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 147,016 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

During the 10-year period from 1980 through 1989 using gonococci isolated in Sapporo, we studied beta-lactamase production capacity and the sensitivity of various antibacterial agents and obtained the following results. 1. The frequency of isolating beta-lactamase producing gonococci (PPNG) displayed a gradual tendency to increase during the first half of the 80's and reached a peak in 1985 of 23.9% (61/255). However, thereafter it tended to decline and in 1989 it was 6.3% (2/32). 2. The sensitivity to penicillin-type antibacterial agents was higher against PPNG than non-PPNG against PCG, ABPC, and AMPC displaying about a 7 level MIC90 so that it was quite sensitive. Against CVA/AMPC, SBTPC it showed a relatively favorable MIC90. Also, the sensitivity of PPNG against AMPC with 1984 as the boundary, thereafter the MIC distribution was observed to decline somewhat. 3. Against the monobactam-type injectable drug, AZT, both non-PPNG and PPNG showed a low MIC distribution and against SPCM both showed a relatively high MIC distribution of 3.13-25 micrograms/ml. 4. In regard to the sensitivity to cephem-type antibacterial agents, against such 3rd generation injectables as CZX, CFTM-PI, etc. it displayed a particularly low MIC distribution. 5. Against tetracycline and macrolide antibacterial agents, it displayed a relatively high MIC distribution. 6. Against new quinolone type antibacterial agents, regardless of being non-PPNG or PPNG, it showed a low MIC.
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PMID:[A study on the beta-lactamase production for Neisseria gonorrhoeae and the sensitivity to various antibacterial agents]. 190 78

Skin penetration of various antimicrobial agents was studied in rats. Skin concentration/serum concentration ratios were classified into three groups, i.e. group I with ratio greater than or equal to 0.7, group II with the ratio 0.7-0.4 and group III with the ratio less than or equal to 0.4. The drugs of group I were OFLX, CPFX, LFLX, FLRX, SPFX, AMK, EM, RXM, CAM, CLDM. The drugs of group II were ABPC, CVA/AMPC, CVA/TIPC, CEX, CED, CXD, CTM-HE, CXM-AX, CPZ, CBPZ, TFLX, ASTM, MINO. The drugs of group III were AMPC, CCL, CDX, CPDX-PR, CFTM-PI, CTZ, CEC, CEZ, CTM, CMZ, CZON, MCR, IPM/CS. Factors which may influence the skin penetration were discussed, but no definite conclusion has not been obtained.
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PMID:[Skin penetration of antimicrobial agents in rats]. 194 92

Susceptibilities of 179 strains of 30 bacterial species or subspecies to clavulanic acid/amoxicillin (CVA/AMPC) combination were determined by the 2-fold agar dilution method as well as by diameters of inhibition zones in the single-disc method, under the experimental conditions established by Kanazawa. The experiments demonstrated significant correlation between MICs by the dilution method and diameters of inhibition zones in each of conventional assays of the over-night (about 16 hours) incubation, the delayed assay (about 24 hours incubation), and the rapid assay (after 3-4 or 5-6 hours incubation), thus confirming applicability of the single-disc assay for activities of CVA/AMPC combination. From an analysis of the data obtained using CVA/AMPC (1:2) combination of disc containing 45 micrograms, the primary regression equations were obtained as follows: D (diameter, mm) = 27.4-10.1 log MIC (micrograms/ml) in the conventional assay; D = 33.7-13.4 log MIC (micrograms/ml) in the delayed assay; D = 20.7-6.6 log MIC (micrograms/ml) in the 5-6 hours rapid assay, and D = 14.5-3.6 log MIC (micrograms/ml) in the 3-4 hours rapid assay. The range of variations in MICs of CVA/AMPC combination estimated from diameters of inhibition zones by the disc test was then calculated in comparison with that in MICs determined by the 2-fold agar dilution method to estimate experimental errors involved in assaying MICs of CVA/AMPC combination by the single-disc assay.
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PMID:[A study on the disc sensitivity test for clavulanic acid/amoxicillin combination]. 324 24

BRL 25000, granules preparation containing 2 parts of amoxicillin (AMPC) and 1 part of clavulanic acid (CVA, beta-lactamase inhibitor) as its potassium salt, has been investigated fundamentally and clinically. An in vitro study of the antibacterial activity of BRL 25000 against clinically isolated S. aureus (34 strains) showed higher activity than for AMPC alone and demonstrated that CVA potentiated the activity of AMPC, showing a synergistic effect against beta-lactamase producing organisms. A total of 27 pediatric patients aged between 6 months and 13 years 8 months (23 with respiratory infections and 4 with urinary tract infections) were treated with a daily dose ranging from 31.7 to 54.5 mg/kg, divided into 3 or 4 doses a day for periods of 4-18 days. The clinical effect was evaluated as excellent in 26 cases, poor in 1 case and the efficacy ratio was therefore 96.3% (26/27). The bacteriological effect against 12 organisms isolated from 9 patients was studied and all were eradicated (12/12). A drug-related side effect was observed in only 1 patient who developed diarrhea on the 4th day of treatment which continued during the treatment for 10 days. However, no severe side effect and no abnormality related to the drug in laboratory findings were observed. From these results it is concluded that BRL 25000 will be a clinically effective drug in the treatment of mild and moderate infections in the pediatric field.
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PMID:[Experimental and clinical studies on BRL 25000 (clavulanic acid-amoxicillin) granules in pediatric infections]. 384 20

