• Biomolecules & Therapeutics
• /
• 제15권3호
• /
• pp.182-186
• /
• 2007

Cefixime is an orally absorbed cephalosporin with a broad spectrum of activity against Gram-negative bacteria and is highly resistant to beta-lactamase degradation. The purpose of the present study was to evaluate the bioequivalence of two cefixime capsules, Suprax capsule (Dong-A Pharmaceutical Co., reference drug) and Alpha-Cefixime capsule (Alpha Pharmaceutical Co., test drug), according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty-four normal subjects, $23.5{\pm}3.72$ years in age and $68.3{\pm}8.89$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. There was one week washout period between the doses. After one capsule containing 100 mg of cefixime was orally administered, plasma was taken at predetermined time intervals and the concentrations of cefixime in plasma were determined using HPLC with UV detector. The pharmacokinetic parameters such as $AUC_{t}$, $C_{max}$ and $T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters. The results showed that the differences in $AUC_{t}$, $C_{max}$ and $T_{max}$ between two products were -3.91%, -2.23% and -3.18%, respectively, when calculated against the reference drug. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of $log0.8{\leq}{\delta}{\leq}log1.25$ (e.g., $log0.8786{\leq}{\delta}{\leq}log1.0523$ and $log0.8889{\leq}{\delta}{\leq}log1.0512$ for $AUC_{t}$ and $C_{max}$, respectively). The 90% confidence intervals using untransformed data was within ${\pm}20%$(e.g., $-10.37%{\leq}{\delta}{\leq}6.73%$ for $T_{max}$). All parameters met the criteria of KFDA for bioequivalence, indicating that Alpha-Cefixime capsule (Alpha Pharmaceutical Co.) is bioequivalent to Suprax capsule (Dong-A Pharmaceutical Co.).

• Journal of Periodontal and Implant Science
• /
• 제35권2호
• /
• pp.401-411
• /
• 2005

The aim of this study was to determine the minimal inhibitory concentration(MIC) of cefixime, which is a 3rd generation of cefalosporin, against 6 species of putative periodontopathogens; Fusobacterium nucleatum, Actinobacillus actinomycetemcomitans, Prevotella intermedia, Prevotella nigrescens, Tannerella forsythia and Porphyromonas gingivalis. The efficacy of cefixime was examined by comparing it with that of several antibiotics(amoxicillin, $Augmentin^{(R)}$ ciprofloxacin, metronidazole, and tetracycline), which were used as the control. The MIC was measured using a microdilution method. The MIC of cefixime against the putative periodotopathogens, as a single use regimen, was relatively lower than that of the other antibiotics. The MIC of cefixime/metronidazole against P. intermedia ChDC KB14, P. nigrescens ChDC KB50, F. nucleatum ChDC PV-F37, F. nucleatum ChDC F130, and F. nucleatum ChDC F175, as a simultaneous regimen, was lower than that of the other antibiotics. The concentration of cefixime in the crevicular fluid of volunteers who received 250mg every 12 hours for 3 days was $9{\mu}g/ml$ after 9 hours. In conclusion, cefixime showed good antimicrobial activity in a single treatment or as a combined therapy with amoxicillin, $Augmentin^{(R)}$ or metronidazole against 6 periodontopathogens.

