• Archives of Pharmacal Research
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• 제18권3호
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• pp.173-178
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• 1995

Ciprofloxacin resistance mechanisms were studied by investigating the inhibitory effect of ciprofloxacin on the gyrase-mediated DNA supercoiling and the intracellular accumulation of ciprofloxacin in clinical isolates of Pseudomonas aeruginosa. A higher amount of ciprofloxacin was required to inhibit the gyrases purified from the ciprofloxacin-resistant strains than that from the sensitive strain. Reconstitution of heterologous gyrase subunits from different strains revealed alterations in the A and/or the B subunits of gyrase in these strains. In addition, the resistant strains accumulated approximately a half amount of ciprofloxacin inside the cells, compared to the sensitive strain. However, when the active efflux was blocked by carbonyl cyanide m-chlorophenyl hydrazone treatment, intracellular concentration of ciprofloxacin was elevated about 4-7 fold in these strains, while the sensitive strain was not significantly affected by this treatment, indicating that the ciprofloxacin-resistant strains developed a drug efflux system. Interestingly, these resistant strains expressed an envelope protein of approximately 51 kD. These studies suggest that alterations in the gyrase as well as the active drug-efflux system conferred dual ciprofloxacin resistance mechanisms to these clinical isolates of P. aeruginosa.

• 약학회지
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• 제44권6호
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• pp.572-577
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• 2000

The effects of ibuprofen on bioavailability of ciprofloxacin were studied in rabbits. Animals were divided into three groups ; group A received 60 mg/kg of ciprofloxacin; group B and C received 60 mg/kg of ciprofloxacin with 60 and 240 mg/kg of ibuprofen, respectively. Ciprofloxacin and ibuprofen were given by single oral administration. Serum concentrations of ciprofloxacin were measured by high performance liquid chromatography with UV detector and pharmacokinetic parameters were calculated. Area under the serum concentrations versus time curve (${\pm}\;S.E.$) of ciprofloxacin were decreased in group B and C compared with group A ($12.26\;{\pm}\;0.94$ and $12.57\;{\pm}\;0.94$ vs. $15.71\;{\pm}\;1.06\;{\mu}g{\cdot}hr/ml$, p<0.05), whereas total clearances were increased ($1.81\;{\pm}\;0.13$ and $1.76\;{\pm}\;0.12$ vs. $1.40\;{\pm}\;0.09\;l/hr/kg$, p<0.05). No significant differances in these parameters were observed between group B and C. Relative bio-availability of group B and C to group A were 78 and 80%, respectively. These results suggest that the coadministration of ibuprofen with ciprofloxacin may reduce the bioavailability of ciprofloxacin.

• Bulletin of the Korean Chemical Society
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• 제28권4호
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• pp.543-546
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• 2007

Herein, a new electrochemical method was described for the determination of ciprofloxacin based on the enhancement effect of an anionic surfactant: sodium dodecyl benzene sulfonate (SDBS). In pH 4.0 phosphate buffer and in the presence of 1.0 × 10-4 mol/L SDBS, ciprofloxacin yields a well-defined and sensitive oxidation peak at the carbon paste electrode (CPE). Compared with that in the absence of SDBS, the oxidation peak current of ciprofloxacin remarkably increases in the presence of SDBS. The experimental parameters, such as supporting electrolyte, concentration of SDBS, and accumulation time, were optimized for ciprofloxacin determination. The oxidation peak current is proportional to the concentration of ciprofloxacin over the range from 8.0 × 10-8 to 5.0 × 10-6 mol L-1. The detection limit is 2.0 × 10-8 mol L-1 after 2 min of accumulation. This new voltammetric method was successfully used to detect ciprofloxacin in drugs.

• 한국수산과학회지
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• 제41권6호
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• pp.440-445
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• 2008

Ciprofloxacin is the most commonly used fluoroquinolones for treating bacterial disease in olive flounder (Paralichthys olivaceus) farming, but its withdrawal time for industrial-scale farming has not been established. The depletion of ciprofloxacin was investigated in the olive flounder under field conditions. Fish were kept in an inland fish farm and fed a commercial diet containing 5 mg/kg of ciprofloxacin for 13 days. Seven fishes per sampling time were examined during and after the treatment. Ciprofloxacin and its major metabolite, enrofloxacin, were analyzed using HPLC with a fluorescence detector. The concentrations of ciprofloxacin and enrofloxacin in muscle increased during the medication period, and then decreased rapidly. The ciprofloxacin and enrofloxacin concentration in the olive flounder peaked on days 11 and 13, respectively, with maximum concentrations in muscle of 0.58 and 0.73 mg/kg. Residual ciprofloxacin and enrofloxacin were eliminated rapidly; 6 days after treatment, the respective levels in muscle were 0.04 and 0.10 mg/kg and neither was detected 15 days post treatment. The level of ciprofloxacin accumulation at the beginning of oral administration was variable according to the farming conditions, but the overall exhaustion time was similar. In conclusion, an adequate withdrawal period for enrofloxacin is 15 days in the case of oral ciprofloxacin administration.

