• Journal of Pharmaceutical Investigation
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• 제32권2호
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• pp.73-80
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• 2002

Cefuroxime axetil is a cephalosporin antibiotic having a high activity against a wide spectrum of Grampositive and Gram-negative microorganisms. It is a cephalosporin antibiotic which exist as 2 diastereoisomers: diastereoisomer A and B. It shows polymorphism of three forms: a crystalline form having a melting point of about $180^{\circ}C$, a substantially amorphous form having a high melting point of about $135^{\circ}C$ and a substantially amorphous form having a low melting point of about 70^{\circ}C$. The crystalline form of cefuroxime axetil is slightly soluble in water because diastereoisomer A has lower solubility than B in water. Substantially amorphous form of which there are no difference in solubility between diastereoisomer A and B has better solubility than crystalline form, but it forms a thicker gel than crystalline form upon contact with an aqueous medium. Based on this reason, cefuroxime axetil is not readily absorbable in the gastrointestinal tract, rendering its bioavailability on oral administration very low. The object of this study was to develop an improved non-crystalline cefuroxime axetil composition having a high physicochemical stability and bioavailability. A non-crystalline cefuroxime axetil solid dispersant showing no peak on a Differential Scanning Calorimetry (DSC) scan is prepared by dissolving cefuroxime axetil and a surfactant in an organic solvent; suspending a water-insoluble inorganic carrier in the resulting solution; and spray drying the resulting suspension to remove the organic solvent, said solid dispersant having an enhanced dissolution and stability of cefuroxime axetil and being useful for the preparation of a pharmaceutical composition for oral administration. Tablet was formulated with this cefuroxime axetil solid dispersant, disintegrants and other ingredients. It disintegrated and dissolved easily and dynamically in dissolution medium, so showed a good dissolution profile.

• Journal of Periodontal and Implant Science
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• 제33권3호
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• pp.341-348
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• 2003

The purpose of this study was to determine the minimal inhibitory concentration (MIC) of cefuroxime axetil,　semisynthetic cefalosporin, for some putative periodotopathogens; F. nucleatum, A. actinomycetemcomitans P. intermedia and P. gingivalis. To investigate the efficacy of cefuroxime axetil, several antibiotics, amoxicillin, metronidazole, and ciprofoxacine, were used as control. The MIC was measured by Murray' s method. The MIC of cefuroxime axetil against some putative microbes, as a single use regimen, was relatively high in comparison with that of the other antibiotics used in this study. The MIC of cefuroxime axetil/metronidazole against some putative microbes, as a simultaneous regimen, was similar to that of the other antibiotics used in this study. The manimal level of cefuroxime concentration in gingival fluid was 9${\mu}$/ml at 36hr after the first dose. In conclusion, within the limited experiment, metronidazole/ cefuroxime axetil therapy of periodontitis may provide a therapeutic benefits in reducing the periodontopathogens.

• Journal of Pharmaceutical Investigation
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• 제37권1호
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• pp.23-26
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• 2007

Two crystal forms of cefuroxime axetil were obtained by the recrystallization from different organic solvents and characterized by differential scanning calorimetry (DSC), X-ray powder diffraction (XRD). It was confirmed that two crystal forms are identical. The dissolution patterns of these two forms were also checked in 0.07 N HCl at $37{\pm}0.5^{\circ}C$, 100 rpm for 180 minutes. The transformation during storage was also studied.

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.2-2
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• pp.237.1-237.1
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• 2003

Cefuroxime axetil, a broad spectrum antibiotic, has been known to form a gelatinous mass in contact with aqueous media, which could lead to poor dissolution. Therefore, this study was conducted for removing the gelling phenomenon and thereby obtaining a favorable dissolution profile. We have found that the addition of poly (methacrylic acid, methyl methacrylate) could not only inhibit the tendency of cefuroxime axetil to form a gel but also showed the good dissolution profile compared to the formula without poly (methacrylic acid, methyl methacrylate). (omitted)

• 대한수의학회지
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• 제50권4호
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• pp.279-284
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• 2010

Combination therapy of antibiotics is leading to improved efficacy or safety profiles with decrease emergence of bacterial resistance. Because of this benefit, many of antibacterial combinations have been used in veterinary practice for the past few decades. The purpose of this study was to examine the in vitro activity of an amoxicillin alone and in combination with other antibiotics against pathogenic bacteria of fish origin. Based on the fractional inhibitory concentration (FIC) index (FIC $$\leq_-$$ 0.5), a synergistic interaction was shown in combination of florfenicol with amoxicillin or cefuroxime. The combination of florfenicol and amoxillin showed higher antibacterial activity than that of florfenicol and cefuroxime. Ratio of amoxicillin and florfenicol in combination was 1 : 1, which showed the antibacterial activity against bacterial isolates of fish as compared with other ratios. A synergetic effect of the combination (amoxicillin and florfenicol) was further confirmed in the time-kill curve study. The study showed a better in vitro antibacterial activity of a 1 : 1 combination of amoxicillin and florfenicol than the individual antibacterial against bacterial isolates of fish. In conclusion, the combination of florfenicol and amoxicillin may serve as a potential antibacterial therapy in fishes infected pathogenic bacteria.