Bacteriological and clinical evaluations of BRL 25000 (1 part clavulanic acid plus 2 parts amoxicillin) granules in the pediatric field have been performed. The MICs of BRL 25000 against 25 clinically isolated strains of S. aureus, 40 E. coli, and 14 K. pneumoniae were compared with those of AMPC. Against beta-lactamase non-producing strains of S. aureus and E. coli, the MICs of both drugs were nearly equal, however, against beta-lactamase producing strains of these species and K. pneumoniae, BRL 25000 was superior to AMPC. The blood levels of AMPC and CVA after single oral administration of approximately 15 mg/kg of BRL 25000 granules to fasted children were studied in 3 subjects. The mean levels of AMPC and CVA peaked about 1 hour after administration at values of 11.40 and 5.49 micrograms/ml, respectively, with half-lives of 0.91 and 1.02 hours, and AUCs of 23.52 and 12.66 hr X micrograms/ml, respectively. The 6-hour urinary recovery of AMPC ranged from 30.59% to 52.03% and for CVA from 16.31% to 45.18%. There was no significant difference between the blood level of AMPC following single oral administration of approximately 10 mg/kg AMPC granules and that of AMPC following single oral administration of approximately 15 mg/kg BRL 25000 granules to the same children. Clinical evaluation of BRL 25000 granules administered orally 3-4 times a day at total daily doses of between 42.9-52.9 mg/kg resulted in improvement, judged excellent or good, in all 7 cases of tonsillitis and 2 cases of pyelonephritis. In particular, the clinical effect was excellent in the case of tonsillitis where a beta-lactamase producing H. influenzae was isolated. In the total 11 cases treated, including 2 cases of mycoplasmal pneumonia excluded from the clinical evaluation, 1 case of rash and eosinophilia was observed. No other adverse reactions or abnormal laboratory findings were observed. The taste and flavor of the drug were well accepted by the children. It was concluded that BRL 25000 granules are promising new drug which should be markedly useful in the treatment of infections in pediatric outpatients.
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PMID:[Bacteriological and clinical evaluation of BRL 25000 (clavulanic acid-amoxicillin) granules in the pediatric field]. 384 23

BRL 25000 granules (containing 2 parts amoxicillin and 1 part clavulanic acid) have been studied fundamentally and clinically. The MICs of BRL 25000 against strains of S. aureus, E. coli, K. pneumoniae which were resistant to CEZ and beta-lactamase producing strains of H. influenzae were determined. The MICs of BRL 25000 at an inoculum of 10(6) cells/ml were 1/4 to 1/128 of those of AMPC and, in particular, the MICs of BRL 25000 were especially reduced against the organisms for which those of AMPC were more than 100 micrograms/ml. The pharmacokinetics of BRL 25000 were studied in 46 children at dose levels of 7.5 mg (8 fasting children, 7 non-fasting children), 10 mg/kg (4 fasting, 4 non-fasting), 15 mg/kg (4 fasting, 4 non-fasting), 20 mg/kg (8 fasting, 7 non-fasting). The peak serum concentrations in fasting children were marginally higher than those in non-fasting subjects. Values for AMPC and CVA from BRL 25000, dosed at 7.5, 10, 15 and 20 mg/kg to fasting children, 0.5-1 hour after dosing were 4.86 and 2.36 micrograms/ml, 5.20 and 1.69 micrograms/ml, 7.50 and 3.27 micrograms/ml, 9.38 and 6.30 micrograms/ml, respectively. In non-fasting subjects, corresponding values were 2.84 and 1.01 micrograms/ml, 4.53 and 2.10 micrograms/ml, 7.29 and 4.08 micrograms/ml, 6.83 and 2.96 micrograms/ml, respectively. The biological half-lives of AMPC and CVA, following the administration of BRL 25000, show no significant difference between the fasting and non-fasting states. Values for AMPC and CVA in fasting children were 0.85-1.15 hours and 0.64-1.03 hours, and in non-fasting children, 1.18-1.79 hours and 0.78-1.02 hours, respectively. The time to reach the peak serum concentration and half-lives were similar for AMPC and CVA when dosed as BRL 25000. Peak urinary concentrations for BRL 25000 (AMPC and CVA) at dose levels of 7.5, 10, 15, 20 mg/kg to fasting children were 681.8 and 148.2 micrograms/ml, 247.1 and 66.3 micrograms/ml, 484.2 and 149.1 micrograms/ml, 1,796.5 and 372.0 micrograms/ml, whilst in the non-fasting state the values were 496.3 and 83.2 micrograms/ml, 991.1 and 156.7 micrograms/ml, 2,397.5 and 460.7 micrograms/ml, 1, 896.3 and 323.4 micrograms/ml, respectively. The peak urinary concentration in the fasting state was observed at 0-2 hours after dosing, and in non-fasting individuals it occurred at 2-4 hours after dosing.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Experimental and clinical studies on BRL 25000 (clavulanic acid-amoxicillin) granules in the pediatric field]. 384 24