• Journal of Pharmaceutical Investigation
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• 제39권6호
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• pp.451-456
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• 2009

The purpose of the present study was to evaluate the bioequivalence of two ciprofloxacin tablets, Ciprobay (Bayer Korea Ltd.) and Rofcin (Binex Co., Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). The release of ciprofloxacin from the two ciprofloxacin tablets in vitro was tested using KP XIII Apparatus I method with dissolution media (0.01 M HCl). The dissolution profiles of two ciprofloxacin tablets were very similar at dissolution media. Twenty four healthy male volunteers were divided into two groups and a randomized 2$2{\times}2$2 cross-over study was employed. After one tablet (250 mg ciprofloxacin) was orally administrated, blood was taken and the concentrations of ciprofloxacin in serum were determined using HPLC with UV detector. The pharmacokinetic parameters such as $AUC_t,\;C_{max}\;and\;T_{max}$ were calculated. The results showed that the differences in $AUC_t,\;C_{max}\;and\;T_{max}$ between two ciprofloxacin tablets based on the Ciprobay were -0.63%, 3.98% and -9.23%, respectively. There were no sequence effects between two tablets in these parameter. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log(0.8) to log(1.25)(e.g., log(0.9520)~log(1.0523) and log(0.9689)~log(1.1663) for $AUC_1\;and\;C_{max}$, respectively). Thus, Rofcin tablet was bioequivalent to Ciprobay tablet.

• 대한수의학회지
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• 제37권1호
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• pp.195-202
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• 1997

A method for the isolation by matrix solid phase dispersion method and liquid chromatographic determination of enrofloxacin and ciprofloxacin in pork muscle tissue is presented. Blank or enrofloxacin and ciprofloxacin spiked samples(0.5g) containing 0.05g oxalic acid were blended with $C_{18}$(octadecylsilyl derivatized silica) packing material. After homogenization, $C_{18}$/muscle tissue matrix was transferred to glass column made from 10ml glass syringe and filter paper, and compressed to 4~4.5ml volume. A column was washed with 8ml of hexane and dried under vacuum. Interfering materials were removed by ethylacetate 8ml and dried, following which enrofloxacin and ciprofloxacin were eluted with 8ml of methanal under gravity. The eluate containing enrofloxacin and ciprofloxacin wase free from interfering compound when analysed by HPLC with UV detection at 278nm. Enrofloxacin and ciprofloxacin showed linear response with UV detector at the range of $0.05{\sim}1.0{\mu}g/ml$ and eluted within 5ml elution volume of methanol from the matrix. Fortified sample containing 0.05g oxalic acid represented more good recoveries than that of control sample. Average percentages of enrofloxacin and ciprofloxacin were $93.30{\pm}4.56%$ and $91.84{\pm}4.17%$, respectively, for the concentration range(0.05, 0.1, 0.25, 0.5 and $0.75{\mu}g/g$). The interassay variability of enrofloxacin was $6.02{\pm}5.33%$ with an intra-assay variability of 4.89% and $6.75{\pm}2.68%$ with 4.54% for ciprofloxacin. Detection limit of enrofloxacin and ciprofloxacin was $0.030{\mu}g/g$ in the spiked sample.

• 대한수의학회지
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• 제44권4호
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• pp.643-648
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• 2004

Efficacy of ciprofloxacin was evaluated in laboratory and field studies for control of streptococcal infection in flounder and eel. In disc diffussion test, all streptococcal strains showed high sensitivity to the ciprofloxacin. Minimum inhibitory concentrations of ciprofloxacin against all streptococcal strains used in this study were less than $0.195{\mu}g/ml/$. In laboratory studies where fishes were challanged with Streptococcus iniae, significant reductions in mortality were observed among fish receiving ciprofloxacin (in fed) at 100 mg/kg/body weight or more daily for 3 d when compared with mortality of non-medicated controls. Similar results were achieved when 100 mg/kg/body weight of ciprofloxacin was used in field trials.

• Tuberculosis and Respiratory Diseases
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• 제38권4호
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• pp.372-378
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• 1991

Some kinds of newer fluoroquinolone antibiotics are known to interact with theophylline, which is widely used as a potent bronchodilator in asthma or chronic obstructive lung disease. To evaluate the effect of enoxacin and ciprofloxacin on the metabolism of theophylline, aminophylline was administered intravenously in bolus (6 mg/kg) over 30 minutes to 6 healthy volunteers (age: $23.3{\pm}4.2$ year, body weight: $63.2{\pm}9.0\;kg$, height: $169.0{\pm}6.5\;cm$, female 3, male 3) before and after per oral 5-day medication of enoxacin and ciprofloxacin, respectively and we measured the level of theophylline in serum. The results were as follows: 1) Enoxacin and ciprofloxacin did not influence the volume of distribution significantly. 2) Enoxacin decreased the clearance of theophylline significantly (from $42.9{\pm}14.6\;ml/min$ to $30.1{\pm}6.3\;ml/min$: p<0.05), but ciprofloxacin did not cause significant decrease (to $32.8{\pm}6.2\;ml/min$: p>0.005). 3) Enoxacin increased the elimination half life of theophylline significantly (from $496{\pm}83\;min$ to $693{\pm}32\;min$: p<0.001), but ciprofloxacin did not cause significant increase (to $687{\pm}222\;min$: p>0.05). These results suggested that enoxacin influenced clearance and elimination half life significantly and thorough monitoring of the level of theophylline in patients with coadminstration of enoxacin and theophylline was necessary. In case of ciprofloxacin, the influence on the metabolism of theophylline was not statistically significant, but one exceptionally large decrease of the clearance and increase of the elimination halflife of theophylline suggested the necessity of monitoring of theophylline level during coadministration of ciprofloxacin and theophylline.

