• 약학회지
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• 제25권4호
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• pp.161-165
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• 1981

The binding of two cephalosporins, cephalothin and cefazoline to human serum albumin(HSA) was studied by difference spectrophotometry using a spectrophotometric probe, 2-(4'-hydroxybenzeneazo) benzoic acid. The probe is strong visible absorbing material which interacts with serum albumin to give characteristic spectrophotometric peaks and provides the basis for a convenient assay to measure free and bound amounts in the presence of serum albumin and competitive drugs. The results obtained showed that the probe and cephalosporin compete for the same binding site on human serum albumin; thus the probe can be used to gauge the displacement of cephalosporins from human serum albumin. The data were interpreted on the basis of theory of multiple equilibria. The number of binding sites of human serum albumin for 2-(4'-hydroxybenzeneazo) benzoic acid(HBAB), cephalothin and cefazoline appears to be 4. By using this technique the binding constants were found as follows: HSA-HBAB, $7.89{\times}10^{4}M^{-1}$; HSA-cephalothin, $1.09{\times}10^{3}M^{-1}$ ; HSA-cefazoline, $1.21{\times}10^{3}M^{-1}$.

• 약학회지
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• 제43권1호
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• pp.128-130
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• 1999

In vitro activity of commonly used antimicrobial agents against several clinical isolates were studied. In the case of E. coli, the MICs at which 90% of the bacteria are inhibited of ampicillin, Unasyn, cefazoline, cefotaxim, carbenicillin, gentamicin and ofloxacin were 100<, 100, 25, 0.2, 100<, 3.13, and $12.5{\;}\mu\textrm{g}/m$ , respectively. In the case of K . pneumoniae, the MICs at which 90% of the bacteria are inhibited of ampicillin, Unasyn, crfazoline, cefotaxim, carbenicillin, gentamicin and ofloxacin were 100<, 12.5, 100<, 0.1, 100<, 1.6, and $0.4{\;}\mu\textrm{g}/m$ , respectively. In the case of Enterobacter sp, the MICs at which 90% of the bacteria are inhibited of ampicillin, Unasyn, cefazoline, cefotaxim, carbenicillin, gentamicin and ofloxacin were 100<, 100, 100<, 6.25, 100<, 100 and $1.57{\;}\mu\textrm{g}/m$ , respectively. In the case of Acinetobacter sp, the MICs at which 90% of the bacteria are inhibited of ampicillin, Unasyn, cefazoline, cefotaxim, carbenicillin, gentamicin and ofloxacin were 100<, 100<, 100<, 100<, 100< 100< and $50{\;}\mu\textrm{g}/m$ , respectively. In the case of Pseudomonas sp, the MICs at which 90% of the bacteria are inhibited of ampicillin, Unasyn, cefazoline, cefotaxim, carbenicillin, gentamicin and ofloxacin were 100<, 100<, 100<, 50, 100<, 25 and $25{\;}\mu\textrm{g}/m$, respectively. In the case of S. aureus, the MICs at which 90% of the bacteria are inhibited of ampicillin, Unasyn, cefazoline, cefotaxim, carbenicillin, gentamicin and ofloxacin were 50, 50, 100<, 100<, 50, 50, and $100{\;}\mu\textrm{g}/m$, respectively.

• Archives of Pharmacal Research
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• 제6권1호
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• pp.55-62
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• 1983

Binding of six cephalosporins (cefotaxime, cefuroxime, cefazoline, cephalothin, cephaloridine, cephacetrile) to bovine serum albumin was studied. Fluorescence probe technique and difference spectrophotometry were employed to evaluate the nature and degree of association of cephalosporin albumin complex. 1-Anilinonaphthalene-8-sulfonate (ANS) was used as the fluorescence probe. 2-(4'-hydroxybenzeneazo) benzoic acid(HBAB) was employed as the UV spectrophotometric probe. Compentitive bindings between cephalosporins and probes were observed. The number of binding sites of bovine serum albumin for each cephalcsporin is 2. Among six cephaloporins, cefotaxime has the highest binding constant followed by cafazoline, cefuroxime, cephalothin, cephaloridine and cephacetrile.

• Maxillofacial Plastic and Reconstructive Surgery
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• 제21권4호
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• pp.370-375
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• 1999