• 한국임상약학회지
• /
• 제8권1호
• /
• pp.19-22
• /
• 1998

Cefixime is an orally absorbed 3rd generation cephalosporin with a broad spectrum of activity against Gram-positive and Gram-negative bacteria and is highly resistant to $\beta-lactamase$ degradation. This study was carried out to evaluate the bioavailability of a new test drug of cefixime (100 mg/capsule) relative to the reference drug. The bioavailability was conducted on 20 healthy volunteers who received a single dose (400 mg) of the test and the reference drugs in the fasting state, in a randomized balanced 2-way crossover design. After dosing, serial blood samples were collected for a period of 12 hours. Plasma was analyzed for cefixime by a sensitive and validated HPLC assay. The major pharmacokinetic parameters $(AUC_{0-12hr},\;C_{max},\;T_{max})$ were calculated from the plasma concentration-time data of each volunteer. The $AUC_{0-12hr},\;C_{max}\;and\;T_{max}$ of the test drug were $36.91\pm11.85\;{\mu}g{\cdot}hr/ml,\;5.47\pm1.61\;{\mu}g/ml,\;and\;4.00\pm0.65\;hr,$ respectively, and those of the reference drug were $34.08\pm8.81\;{\mu}g{\cdot}hr/ml,\;5.25\pm1.40\;{\mu}g/ml,\;and\;4.20\pm0.62\;hr$, respectively. Mean differences of those parameters were 8.32, 4.29, and $4.76\%$, respectively, and the least significant differences at $\alpha$=0.05 for $AUC_{0-12hr},\;C_{max},\;T_{max}$ were 16.02, 13.78, and $11.76\%$, respectively. In conclusion, the test drug was bioequivalent with the reference drug.

• Clinical and Experimental Pediatrics
• /
• 제49권7호
• /
• pp.777-783
• /
• 2006

목 적 : 최근 소아 요로감염의 가장 흔한 원인균인 E. coli에 대한 항생제 내성 문제가 점차 대두되고 있다. 본 연구에서는 소아 원외 요로감염 환아에서 분리된 E. coli에 대한 cefixime을 포함하여 흔히 사용되고 있는 경구용 항생제의 시험관 내 감수성 연구를 시행하여 적합한 치료 항생제 선택의 기초 자료를 얻고자 하였다. 방 법 : 2004년 10월부터 2005년 9월까지 연구 참여 병원 소아과 외래에서 요로감염으로 진단된 206명 환아의 요 배양검사에서 동정된 211개 균주 중 188개 E. coli를 대상으로 경구용 항생제(ampicillin, amoxillin, ampicillin-sulbactam, cefaclor, TMP-SMX, cefixime)에 대한 시험관 내 감수성 검사를 실시하였다. 결 과 : 분리된 E. coli 균주에 대한 항생제별 감수성 결과에서 내성률은 각각 ampicillin 81.4%, amoxicillin 85.6%, ampicillin-Sulbactam 77.2%, cefaclor 93.6%, TMP-SMX 50.5%, cefixime 13.3%이었다. ESBL 생성 E. coli는 7.0%이었다. 결 론 : Aminopenicillins계, cefaclor, sulfa약제들은 E. coli에 대한 내성률이 매우 높아 소아 요로감염의 일차 선택 항생제로 유용하지 못한 것으로 추정할 수 있었다. 그러나 cefixime과 같은 3세대 cephalosporin은 일차 치료 실패할 경우 이차 선택항생제로 유용할 수 있으며, 일차 선택 항생제로도 사용될 수 있을 것으로 추정되었다. E. coli의 항생제 내성 양상에 대한 광범위한 연구와 지속적 감시를 통하여 소아 원외 요로감염 치료에서 1차적으로 선택될 수 있는 경구용 항생제에 대한 지침 자료가 요구된다.

• Journal of Pharmaceutical Investigation
• /
• 제29권2호
• /
• pp.145-149
• /
• 1999