• Bulletin of the Korean Chemical Society
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• 제29권6호
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• pp.1173-1178
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• 2008

A simple and sensitive high-performance liquid chromatographic method was developed for the simultaneous identification of enrofloxacin and its active metabolite ciprofloxacin in chicken muscle. Norflorxacin imprinted polymers synthesized in water-containing systems show high selectivity to enrofloxacin and ciprofloxacin in an aqueous environment. Using these water-compatible imprinted polymers as selective adsorbents in the solid-phase extraction of enrofloxacin and ciprofloxacin from chicken samples, the remaining biological matrix could be quickly washed out from the imprinted column while enrofloxacin and ciprofloxacin were selectively retained and enriched. Analytical separation was performed on a $C_{18}$ column using acetonitrile-water as a mobile phase and fluorescence detection. Good linearity was obtained from 0.8 to 500 ng/g (r > 0.998) with relative standard deviation of less than 3.9%. The mean recoveries of enrofloxacin and ciprofloxacin from chicken muscle were 80.6-94.5% and 77.8-91.8% at three different concentrations. The limits of determinations based on S/N=3 were 0.07 ng/g and 0.09 ng/g, which are below the maximum residue limits established in many countries.

• 대한핵의학회지
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• 제35권1호
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• pp.75-80
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• 2001

목적: 새로운 감염영상법인 Tc-99m Infecton 스캔은 4-fluoroquinolone 계열의 광범위 항생제인 ciprofloxacin의 유도체를 이용한 것인데 이에 사용되는 Infecton의 항균력에 대한 연구는 접하기 어렵다. 저자들은 표준 균주에서의 Infecton의 항균력을 ciprofloxacin과 비교 분석하고자 본 연구를 시행하였다. 대상 및 방법: Infecton의 표준 균주 3종 (Staphylococcus aureus ATCC 29213, Escherichia coli ATCC 25922, 및 Pseudomonas aeruginosa ATCC 27853)에 대한 최소발육억제농도(minimum inhibitory concentration, MIC)와 최소살균농도 (minimum bactericidal concentration, MBC)를 검사하여, ciprofloxacin과 비교하였다. Ciprofloxacin과 Infecton의 MIC와 MBC는 표준균주에서 5회 검사하여 결과를 평균${\pm}$표준오차(범위)로 나타내었다. 결과: Infecton과 ciprofloxacin 의 MIC 결과는 S. aureus ATCC 29213에서 각각 $1.12{\pm}0.2\;(0.8{\sim}1.6){\mu}g/ml$이었으며 (p=0.016), E. coli ATCC 25922 에서는 각각 $0.03{\pm}0.005\;(0.025{\sim}0.05){\mu}g/ml,\;0.011{\pm}0.001\;(0.006{\sim}0.012){\mu}g/ml$이었고(p=0.007), P. aeruginosa ATCC 27853에 대해서는 각각 $0.96{\pm}0.16\;(0.8{\sim}1.6){\mu}g/ml,\;0.56{\pm}0.1\;(0.4{\sim}0.8){\mu}g/ml$로(p=0.66), 표준 균주 3종 모두에서 Infecton의 MIC가 ciprofloxacin 보다 $2{\sim}4$배 더 높았으나, 미국 National Committee for Clinical Laboratory Standards (NCCLS)가 정한 바에 의한 MIC 정도관리범위 내의 농도을 보이고 있었다. 또한, Infecton 과 ciprofloxacin의 MBC 결과는 S. aureus ATCC 29213에서 각각 $2.6{\pm}0.4\;(1.6{\sim}3.2){\mu}g/ml,\;0.88{\pm}0.19\;(0.4{\sim}1.6){\mu}g/ml$였고(p=0.009), E. coli ATCC 25922에서는 각각 $0.035{\pm}0.006\;(0.025{\sim}0.05){\mu}g/ml,\;0.02{\pm}0.008\;(0.025{\sim}0.05){\mu}g/ml$ 였으며 (p=0.114), p. aeruginosa ATCC 27853에서는 각각 $2.2{\pm}0.4\;(1.6{\sim}3.2){\mu}g/ml$와 $1.4{\pm}0.2\;(0.8{\sim}1.6){\mu}g/ml$로서(p=0.16), 표준균주 3종 모두에서 Infecton의 MBC 또한 ciprofloxacin에 비해 $2{\sim}4$배가 높았다. 결론: Tc-99m Infecton은 ciprofloxacin 보다는 약하였지만 표준균주에 대해 생체외 항균력을 보였다.