To evaluate the efficacy of antibiotic administration in the impacted mandibular third molar extraction the author investigated 107 patients requiring extraction of the lower third molar who visited at the Department of oral and maxillofacial Surgery, Chosun Dental Hospital and were healthy without medical problems and had no signs and symptoms of infection around the lower third molar. The patients were divided into 4 groups according to the method of antibiotics administration: 13 patients without antibiotics administration(group 1), 30 patients with only intravenous injection of $Cefazoline^{(R)}$ 2.0g 30 minutes before the procedure(group 2), 39 patients with intravenous injection of $Cefazoline^{(R)}$ 2.0g 30 minutes before the procedure and oral administration of follow-up dosages of $Augmentin^{(R)}$ for 1 day(group 3), and 25 patients with intravenous injection of $Cefazoline^{(R)}$ 2.0g 30 minutes before the procedure and oral administration of follow-up dosages of $Augmentin^{(R)}$ for 3 day(group 4). Infection rates after extraction were calculated and compared according to gender, the age of the patients, the level of impaction, and also compared between four groups. The results were as follows. 1. The overall infection rate was 8.4%. 2. The infection rate was higher in male(11.9%) than in female(4.2%), but there were statistically no significant differences between them. 3. Infection rate was lower in patients under age 30(7.2%) than in patients over age 30(12.5%), but there were statistically no significant between them. 4. Infection rate was higher in patients with complete bony impacted tooth(11.1%) than in patients with partial bony impacted tooth(6.5%), but there were statistically no significant differences between them. 5. Infection rate was 7.7% in group 1, 10.0% in group 2, 10.3% in group 3, 4.0% in group 4 and there were statistically no significant differences between groups. In summary, it is more important to extract the impacted lower third molar under aseptic condition and to minimize the injury of tissue if possible than to administer the preventive antibiotics in reducing the infection rate in healthy patients without medical problems who had no signs and symptoms of infection around the lower third molar.

• 한국응용약물학회:학술대회논문집
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• 한국응용약물학회 1994년도 춘계학술대회 and 제3회 신약개발 연구발표회
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• pp.171-171
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• 1994

Cephem ring의 C-7위치에 aminothiazoly lmethoxyimino기를 가진 화합물들이 항균활성을 증가시키고, G(-)균의 외막투과성을 촉진시킬뿐 아니라 광범위항균 spectrum을 갖게 하고 $\beta$-lactamase에 안정하며 PBP(penicillin binding protein)에 대한 결합친화성을 증가시킨다는 보고에 따라 본 저자는 C-7위치에 cefotaxime구조와 같이 aminothiazolylmethoxyimino acetamido moiety를 고정시키고 항균활성을 증가시키기 위하여 약리활성이 기대되는 5-(substituted)-2H-tetrazole유도체들을 합성하여 C-3 위치에 도입시킨 새로운 화합물 7$\beta$-〔(z)-2-(2-aminothiazol-4-yl)-2_(methoxyimino)acetamido〕-3-〔5-(substituted)tetrazol-2-yl〕 methyl-3-cephem-4-carboxylic acid 유도체를 합성하여 B. subtilis ATCC 6633, M. luteus ATCC 1004, E. coli KCTC 1039, E. coli ESS, K. pncumonia KCTC 1560, P. aeruginosa IF0 13130, S. typhimurium KCTC 1925, S. typhimurium SL 1102, 및 C. albicans ATCC 10231 등의 균과 fungus에 대하여 기존의 cefotaxime과 cefazoline을 대조물질로 사용하여 항균력을 비교하였다. 이들 화합물들은 대체적으로 M. luteus ATCC 6633, E. coli ESS, S. typhimurium SL 1102 균에 대해서는 cefotaxime보다 항균력이 우수하였으나 P. aeruginosa IF0 13130에 대해서는 항균력이 저하되었고 cefazolin보다는 대체적으로 항균력이 우수하였다.

• Archives of Pharmacal Research
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• 제7권2호
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• pp.87-93
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• 1984

The effects of ionic strength and pH on the binding of cefazolin to bovine serum albumin (BSA) were studied by UV difference spectrophotometry. As ionic strength at constant pH and temperature increases, the apparent bining constant decreased but the number of binding sites remained almost constant at 2. The constancy of the number of binding sites with increasing the ionic strength suggests that purely electrostatic forces between BSA and drug do not have great importance in the drug binding, even though there is a decrease in the apparent binding constant. Thus, the effect of ionic strength on the interaction between drug and BSA may be explained by the changes in ionic atmosphere of the aggregated BSA molecules and competitive inhibition by phosphate ions. In addition, the higher apparent binding constant at high ionic strength is explained by conformational changes of BSA from its aggregate forms into subunits. The pH effects on the afinity of interactions indicated that the binding affinity of cefazoline is higher in the neutral region than in the alkaline region. An d at high pH value, the number of binding sites decreased from 2 to 1 because of the conformational change of BSA in the alkaline region.

• 약학회지
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• 제38권3호
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• pp.322-331
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• 1994

For the development new cephalosporin antibiotics with aminothiazolmethoxyimino moiety in the C-7 position and triazolthiomethyl moiety in the C-3 position of cephem ring, $7{\beta}$-[(z)-2-(2-aminothiasol-4-yl)-2-(methoxyimino)acetamido]-3-[5-(aryl or het.)-4-phenyl-4H-1,2,4-triazol-3-yl]thiomethyl-3-cephem-4-carboxylic acids were synthesized. These compounds were tested for antimicrobial activitiy in vitro against ten species of microorganisms. It showed remarkable antibacterial activity against Bacillus subtilis ATCC 6633, Micrococcus luteus ATCC 9341 and Escherichia coli ESS. The antibacterial activity of most new compounds showed more active than cefazoline, but these compounds were lower active than cefotaxime against Pseudomonas aeruginosa IFO 13130.

