• 대한본초학회지
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• 제20권2호
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• pp.171-179
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• 2005

Objectives & Methods : In order to evaluate the in vivo synergic effect of Mawhangyounpye-tang which was a traditional poly-herbal formula has been used in the treatment of respiratory diseases in Korea, with quinolone antibiotic, ciprofloxacin (CPFX), the viable bacterial number and histopathological changes were monitored after experimental respiratory infection with Klebsiella peumoniae NCTC 9632. Results : The obtained results were as follows : 1. In CPFX group, the viable bacterial numbers were significantly decreased compared to that of control group and these were more dramatically decreased compared to that of single treatment with CPFX, respectively in concomitant treated groups with Mawhangyounpye-tang. 2. In control group, severe infiltration of inflammatory cells, hemorrhage and hypertrophy of alveolar linings were demonstrated at microscopical levels. However, these abnormal histopathological changes were significantly decreased compared to that of control group in CPFX group, and these were more dramatically decreased compared to that of single treatment with CPFX, respectively in concomitant treated groups with Mawhangyounpye-tang. 3. In CPFX group, the LSA (luminal surface of alveoli %) were significantly increased compared to that of control group and these were more dramatically decreased compared to that of single treatment with CPFX, respectively in concomitant treated groups with Mawhangyounpye-tang. Conclusions : It is considered that in vivo antibacterial activity of CPFX was dramatically increased by concomitant use of Mawhangyounpye-tang against Kebsiella pneumoniae NCTC 9632 infection of respiratory tract.

• 약학회지
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• 제35권6호
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• pp.522-529
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• 1991

The purpose of this research is to evaluate effects of chloramphenicol, phenobarbital and progesterone on damage of DNA, RNA and protein which was induced by dimethylnitrosamine. $N,N-Di[^{14}C]$ methyl-nitrosamine (DMN) was used as a damaging agent and levels of DNA, RNA and protein damage in liver, brain and pancreas were compared with a control group. Pretreatment of mice with chloramphenicol increased protein damage in pancreas two times more than the control level. Liver RNA damage was increased up to 5.8 times and brain DNA damage up to 6.95 times by treatment of phenobarbital but brain RNA damage was decreased significantly down to 21% of the control group. The damage of liver RNA was significantly decreased by treatment of progesterone, although liver protein damage, pancreas RNA damage and pancreas protein damage were increased.

• Archives of Pharmacal Research
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• 제19권2호
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• pp.143-147
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• 1996

LB20304 is a novel fluoroquinolone that exhibits a potent broad spectrum antibacterial activity against both gram-positve and gram-negative bacteria. The MICs (Minimal Inhibitory Concentration) of LB20304 were determined against both gram-positve and gram-negative bacteria under various conditions including several media, pHs, and inoculum concentrations. The in vitro activity of LB20304 was not significantly affected by the changes in testing conditions such as components of media and inoculum concentrations, but it was slightly reduced by acid condition. The MICs and MBCs (Minimal Bactericidal Concentration) of LB20304 against Staphylococcus aureus, Escherichia coli and Pseudomonas aeruginosa were hardly affected by the presence of 50 % human serum, mouse serum, guinea pig serum or horse serum, and the MBCs were equal to or at most four-times higher than the MiCs. The activities of LB20304 were decreased by the presence of high concentraion of $Mg^{++}$ or human urine (pH, 5.5) in the test media. The frequencies of mutants resistant to LB20304 were similar to or lower than those found in ciprofloxacin and sparfloxacin.

• 약학회지
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• 제37권3호
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• pp.235-242
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• 1993

8-Fluorociprofloxacin(8-FCP) is an investigational quinolone derivative that is substituted with fluorine at the C-8 position of ciprofloxacin(CP). It was found that the in vitro activity of 8-FCP against Gram(+) bacteria was more potent that of CP, but the opposite against Gram(-) bacteria was true. However, 8-FCP showed better in vivo efficacy than CP against representative Gram(-) organisms, E. coli and K pneumoniae. In an attempt to seek for factors causing this discrepancy in the antibacterial activities, a comparative pharmacokinetic study of 8-FCP and CP was conducted in mice and rats treated either intravenously or orally at a single dose of 30 mg/kg. The pharmacokinetic parameters in mice were as follows; the mean peak serum concentrations(C$_{max}$) following i.v. and oral doses were 12.4 and 5.3 $\mu\textrm{g}$/ml for 8-FCP, and 9.5 and 2.5 $\mu\textrm{g}$/ml for CP, respectively. The terminal half-life(t$_{1/2\beta}$) was 72.9 min for 8-FCP, and 98.2 min for CP, and the oral bioavailability(F) was 89.9% for 8-FCP, and 50.5% for CP. In rats, the mean ($\pm$SD) $C_{max}$ after i.v. administration were 11.6$\pm$1.6 $\mu\textrm{g}$/ml for 8-FCP, and 10.2$\pm$1.3 $\mu\textrm{g}$/ml for CP, whereas oral administration produced $C_{max}$ of 5.9$\pm$1.8 $\mu\textrm{g}$/ml for 8-FCP and 1.1$\pm$0.9 $\mu\textrm{g}$/ml for CP, respectively. The t$_{1/2\beta}$ was 67.9$\pm$8.4 min for 8-FCP, and 76.4$\pm$7.2 min for CP. The F was 88.6$\pm$6.3% for 8-FCP, and 40.7$\pm$6.5% for CP. Marked differences were observed between the two quinolones in the $C_{max}$ and the area under the concentration-time curve obtained after oral administration in mice and rats. The extent of 8-FCP absorption in both mice and rats was approximately 2-fold higher than that of CP, suggesting that the fluorine atom attached to C-8 plays an important role in facilitating oral absorption from the gastrointestinal tract.

