• 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)

• 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'.

• International Journal of Oral Biology
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• 제40권1호
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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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• 제7권1호
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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.

• 미생물학회지
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• 제42권3호
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• pp.185-194
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• 2006

본 연구는 치근관 감염병소에서 세균을 분리 및 동정하고, 8종의 항생제들에 대한 분리균주들의 감수성을 조사하기 위하여 실시하였다. 세균에 감염된 27개 치아의 괴사된 치근부 치부소직을 바비드 브로치나 페이퍼 포인트로 무균적으로 채취하였다. 치수가 채취된 부위의 바비드 브로치와 페이퍼 포인트를 500 ul의 $1{\times}PBS$ 용액에 담아 잘 혼합하고, 이를 5% 양혈이 포함된 BHI 한천배지(혈액한천배지)에 도말하여 $37^{\circ}C$ 혐기성 배양기에서 2-5일 동안 배양하였다. 혈액한천배지에서 자라난 세균은 16S rRNA 유전자(rDNA) 염기서열결정법을 이용하여 종수준으로 동정하였다. 이들 균주들의 8종 항상제에 대한 감수성은 최소성장억제농도 측정법으로 조사하였다. 본 연구결과, 101개의 세균 집락이 생겼고, Streptococcus spp. (29.7%)와 Actinomyces spp. (21.8%)가 가장 많이 검출되었다. 이들 균주들 중 9균주는 실험 도중 소실되거나 액체배지에 자라지 않아서 항생제 감수성 심험에서는 제외되었다. 각 항생제들에 대한 감수성을 조사한 결과, 분리된 균주들 중 80(87.0%) 균주가 클린다마이신에 감수성을 보였으며, 세프록심 아세틸과 테트라사이클린에 69(75.0%)가, 오그멘틴에 66(71.7%) 균주가, 페니실린 G에 63(68.5%) 균주가, 에리트로마이신에 61(66.3%) 균주가, 아목시실린에 41(44.6%) 균주가 감수성을 보였다. 그러나 시플록사신에는 29(31.5%) 균주만이 감수성을 보였다. 이러한 8종 항생제에 대한 균주들의 감수성 양상은 세균 종의 종류보다는 분리된 숙주에 따라 차이가 있었다. 이러한 결과는 치근관 감염질환의 치료에 항생제가 필요할 경우 항생제 감수성검사를 병행하는 것이 효과적임을 시사한다.