BRL 25000 (187.5 and 375 mg tablets), a formulation of CVA-K and AMPC in the ratio of 1:2, and AMPC (as control drug) were administered to healthy volunteers, aged 20 approximately 28 years and weighing 60 approximately 85 kg (68.8 kg, on average). Each drug was administered 3 times a day (after meals) for 5 days and the volunteers were separated into 3 groups of 4 subjects each. The effect on the fecal flora was studied before dosage, during administration (day 3 and 5) and day 3 and 5 after the administration course was completed. Studies were undertaken to isolate C. difficile on the last day of administration and 3 and 5 days after administration had ceased. Fecal concentrations and the susceptibility of the isolates to AMPC, CVA-K and BRL 25000 were measured. Side effects and laboratory findings were studied. The results obtained were as follows: 1. In BRL 25000 (187.5 mg X 3/day) group, the population of E. coli was on average, 1 X 10(6) approximately 9 X 10(6) cells/g feces before initiation of administration and it increased by 2 logarithms 3 and 5 days after initiation of administration. By 3 and 5 days after end of administration, the E. coli population was similar to the initial population. The population of Klebsiella sp. was 1 X 10(6) approximately 9 X 10(6) cells/g feces on average before commencement of dosage and it increased by 2 logarithms 3 days after initiation of administration but there was no consistent change in the Klebsiella sp. population thereafter. The Enterobacter sp., population was not consistent neither was the population of other Enterobacteriaceae. In total, the mean Enterobacteriaceae population was 1 X 10(7) approximately 9 X 10(7) cells/g feces before initiation of administration and increased by 2 logarithms 3 days after initiation of administration, and then returned to the initial level 5 days after end of administration. No consistent changes in population were noted for the other Gram-negative bacilli. The Staphylococcus sp. population was 1 X 10(6) approximately 9 X 10(6) cells/g feces on average before initiation of administration. This organism was detected in only 1 case 3 days after initiation of administration and in another 5 days after initiation of administration, thereafter, the population was similar to the initial population.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Effect of BRL 25000 (clavulanic acid-amoxicillin) on bacterial flora in human feces]. 384 25

MICs of BRL 25000, a combination of a newly developed beta-lactamase inhibitor CVA and AMPC in the ratio of 1 to 2, were determined against a number of bacterial strains and compared with those of AMPC, CVA, CEX and CCL. The 98 bacterial strains tested included 2-S. aureus, 23-H. influenzae, 25-E. coli, 22-K. pneumoniae and 26-P. mirabilis. In pharmacokinetic studies, BRL 25000 medium granules were administered to groups of 3 male subjects, aged between 7 years 8 months and 9 years 5 months, at doses of 10, 15 and 20 mg/kg, 2 hours after a meal. The resultant serum and urine concentrations and drug recoveries were measured. Furthermore, BRL 25000 was administered to a total 43 patients (2-pharyngitis, 8-tonsillitis, 3-bronchitis, 2-pneumonia and 28-urinary tract infection) whom clinically evaluable. An average daily dosage of 45.3 mg/kg was given, in 3 or 4 divided doses, for a period of 8 days on average. Clinical and bacteriological effects as well as side effects were studied. In the microbiological studies on 98 clinical strains, including beta-lactamase negative bacteria, BRL 25000 showed MICs against the Gram-positive cocci (2-S. aureus) superior to the other 4 drugs at inoculum sizes of 10(8) and 10(6) cells/ml. For the Gram-negative bacilli, against H. influenzae at inoculum sizes of 10(8) and 10(6) cells/ml, BRL 25000 was inferior in the small MIC range but superior in the large MIC range to AMPC, and was superior to the other 3 drugs. Against E. coli at an inoculum of 10(8) cells/ml, BRL 25000 showed antibacterial activity next to AMPC and CCL whilst at an inoculum of 10(6) cells/ml, it was inferior in the small MIC range but superior in the large MIC range to AMPC and CEX and was inferior to CCL but superior to CVA. Against K. pneumoniae at an inoculum of 10(8) cells/ml, BRL 25000 was equal to AMPC, CVA and CEX but inferior to CCL, whilst at an inoculum of 10(6) cells/ml, it was inferior to CCL but superior to the other 3 drugs. Against P. mirabilis at inoculum sizes of 10(8) and 10(6) cells/ml, BRL 25000 was inferior in the small MIC range but equal or superior in the large MIC range to AMPC, and was superior to CVA and CEX.(ABSTRACT TRUNCATED AT 400 WORDS)
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PMID:[Experimental and clinical trials of BRL 25000 (clavulanic acid-amoxicillin) granules in the field of pediatrics]. 389 76