• 한국어병학회지
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• 제10권2호
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• pp.125-135
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• 1997

어류조직내에 잔류하는 항균물질을 미생물학적 방법인 disk assay를 이용하여 항균물질의 계열별로 확인이 가능한지를 검토하였다. 본 검사법에 사용한 균주는 Bacillus subtilis BGA, Micrococcus luteus ATCC 9341, Bacillus cereus var, mycoides ATCC 11778 이었다. 본 검사법에는 보다 간편한 clean-up 전처리 조작을 실시하였다. 즉, 피검시료(10g)는 Mcilvaine 완충액으로 마쇄하여 수용액충을 추출하고, 이 수용액층을 핵산에 의해 탈지시킨 후, 클로르포름 및 Sep-Pak $C_{18}$ 카트리지를 이용하여 분획액 2종류(fraction A 및 B)를 추출하였다. 그리고 이들 분획액은 각각 disk assay에 사용하였다. 분획액 A인 클로르포름 용액층은 마크로라이드(ML)계, 설파(SA)계, 클로람페니콜(CP)계 및 퀴놀른(QN)계의 확인시험에 제공되었고, 분획액 B인 Sep-Pak $C_{18}$에 흡착된 물질은 페니실린(PC)계, 테트라사이클린(TC)계 및 니트로푸란(NF)계의 확인시험에 제공되었다. 본 검사법에 의한 항균물질의 검출 최저농도는 oxytetracycline, tetracycline, doxycycline, spiramycin 및 ciprofloxacin이 $0.1{\mu}g$/g, erythromycin과 ampicillin이 $0.025{\mu}$/g, sodium nifurstyrenate와 florfenicol이 $1.0{\mu}g$/g, sulfamonomethoxine과 sulfadimethoxine이 $0.25{\mu}g$/g, oxolinic acid와 flumequine이 $2.5{\mu}g$/g, piromidic acid는 $15{\mu}g$/g이었다. TC계 및 NF계에 대해서는 B. cereus>B. subtilis>M. luteus, ML계 및 PC계에 대해서는 M. lureus>B. subtilis>B. cereus, CP계 및 QN계에 대해서는 B.cereus=B. subtilis>M. luteus, SA계에 대하여는 B. subtilis>B. cereus=M. luteus로 항균물질의 계열에 따라 서로 다른 감수성 유형을 나타내었다. 따라서 본 미생물학적 검사법은 어류 조직내에 잔류하는 항균물질의 계열을 스크리닝하는 일상 검사법으로서 유용하게 활용될 수 있을 것으로 사료된다.

• Tuberculosis and Respiratory Diseases
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• 제55권1호
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• pp.69-87
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• 2003