• 한국동물위생학회지
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• 제18권2호
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• pp.113-123
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• 1995

The present study was conducted to investigate the prevalent characteristics of Fowl Typhoid and antibiotic susceptibility of Salmonella gallinarum isolated from 56 infective or dead chickens of 20 egg laying farms in Kyung Buk province during the period from August to December 1994. 1. Among 416, 000 chickens of 92 flocks in 20 egg laying farms, 17, 360 chickens of 31 flocks were died of Fowl Typhoid. 2. Salmonella gallinarum was isolated from 56 chickens in liver and spleen, and then blood of infective chickens was positive to Pullorum antigen. 3, In the survey of gross lesion of 56 chickens, 43 chickens(76.8%) were swelled at liver, 39(69.6%) were swelled at spleen, 12(21.4%) were changed with bronze, 3(5.4% ) were hemorrhagic in peritoneal cavity. 4. In transmission pattern, 4 farms were outbreaked the entrance of chicken house at first, but the others were outbreaked at various place. They were transmitted at right and left directions in flock. 5. 2 farms confirmed at the early stage of infection were eradicated by removing infective chickens and administrating antibiotics, but 18 farms at chronic stage were not. 6. The biochemical properties of 112 Salmonella gallinarum from chickens were generally identical to those of the referance, but H$_2$S was not productive, cellobiose was fermentive. 7 Minimum inhibitory concentration(MIC) of 20 isolates was performed by using 21 antibiotics, MICs of Amikacin(Ak), Gentamicin(Gm), Kanamycin(Km), and Tetracycline (Tc) were below 1.6 ug/ml, Ampicillin(Am), Furazolidone(Fu) and Neomycin(Nm) were below 3.1 ug/ml, Cephalothin(Ce), Cefazoline(Cf) and Chloramphenicol(Cm) were below 6.3 ug/ml, Nalidixic acid(Na), Polymyxin(Po) and Rifampicin(Rf) were below 12.5 ug/ml, Penicillin (Pm) was below 25 ug/ml, Colistin(Co) and Streptomycin(Sm) were below 50 ug/ml, Sulfamerazine(Sr) and Sulfamethazine (St) were below 200 ug/ml, Lincomycin(Lm) and Spiramycin(Sp) were below 400 ug/ml, Bacitracin(Ba) was below 800 ug/ml. 8. Among the 20 isolates, all(100%) of those were sensitive to Ak, Am, Ce, Cf, Cm, Fu, Gm, Km, Na, Nm, Po, Rf, Sr, St and Tc, but 6 isolates(30%) were resistent to Co, 20(100% ) to Ba, Lm, Pm, Sm, and Sp. The drug resistance patterns were simple which 6 strains were BaCoLmPmSmSp type, and 14 were BaLmPmSmSp type.

• Childhood Kidney Diseases
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• 제10권1호
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• pp.18-26
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• 2006

목적 : 요로감염은 조기 진단 및 치료를 적절히 하지 않으면 비가역적 신손상, 패혈증 등을 유발하므로 원인 균주를 알기 전에 경험적 항생제 요법을 시행하는 것이 중요하다. 따라서 경험적 항생제의 적절한 선택을 위하여 원인 균주의 분포와 임상특징을 알아보고, 원인 균주의 대부분을 차지하는 E. coli의 항생제 감수성 정도에 대해 알아보고자 하였다. 방법 : 2004년 2월부터 2005년 2월까지 발열을 주소로 분당차병원 응급실과 소아과 외래를 방문하여 요로감염으로 진단된 환아 103명을 대상으로 요 배양검사 결과, 성별, 연령, DMSA 신스캔상 결손 유무, 방광 요관 역류 유무, 6개월이내 재발 여부 등을 후향적으로 조사하고 원인 균주 중 가장 흔한 균인 E. coli에 대해 항생제 감수성 정도를 분석하였다. 결과 : 103명의 환아 중 92명(89.3%)이 E.coil에 의한 요로감염이었으며 ESBL 생성 E.coli는 3명(3.3%)에서 동정되었다. E. coli의 항생제 감수성 조사 결과 AMP, AMS, SXT는 각각 27.2%, 34.8%, 65.2%로 낮은 감수성을 보였으며 cephalosporin계 항생제는 1세대 cephalosporin인 cefazoline이 91.3%, 2세대인 cefoxitin이 100%, 3세대인 ceftriaxone 97.8%를 보여 대부분 매우 높은 감수성을 나타내었다. 또한 AMP와 SXT의 경우 연령이 1세 이상일 경우 1세 미만인 경우에 비해 내성의 위험이 증가하였다. 결론 : 1세 이상의 환아에서는 소아과 외래에서 흔히 사용하는 AMP, SXT에 대한 내성발생의 위험이 증가하므로 3세대 cephalosporin계 항생제를 초기 경험적 치료에 사용하는 것이 권장되나, ESBL 생성 E. coli에 대한 지속적인 조사와 발생 위험 요인에 대한 연구가 더욱 필요하다.