• Journal of Pharmaceutical Investigation
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• v.32 no.2
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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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• v.33 no.3
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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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• v.37 no.1
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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.

• Proceedings of the PSK Conference
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• 2003.10b
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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)

• Journal of Pharmaceutical Investigation
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• v.29 no.4
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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'.

• International Journal of Oral Biology
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• v.40 no.1
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• pp.41-50
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• 2015

The aim of this study was to identify bacteria isolated from the oral cavities and to determine their antimicrobial susceptibility against eight antibiotics. The bacterial strains were obtained from the Korean Collection for Oral Microbiology (KCOM). The bacteria were identified by comparing 16S rDNA sequences at the species level. The data showed that 77 bacterial strains were predominantly identified as streptococci (49.4%) and staphylococci (14.3%). Minimum inhibitory concentrations (MIC) were determined using a broth dilution assay to test the sensitivity of the bacterial strains. The MIC values of the oral bacterial strains against antibiotics were different. Streptococci were sensitive to clindamycin, cefuroxime axetil, and vancomycin, and they were resistant to tetracycline. Staphylococci also were sensitive to clindamycin, cefuroxime axetil, and vancomycin, and they were resistant to penicillin antibiotics. Gramnegative bacterial strains were sensitive to tetracycline and were resistant to clindamycin. These results suggest that the antimicrobial susceptibility test is necessary in deciding the prescription for antibiotics, to prevent the misuse or abuse of antibiotics.

• Biomolecules & Therapeutics
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• v.7 no.1
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• pp.44-53
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• 1999

The resistant strains due to the extended-spectrum $\beta$-lactamase (ESBL) were susceptible to cefatrizine combined with clavulanic acid. The purpose of this study was to evaluate the in vitro and in vivo antibacterial activities of cefatrizine/clavulanic acid (CTRZ/CV) combination at a ratio of 2 : 1 in comparison with cefaclor (CCLO), cefuroxime (CRXM), cefuroxime axetil (CRXMA) and amoxicillin/clavulanic acid (AMXCCV). CTRZ/CV showed good activity against laboratory strains of gram-positive and gram-negative bacteria and exhibited excellent antibacterial activity against $\beta$-lactamase-producing strains. The bactericidal activity of CTRZ/CV was superior to that of CCLO and CRXM, and almost equal to that of AMXCCV against the $\beta$-lactamase-producing strains. The in vitro results were substantiated. by in vivo mouse experimental infection studies with $\beta$-lactamase-producing and non-producing strains. In mixed experimental infection due to $\beta$-lactamase-producing and non-producing strains, the therapeutic efficacy of CTRZ/CV was superior to that of CTRZ, CCLO, CRXMA and AMXCCV. In respiratory tract infection in mice due to Klebsiella pneumoniae EB4O, CTRZ/CV was more erective than CCLO, CRXMA and AMXCCV and also more efficacious than CCLO, CRXMA and AMXCCV in urinary tract infection in mice due to Escherichia coli EB13. These results indicate that CTRZ/CV is a useful drug for the treatment of infection caused by $\beta$-1actamase-producing strains including ESBL-producing strains.

• Korean Journal of Microbiology
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• v.42 no.3
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• pp.185-194
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• 2006

The aim of this study was to identify the bacteria isolated from endodontic lesions by cell culture and to determine the antimicrobial susceptibility of them against 8 antibiotics. The necrotic pulpal tissues were collected from 27 infected root canals, which were diagnosed as endodontic infection. Samples were collected aseptically from the infected pulpal tissue of the infected root canals using a barbed broach and a paper point. The cut barbed broaches and paper points were transferred to an eppendorf tube containing $500{\mu}l\;of\;1{\times}PBS$. The sample solution was briefly mixed and plated onto a BHI-agar plate containing 5% sheep blood. The agar plates were incubated in a $37^{\circ}C$ anaerobic chamber for 2 to 5 days. The bacteria grown on the agar plates were identified by comparison of 16S rRNA gene (rDNA) sequencing method at the species level. To test the sensitivity of the bacteria isolated from the infected root canals against 8 antibiotics, minimum inhibitory concentrations (MIC) were determined using broth dilution assay. The data showed that 101 bacterial strains were isolated and were identified. Streptococcus spp. (29.7%) and Actinomyces spp. (21.8%) were predominantly isolated. The 9 strains were excluded in antimicrobial susceptibility test because they were lost during the experiment or were not grown in broth culture. The percentage of bacteria susceptible for each antibiotic in this study was clindamycin, 87.0% (80 of 92); tetracycline, 75.0% (69 of 92); cefuroxime axetil, 75.0% (69 of 92); amoxicillin + clavulanic acid (5:1), 71.7% (66 of 92); penicillin G, 66.3% (61 of 92); erythromycin, 66.3% (61 of 92); amoxicillin, 44.6% (41 of 92); and ciprofloxacin, 31.5% (29 of 92). The susceptibility pattern of 8 antibiotics was dependent on the host of the bacteria strains rather than the kinds of bacterial species. These results indicate that antibiotic susceptibility test should be performed when antibiotics are needed for the treatment of infected root canals.