배 경 : Gemifloxacin은 그람음성 및 그람양성 균주에 대해서 모두 좋은 활성을 가지고 있는 fluoroquinolone 항균제로서, 임상균주를 이용한 in vitro 시험에서 다른 대조 quinolone에 비하여 S. pneumnoniae의 penicillin 내성 균주에 대해서 활성이 높을 뿐만 아니라, 다른 quinolone 항균제에 내성을 나타내는 S. pneumoniae 임상 균주에 대해서도 좋은 활성을 유지하는 것으로 밝혀져 만성기관지염의 급성악화(AECB)시 사용하기 적절한 치료제로 여겨진다. 목 적 : 한국인에서 AECB를 치료하기 위한 LB20304(gemifloxacin) 160mg 또는 320rng 1일 1회 7일간 투여의 유효성과 안전성을 평가하고자 하였다. 방 법 : Gemifloxacin 100mg과 위약을 1일 1회 7일간 경구 투여한 환자 67명, gemifloxacin 320mg을 1일 1회 7일간 경구 투여한 환자 70명의 환자를 대상으로 무작위 배정, 이중맹검, 병행 치료군, 다기관, 2상 임상시험으로 실시하였다. 결 과 : 두 치료군의 인구통계학적 특징과 임상적 및 흡연 기왕력 등 기저 상태는 대등하였다. Per-protocol(PP) 환자군에서, 추적관찰 시점(days 14-21) 및 치료종료 시점(days 7-10)에서의 임상적 반응은 gemifloxacin 100mg군이 각각 84.2%, 96.5%, 320mg군이 각각88.7%, 96.4%로 두 군간에 유의한 사이가 없었고(각각 p=0.49, p=0.99), 추적관찰 시점 및 치료종료 시점의 미생물학적 반응도 gemifloxacin 160mg군이 각각 78.9%, 81.8%, 320mg군이 각각 84.2%, 86.4%로 두 군간에 유의한 차이가 없었다(각각 p=0.68, p=0.68) 본 임상시험에서 치료 전에 많이 배양된 병원균으로는 S. pneumoniae(12/52), H. influenzae(10/52), K. pneumoniae(6/52), M. catarrhalis(3/52) 로 K. pneumoniae가 비교적 많이 배양된 점을 제외하고는 기존에 알려진 AECB 시 배양되는 병원균의 분포와 큰 차이가 없었다. S. pneumoniae, H. influenzae, K. pneumoniae, M. catarrhalis 등 주요 병원 균에 대한 MIC는 전반적으로 다른 quinolone 항균제보다 gemifloxacin이 더 낮았고, 특히 S. pneumoniae(3 PRSP, 7 ERSP 포함)에 대한 gemifloxacin의 MIC(${\leq}0.03ug/ml$)는 다른 quinolone, beta-lactam, macrolide 항균제보다 월등히 낮아 gemifloxacin 이 AECB의 치료에 매우 유용한 항균제임을 보여주었다. 안전성 결과에서는 gemifloxacin 160mg 및 320mg 투여군 모두 시험약과의 관련성을 배제할 수 없거나 관련이 의심되는 중대한 이상반용은 관찰되지 않았고, 치료 중 및 치료 후 30일 기간동안, 이상반응을 최소한 하나 이상 보고한 환자가 gemifloxacin 160mg군은 26.9%, 320mg군은 31.4%이었다. 가장 흔히 보고된 이상반응은 간효소 수치의 증가로서, 발생 빈도는 160mg군에서 1/67명(1.5%), 320mg군에서 5/70명(7.1%) 이었다. 간효소 수치의 증가로 인해 탈락한 환자는 없었고, 중증도(severity)는 모두 경도(mild)였으며, 별다른 처치 없이 정상으로 회복되었다. 전반적인 이상반응의 profile에서 치료군간 주요한 차이는 없었다. 결 론 : 본 임상시험의 결과, 한국인에서 AECB를 치료하기 위한 gemifloxacin 160mg 또는 320mg 1일 1회 7일간의 투여는 임상적 및 미생물학적으로 매우 유효하고 안전하였다.

• 동의생리병리학회지
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• 제18권6호
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• pp.1740-1745
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• 2004

In order to evaluate the in vitro synergic effect of Eunkyo-san, with quinolone antibiotics, rufloxacin (RUFX), the minimal inhibitory concentration (MIC), MIC50 and MIC90 of single use of quinolones and concomitant treatment with Eunkyo-san against 9 strains of aerobic gram positive bacteria. The obtained results were as follows : In the case of aerobic gram positive bacteria, the MIC, MIC50 and MIC90 against Staphylococcus aureus, Staphylococcus aureus smith, Staphylococcus epidermidis, Staphylococcus pyogens, Streptococcus pneumoniae Type Ⅰ, Type Ⅱ and Type Ⅲ was significantly decreased in concomitant treated groups with Eunkyo-san compared to those of single treated groups of RUFX, respectively. However, no significant changes were demonstrated against Bacillus subtilis and Enterococcus faecalis. In conclusion, the in vitro antibacterial activity of RUFX were increased against some strains of aerobic gram positive strains, especially, pneumococcus such as Staphylococcus and Streptococcus by concomitant use of Eunkyo-san.

