determined after 1 hour intravenous drip infusion of 1 g.
    The maternal serum concentration was 32.2 μg/ml at 26 minutes after administration, gradually decreasing thereafter to 13.2 μg/ml at 2 hours 33 minutes, 4.9 μg/ml at 3 hours 21 minutes and 2.9 μg/ml at 5 hours 3 minutes.
    Umbilical cord serum concentration was 17.0 μg/ml at 36 minutes after drip infusion and still remained at 4.0-6.1 μg/ml at 5 hours after administration. Amniotic fluid concentration was 9.9 μg/ml at 3 hours 21 minutes after drip infusion and showed 3.3 μg/ml at 16 hours 26 minutes after administration.
    Most of the maximum serum concentrations of newborns between 3 to 24 hours afterdelivery were not detectable, with only one case with 2.2 μg/ml at 9 hours after delivery.
    2. AZT 1 or 2gx2/day was given by intravenous drip infusion to 12 cases of perinatal infections in obstetrics and gynecology for 5 to 8 days. Clinical efficacies were evaluated as excellent in 8 cases, effective in 2 and not effective in 2 with 83.3% efficacy rate.
    With respect to side effects, minor degree of urticaria was observed in 1 case. Another case showed a transient elevations of GOT, GPT and Al-P in laboratory tests.
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  • A STUDY OF AZTREONAM IN THE PERINATAL CO-RESEARCH GROUP
    SEIJI MATSUDA, KINKI OH, HIROAKI HIRAYAMA, TETSUYA SHIMIZU, KAZUO SENG ...
    1990 Volume 43 Issue 4 Pages 736-753
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    Pharmacokinetics and clinical studies on an injectable monobactam antibiotic, aztreonam (AZT), were carried out in perinatal infections in obstetrics and gynecology and the obtained results are summarized as follows.
    1. Pharmacokinetic study
    (1) Upon one-shot intravenous injection of AZT 1 g before delivery, maternal serum concentration of AZT was 89.0 μg/ml immediately after the injection and a half-life (T 1/2) of 0.96 hour was observed. Umbilical-cord serum concentration showed a peak value of 16.5 μg/ml at 1.26 hours after the injection and gradually decreased with a T 1/2 of 1.91 hours. The transfer into amniotic fluid was observed and the peak value of AZT in amniotic fluid reached 12.9 μg/ml at 5.57 hours after the injection and slowly decreased thereafter with a T 1/2 of 4.42 hours. Transfer and disappearance in one-shot 2 g intravenous injection and 1 g intravenous drip infusion (1 hour) of AZT were very similar to the results obtained with the one-shot 1 g intravenous injection.
    (2) The residual serum concentration in neonates after one-shot 1 g intravenous injection of AZT to the mother was almost below the detectable limit. Transfer of AZT into milk was scarcely recognized.
    2. Clinical studies
    (1) AZT was injected to 47 cases with various perinatal infections and it was more than“effective” in 45 cases with an efficacy rate of 95.7%. Also, all the 12 cases to which AZT was administered for prophylaxis of infections showed prophylactic effect. Bacterial eradication was obtained with 25 strains out of 29 aerobic Gram-negative bacteria, but 1 strain “persisted” and for 3 strains results were “unknown”, hence an eradication rate of 96.2% was obtained. However, AZT treatment resulted in a little lower eradication rate against Gram-positive bacteria.
    (2) One case (1.3%) of minor degree of urticaria was found as a side effect, and one case each of eosinophilia and elevation of GOT, GPT and Al-P was observed as abnormal laboratory value.
    From the above results of pharmacokinetics and clinical evaluation, it has been concluded that AZT is a usejul and highly safe drug in various perinatal infections and prophylaxis.
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  • KOJI OHARA, HIDEYUKI FUKUDA, TOSHIHISA KANDA, MEGUMI KONO
    1990 Volume 43 Issue 4 Pages 754-756
    Published: April 25, 1990
    Released on J-STAGE: May 17, 2013
    JOURNAL FREE ACCESS
    A specific protein (MW 18,000) was found using chloramphenicol (CP) base-affinity chromatographyof periplasmic-space proteins obtained from an impermeability-type CP-resistant Pseudomonas aeruginosa harboring plasmid kR102.
    Membrane reconstitution experiments using a liposome system appeared to indicate that the permeability of CP was inhibited by the specific protein.
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