• Journal of Pharmaceutical Investigation
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• 제29권4호
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• pp.361-365
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• 1999

The bioequivalence of 'Bearcef tablet' (Daewoong Pharmaceutical Co.), containing 250 mg cefuroxime (as cefuroxime axetil), in reference to 'Zinnat tablet' (GlaxoWellcome Korea Co.) was evaluated in 16 normal volunteers $(age\; 21{\sim}29\;yrs)$ following the oral administration. After one tablet was administered, blood was taken at predetermined time intervals and the concentration of the drug in plasma was quantitated with an HPLC method. AUC, $C_{max}$ and $T_{max}$ were calculated and statistically analyzed for the bioequivalence of the two products. The results showed that the differences in AUC, $C_{max}$ and $T_{max}$ between two products were 6.92%,3.49% and 5.26%, respectively. The powers for AUC, $C_{max}$ and $T_{max}$ were >90%, >90% and 89.0%, respectively. Confiderice intervals for these parameters were all within ${\pm}20%$. Judging based on the above results, 'Bearcef tablet' is regarded to be bioequivalent to 'Zinnat tablet'.

• 한국임상약학회지
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• 제6권2호
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• pp.28-31
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• 1996

The in vitro inactivation of gentamicin and tobramycin by four cephalosporins (cefotetan, cefuroxime, cefodizime, cefotiam) in human serum was investigated. Each cephalosporin was added to human serum samples containing gentamicin sulfate or tobramycin sulfate. Blank samples containing only aminoglycosides were used as controls. Samples were stored at -20, 4 and $25^{\circ}C$ and were analyzed for aminoglycoside concentrations by fluorescence polarization immunoassay ($TDxFLx^{TM}$ system) at 0, 2, 4, 8, 12, 24, 48 and 72 hours after mixing. The serum containing cefotiam stored at $25^{\circ}C$ showed significant inactivation of gentamicin by $12\%$ at 72 hours. The results indicate that cefotitan, cefuroxime and cefodizime do not inactivate gentamicin and tobramycin while cefotiam inactivates gentamicin.

• 한국임상약학회지
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• 제15권2호
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• pp.75-81
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• 2005

Community acquired pneumonia (CAP) remains a prevalent and potentially life threatening illness. American Thoracic Society and Infectious Disease Society America recommend combination therapies with ${\beta}-lactam$ plus a macrolide or a fluoroquinolone monotherapy for the empirical treatment of CAP. The aim of this study was to compare moxifloxacin monotherapy with cephalosporin plus azithromycin combination therapies. From January 2004 to March 2005, 18 patients in the moxifloxacin group(MG) and 21 patients in the cefuroxime or ceftriaxone plus azithromycin group(CAG) with CAP were retrospectively reviewed with regard to clinical, laboratory and microbiological data. Each patient was stratified into mild (risk class I-II), moderate (risk class III) and severe (risk class VI, V) group according to and PSI (Pneumonia Severity Index) score. Each group was compared for microbiological eradication, clinical assessment, the length of hospital stay. As results, Total 39 patients with CAP were reviewed. The appropriateness of admission was 83.3% in MC vs. 76.2% in CAC. The mean length of the hospital day was for 8.31 days vs. 7.39 days, days switching parenteral to oral antibiotics in 5.19 days vs. 5.28 days, clinical improvement in 2.43 days vs. 2.61 days in MG vs. CAC. Radiological improvement required 3.75 days vs 3.63 days in MG vs. CAG and bacteriological eradication rate at discharge was the same in the both groups. Mortality rate was 11.1% (2 of 18) vs 14.3% (3 of 21) in MG vs. CAG (p=0.77). Drug cost of the mean 5 hospital days requiring parenteral antibiotics was the most inexpensive in moxifloxacin group for the 147,045 won, and ceftriaxone 1g-azithromycin group for the 170,285 won, cefuroxime bid-azithromycin group for the 207,800 won, ceftriaxone 2g-azithromycin group far the 220,570 won, cefuroxime tid-azithromycin group for the 251,700 won. There was no significant statistical difference in clinical, bacterial, radiological cure and hospital days, and switch to oral days. In conclusion, that i.v. moxifloxacin monotherapy was as effective as azithromycin plus cefuroxime or ceftriaxone combination therapies fur the treatment of CAP. In drug cost analysis, moxifloxacin is less expensive than CAG.

• Archives of Pharmacal Research
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• 제7권1호
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• pp.11-15
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• 1984

Binding of sic cephalosporins (cefotaxime, cefuroxime, cafazoline, cephalothin, cephaloridine, cephacetrile) to human 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-surfonate was used as the fluorescence probe, and 2-(4'-hydroxybenzeneazo)benzoic acid as the UV spectrophotometric probe. Competitive bindings between cephalosporins and probe were observed. For the binding of cephalosporins to human serum albumin, three binding sites were identified by fluorescence probe technique but four binding constants of cephalosporins to human serum albumin measured by fluorescence probe technique are higher than those meausred by UV spectrophotometry.

• 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.