• 대한한의학회지
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• 제26권2호
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• pp.13-24
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• 2005

Objectives & methods; In order to evaluate the in vivo synergic effect of Mawhangyounpye-tang, a traditional poly-herbal formula used in the treatment of respiratory diseases in Korea, with the quinolone antibiotic ciprofloxacin (CPFX), the viable bacterial number and histopathological changes were monitored after experimental respiratory infection with Streptococcus Pneumoniae ATCC 6303. Results: 1. In CPFX groups, the viable bacterial numbers were significantly decreased compared to that of the control group, and were even more dramatically decreased in concomitant group treated with Mawhangyounpye-tang. 2. In the control group, severe infiltration of inflammatory cells, hemorrhage and hypertrophy of alveolar linings were demonstrated at microscopic levels. However, these abnormal histopathological changes were significantly decreased compared. to that of the control group in CPFX groups, and were even more dramatically decreased in concomitant groups treated with Mawhangyounpye-tang. 3. In CPFX groups, the LSA (Iuminal surface of alveoli $\%$) were significantly increased compared to that of the control group, and more dramatically in concomitant groups treated with Mawhangyounpye-tang. Conclusions: According to these results, it is considered that the in vivo antibacterial activity of CPFX against Streptococcus Pneumoniae ATCC 6303 infection of respiratory tract was dramatically increased by concomitant use of Mawhangyounpye-tang.

• 한국동물위생학회지
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• 제23권1호
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• pp.19-28
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• 2000

There are several main antibacterial susceptibility tests, such as agar dilution method, broth dilution method and disk diffusion technique. Especially, for minimal inhibitory concentration (MIC) test, agar dilution method has been widely used. But that method is so complicated and bothering that it's difficult to treat a large amount of strains. On the other hand, modified broth dilution method(add 1% glucose and 0.018% phenol red as a pH indicator to broth) is fast and easy to perform. Most of all, it can visualize the result by color. The MICs of 22 antibiotics Including penicillins, aminoglycosides, cephalothin, chloramphenicol, lincomycin, ceftiofur, vancomycin and quinolones, erythromycin, colistin. sul-fadimethoxine, trimethoprim for arcanobacterium pyogenes 14 strains, actinobacillus pleuropneu-moniae 41 strains and pasteurella multocida 37 strains, which were collected from porcine during 1996 ∼ 1999, were determined by modified broth dilution method. Actinobacillus pleuropneumoniae was highly susceptible to all kinds of quinolones such as ciprofloxacin, enrofloxacin and norfloxacin and to all aminoglycosides, like gentamicin, apramycin, kanamycin and ampicillin, cephalothin and ceftiofur. But It was quite resistant to solfadimethoxin, colistin and vancomycin. Pasteurella multocida was found to have high susceptibility to ampicillin, cephalothin, chlorampenicol and gentamicin but had mid-degree susceptibility to other aminoglycosides. In addition, it was susceptible to norfloxacin and nalidixic acid, but not to newer fluoroquinolone like ciprofloxacin and enrofloxacin and it was resistant to colistin and kanamycin. Arcanobacterium pyogenes was highly susceptible to most of quinolones such as cipoofloxacin, enrofloxacin and norfloxacin and gentamicin and penicillin G. But it also obtained high resistance against the early quinolone, nalidixic acid and aminoglycosides such as amikacin, apramycin and kanamycin and erythromycin, chlorampenicol, tetracyclin and vancomycin.

• 공업화학
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• 제5권3호
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• pp.501-508
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• 1994

방출조절성 약제를 개발하기 위한 방법으로 1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-7-(1-piperazinyl)quitoline-3-carboxylic acid의 $C_3$ 위치를 Vilsmeier reagent로 chlorination하여 이를 dextran과 반응시켜 1-ethyl-6-fluoro-1, 4-dihydro-4-oxo-7-(1-piperazlnyl) quinoline-3-carboxylic acid-dextran 중합체약을 합성하였다. 중합체약에 대한 최소발육저지농도(MICs)로서 Gram 양성세균 Bacillus subtillis ATCC 6633, Staphyloccus aureus ATCC 25923, Mycrobacterium phlei IFO 3158 및 Salmonella typhimurium KCTC 1925에 대해서 각각 $5{\mu}g/ml$의 농도로 균의 발육을 억제하였다. Micrococcus luteus ATCC 9341에 대해서는 $80{\mu}g/ml$로 약한 활성을 보였을 뿐, Gram 양성세균들에 대하여 전반적으로 강한 저항성을 보여주었다. Gram 음성세균인 Escherichia coli KCTC 1039, Escherichia coli ESS, Klebsiella puenmouiae KCTC 1560 및 Psendomonas aeruginosa IFO 13130 균주들에 대해서도 각각 $5{\mu}g/ml$로 대조물질과 유사한 항균성을 보여주었다. 한편, quinolone계 항균제가 진균류에 대하여 감수성을 보이지 않는 것처럼 중합체약도 진균인 Candida albicans ATCC 10231에 대해서는 감수성을 보여주지 않았다.