Bioequivalence of two cefixime capsules, test drug ($Cepirin^R$ capsule: Cheiljedang Corp.) and reference drug ($Suprax^R$ capsule: Dong A Pharm. Com.), was evaluated according to the guidelines of Korea Food and Drug Administration (KFDA). Sixteen healthy volunteers were divided randomly into two groups and administered the drug orally at the dose of 400 mg as cefixime in a $2{\times}2$ crossover study. There was a 1-week washout period between the administrations. Blood samples were taken at predetermined time intervals for 12 hour and the plasma concentration of cefixime was determined with a HPLC method. $AUC_{0-12hr}$ (area under the plasma concentration-time curve form time zero to 12 hour), $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{max}$) were estimated from the plasma drug concentrationtime data. Analysis of variance (ANOVA) revealed no difference in $AUC_{0-12hr}$, $C_{max}$ and $T_{max}$ between the formulations. The apparent differences of these parameters between the formulations were less than 20% (i.e., 8.62, 11.10 and 0.00% for $AUC_{0-12hr}$, $C_{max}$ and $T_{max}$,respectively). The powers $(1-{\beta})$ for $AUC_{0-12hr}$ $C_{max}$ and $T_{max}$ were over 0.9. Minimal detectable difference $({\Delta})$ at ${\alpha}=0.05$, $1-{\beta}=0.8$ were less than 20% (i.e., 12.84, 11.05 and 17.99% for $AUC_{0-12hr}$, $C_{max}$ and $T_{max}$, respectively). The 90% confidence intervals $({\delta})$ for these parameters were also within ${\pm}20%$ (i.e., $-0.53{\le}{\delta}{\le}17.76$, $3.23{\le}{\delta}{\le}18.97$ and $-12.81{\le}{\delta}{\le}12.81$ for $AUC_{0-12hr}$, $C_{max}$ and $T_{max}$, respectively). These results satisfied the criteria of KFDA guideline for bioequivalence, indicating the two formulations of cefixime were bioequivlent.

• 약학회지
• /
• 제38권2호
• /
• pp.114-122
• /
• 1994

A study on the absorption mechanism of cefixime(CF), an oral ${\alpha}-amino$ group deficient cephalosporin antibiotic, has been undertaken through the rat jejunum and nasal cavity using an in situ simultaneous perfusion technique developed in our laboratory. CF was well absorbed in the jejunum and nasal cavity of rats at pH 5.0, but not at pH 7.0. CF absorption was studied over four orders of magnitude in concentration to determine saturability. Disappearance of CF in the perfusate followed first-order kinetics at all tested concentrations. The apparent first-order absorption rate constant was found to be dependent on the concentration over the range of $0.1\;mM{\sim}3\;mM$ in the jejunum and nasal cavity of rats. Inhibitors were added to determine the competitive inhibition of CF absorption. The presence of L-tyrosine, L-phenylalanine, alanine-alanine, glycine-glycine and cefadroxil produced the significant inhibition of CF absorption in the nasal cavity and jejunum. However, there was no evidence of the inhibition in the presence of cefazolin. In addition, The CF absorption in the nasal cavity and jejunum was inhibited significantly by ouabain and 2,4-dinitrophenol(DNP). This study suggested that CF is absorbed across the rat nasal cavity and jejunum by carrier-mediated transport mechanism and energy consuming system.

• 대한치주과학회:학술대회논문집
• /
• 대한치주과학회 2005년도 제45회 종합학술대회 연제초록
• /
• pp.185-185
• /
• 2005

• 대한수의학회지
• /
• 제39권4호
• /
• pp.765-771
• /
• 1999

Unlike most Escherichia coli strains, E coli O157 : H7 didn't ferment sorbitol within 24h of incubation and showed a negative reaction for $\beta$-glucuronidase. We developed a new medium for the rapid isolation of E coli O157 : H7 using sorbitol MacConkey agar with cefixime, potassium tellurite and 4-methylumbelliferyl-${\beta}$-D-glucuronide (MUG) as a primary plating medium. The addition of $20{\mu}g/ml$ of vancomycin in enrichment broth for E coli O157 : H7 inhibited lots of Gram positive bacteria. Three strains (10.3%) of 29 non-O157 E coli strains and 3 strains (8.3%) of 36 Salmonella spp were inhibited at the $0.05{\mu}g/ml$ of cefixime and 23 strains (79.3%) of 29 non-O157 E coli strains and 12 strains (33.3%) of 36 Salmonella spp were inhibited at the $2.0{\mu}g/ml$ of potassium tellurite. But none of the E coli O157 : H7 was affected at these concentration. The addition of MUG at $100{\mu}g/ml$ level to sorbitol MacConkey agar with cefixime and potassium tellurite (CTM-SMAC) aided in the rapid isolation of E coli O157 : H7 from samples by checking sorbitol-negative and $\beta$-glucuronidase negative phenotypes simultaneously. In conclusion, inoculation of a positive in the O157 screening test from enrichment broth on CTM-SMAC appeared to be a rapid, cost-effective and sensitive method for the isolation of E coli O157 : H7.