The authors have carried out laboratory and clinical studies on the BRL 25000 granule (containing 2 parts amoxicillin and 1 part clavulanic acid). The antibacterial activity of BRL 25000 against 29 clinically isolated strains of S. aureus, 30 E. coli and 30 K. pneumoniae were measured by the agar dilution method using an inoculum size of 10(6) cells/ml. beta-Lactamase production was detected by the Nitrocefin method. The MICs of BRL 25000 against S. aureus ranged from 0.2 approximately 12.5 micrograms/ml, with the majority of strains being inhibited by 1.56 micrograms/ml or less. Seven beta-lactamase producing strains of S. aureus were all inhibited by less than 12.5 micrograms/ml. The range against E. coli was 1.56 approximately 100 micrograms/ml, with the majority inhibited by 6.25 micrograms/ml or less. Fifteen beta-lactamase producing strains of E. coli were inhibited by 6.25 approximately 100 micrograms/ml and the majority by 25 micrograms/ml or less. All strains of K. pneumoniae were beta-lactamase producers and the MIC distribution against K. pneumoniae was 1.56 approximately 50 micrograms/ml, with a majority inhibited by 3.13 micrograms/ml or less, 96% of strains, were inhibited by less than 6.25 micrograms/ml. Against K. pneumoniae, BRL 25000 showed a 8 to 16-fold superiority when compared with AMPC. In a pharmacokinetic study, BRL 25000 granules were orally administered to children in the fasting state at single doses of 7.5 mg/kg and 20 mg/kg. The peak serum levels of AMPC were 6.13 and 6.94 micrograms/ml approximately 1 hour after administration and decreased with half-lives of 1.08 and 0.97 hours, respectively. The corresponding serum levels of CVA were 1.16 and 1.90 micrograms/ml at 1 hour after administration, with half-lives of 0.99 and 0.87 hour, respectively. In clinical studies, the BRL 25000 granule was effective in 39 cases of bacterial infection out of a total of 41 treated. Side effects were limited to 2 cases of diarrhea and minor changes in laboratory findings were elevation of serum GOT (1 case), elevation of serum GPT (1 case), and eosinophilia (2 cases).
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PMID:[Laboratory and clinical studies of BRL 25000 (clavulanic acid-amoxicillin) granules in the pediatric field]. 400 52

We assessed the in vitro antimicrobial activity and the clinical efficacy and safety of SY5555 in the field of pediatrics. The results obtained are summarized below. 1. In vitro antibacterial activities of SY5555 against 52 clinical isolates were compared with those of clavulanic acid/amoxicillin (CVA/AMPC), cefotiam (CTM), cefpodoxime (CPDX), cefaclor (CCL) and cefdinir (CFDN). Against Gram-positive bacteria, including Staphylococcus aureus, Streptococcus pneumoniae and Streptococcus pyogenes, SY5555 displayed antimicrobial activities superior or nearly equivalent to those of the reference agents used in the study. In cases of Gram-negative bacteria, the antimicrobial activity of SY5555 against Haemophilus influenzae was inferior to those of CPDX and CFDN. Against Klebsiella pneumoniae, the antimicrobial activity of SY5555 was less potent than that of CPDX. 2. Forty-seven children with infectious diseases were treated with SY5555 dry syrup (powder dissolved just before use). The clinical results were excellent in 24 and good in 16, with an efficacy rate of 85.1%. 3. Bacteriological screening identified 30 pathogenic organisms, and the eradication rate was 76.7%. 4. Side effects consisted of diarrhea in 12.5% (6 cases), loose stools in 4.2% (2 cases) and urticaria in 2.1% (1 case) of the patients. The only abnormal laboratory test value observed was an increase in eosinophil count in one child. 5. The palatability of SY5555 dry syrup was very good; it was very easily ingestable or easily ingestable by 32 of the 48 children. From the above results, SY5555 dry syrup appears to be a useful drug with a preferable safety profile in the treatment of pediatric patients with infectious diseases.
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PMID:[Fundamental and clinical studies of SY5555 in pediatrics]. 769 47


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