• 한국임상수의학회지
• /
• 제22권2호
• /
• pp.114-118
• /
• 2005

Bacterial disease caused by Aeromonas are among the most common and troublesome diseases of fish raised in aquaculture systems. In this study, some strains identified as belonging to the Aeromonas were isolated from neon tetra (Hyphessobrycon herbertaxelrodi) skin and fin, as well as from water samples. VITEK system and API ZYM examination of the isolated strains were undertaken, and it seemed to correlate with the Aeromonas, proved to be Aeromonas veronii. The antibiotic susceptibility test of isolated strains to different groups of antibiotics was evaluated using the disc diffusion method. Cefixime was the most sensitive antibiotic.

• Pediatric Gastroenterology, Hepatology & Nutrition
• /
• 제5권2호
• /
• pp.150-157
• /
• 2002

목 적: 비장티푸스성 살모넬라균은 세균성 위장관염 및 장열 등을 일으키는 중요한 원인균으로 전 세계적으로 발생률이 증가할 뿐 아니라 항생제에 대한 다제내성률도 증가하는 추세이다. 그러나 이에 대한 소아에서의 연구 보고는 많지 않아 저자들은 비장티푸스성 살모넬라 위장관염의 임상양상과 항생제 내성률 등에 대하여 알아보고자 하였다. 방 법: 2000년 1월부터 2002년 6월까지 서울대학교 어린이병원에 내원하여 비장티푸스성 살모넬라 위장관염으로 진단받은 환아를 대상으로 임상양상, 항생제 내성률 및 변역 상태에 따른 내성률과 다제내성률 등을 조사하였다. 결 과: 대변 검사상 비장티푸스성 살모넬라균이 분리된 99례 중, 남아가 66례 여아가 33례였다. 2세 이상 3세 미만이 23례로 가장 많았으며 5세 미만에서 발생한 경우가 전체의 71%에 해당하였고 평균 연령은 4.0세였다. 25례는 항암 화학요법이나 스테로이드 및 면역 억제제 치료 등으로 면역 기능이 저하된 환자였다. 혈청군 중 D군이 65례로 가장 많았고 B군이 16례, C군과 E군이 각각 8례였다. 3례에서 균혈증이 동반되었다. 항생제에 대한 내성률을 보면 ampicillin에 31%, chloramphenicol에 12%, TMP-SMX에 20%, cefotaxime에 11%, cefixime에 8%의 내성률을 보였으며 ciprofloxacin은 모든균주에서 감수성을 보였다. Cefotaxime과 cefixime에 대한 내성률은 변역가능이 저하된 환아군에서 각각 24%, 14.3%로 정상군에서의 6.8%, 5.6%보다 유의하게 높았다 (p<0.05). 연령별(5세 미만 vs 5세 이상), 혈청군별(D군 vs 비D군) 내성률의 차이는 없었다. 한편 3가지 이상의 항생제에 내성을 보이는 다제내성균은 11례에서 동정되었고, 변역가능이 저하된 환아군에서의 동정률이 24%로 정상군에서의 동정률인 6.8%보다 유의하게 높았다(p<0.05). 결 론: 비장티푸스성 살모넬라 위장관염인 소아환자에서 항생제 치료를 해야 하는 경우에, 소아에서 안정성이 확립되지 않은 quinolone을 제외한다면 3세대 cephalosporin을 1차 선택제로 고려할 수 있다. 그러나 본 연구에서처럼 변역 가능이 저하된 환자에서는 cefotaxime과 cefixime에 대한 내성률과 다제내성률이 유의하게 높으므로 적절한 항생제 선택에 주의해야 할 것이며 향후 이에 대한 연구가 더 필요하리라 생각된다.