• Title/Summary/Keyword: cefaclor

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Bioequivalence of Cefaclor 375 mg SR Tablet (세파클러 375 mg서방정의 생물학적 동등성)

  • Lee, Shin Hwa;Yun, Min Hyuk;Choi, Kyung Eob;Kwon, Kwang Il
    • Korean Journal of Clinical Pharmacy
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    • v.13 no.1
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    • pp.13-17
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    • 2003
  • This study was carried out to compare the bioavailability of $Ceclex^{(R)}$ SR TAB (test drug, cefaclor 375 mg/Tablet) with that of Ceclor $MR^{(R)}$ SR IAB (reference drug) and to estimate the pharmacokinetic parameters of cefaclor in healthy Korean volunteers. The bioavailability was examined on 24 healthy volunteers who received a single dose (375 mg) of each drug in the fasting state in a randomized balanced 2-way crossover design. After dosing, blood samples were collected for a period of 7 hours. Plasma concentrations of cefaclor were determined using HPLC with UV detection. The pharmacokinetic parameters $(AUC_{0-7h},\;C_{max},\;T_{max},\;AUC_{inf},\;K_e,\;t_{1/2},\;V_d/F,\;and\;CL/F)$ were calculated with non-compartmental pharmacokinetic analysis. The ANOVA test was utilized for the statistical analysis of the $T_{max}$, log-transformed $AUC_{0-7h$}$, log-transformed $C_{max},\;t_{1/2},\;V_d/F$, and $CL/F$. The ratios of geometric means of $AUC_{0-7h}\;and\;C_{max}$ between test drug End reference drug were $95.67\%\;(8.55\;vs\;8.18{\mu}g{\cdot}hr/ml)\;and\;103.86\%\;(2.85\;vs\;2.96{\mu}g/ml)$, respectively. The $T_{max}$ of test drug and reference drug was $2.56\pm0.15\;and\;2.23\pm0.13\;hrs,\;respectively.\;The\;90\%$ confidence intervals of mean difference of logarithmic transformed $AUC_{0-7h}\;and\;C_{max}$ were log0.90-log1.04 and log0.91-log1.13, respectively. It shows that the bioavailability of test drug is equivalent with that of reference drug.

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Bioequivalence of Cefaclor (250 mg) Capsule (세파클러 250 mg 캅셀의 생물학적 동등성)

  • Yun, MH;Kim, HS;Choi, YP;Kwon, KI
    • Korean Journal of Clinical Pharmacy
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    • v.12 no.2
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    • pp.71-75
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    • 2002
  • This study was carried out to compare the bioavailability of $Ceclex^{(R)}$ (test drug, cefaclor 250 mg/capsule) with that of $Ceclor^{(R)}$ (reference drug) and to estimate the pharmacokinetic parameters of cefaclor in healthy Korean adult. The bioavailability was examined on 20 healthy volunteers who received a single dose (250 mg) of each drug in the fasting state in a randomized balanced 2-way crossover design. After dosing, blood samples were collected for a period of 6hours. Plasma concentrations of cefaclor were determined using HPLC with UV detection. The pharmacokinetic parameters $(AUC_{0-6hr},\;C_{max},\;T_{max},\;AUC_{int},\;K_e,\;t_{1/2},\;Vd)$ F, and CL/F) were calculated with non-compartmental pharmacokinetic analysis. The ANOVA test was utilized for the statistical analysis of the $T_{max},\;log-transformed\;AUC_{0-6hr}\;log-transformed\;C_{max},\;t_{l/2},\;V_d/F$, and CL/F. The ratios of geometric means of AUC0-6hr and $C_{max}$ between test drug and reference drug were $103.2\%\;(6.74\;{\mu}g{\cdot}hr/ml\;vs\;6.53{\pm}g{\cdot}hr/ml)\;and\;100.4\%\;(4.85\;{\mu}g\ml\;vs\;4.82\;{\mu}g/ml)$, respectively. The $T_{max}$ of test drug and reference drug were $0.9\pm0.38\;hr\;and\;0.83\pm0.34$ hrs, respectively. The $90\%$ confidence intervals of mean difference of logarithmic transformed $AUC_{0-6h},\;and\;C_{max}$ were log $0.98{\sim}log$ 1.08 and log $0.88{\sim}log1.15$, respectively. It shows that the bioavailability of test drug is equivalent with that of reference drug. The estimated half-life of this study was longer $(1.21\pm0.27\;hrs\;vs\;0.5-1\;hr)$, the Vd/F was larger $(68.89\pm25.72L$ vs 24.9L), and the CL/F was higher $(38.62\pm7.09\;L/hr$ vs 24.9 L/hr) than the previously reported values.

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Penicillin Resistant Distribution and in-vitro Susceptibility of Oral Antibiotics against Streptococcus pneumoniae, isolated from Pediatric Patients with Community-Acquired Respiratory Infections in Korea (급성 호흡기감염 환아에서 분리된 폐구균에 대한 페니실린 내성분포와 경구 항생제에 대한 감수성 연구)

  • Kang, Jin Han;Kim, Sun Mi;Kim, Jong Hyun;Hur, Jae Kyun;Lee, Kyung Yil;Shin, Young Ku;Park, Su Eun;Ma, Sang Hyuk;Hong, Young Jin
    • Clinical and Experimental Pediatrics
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    • v.48 no.1
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    • pp.40-47
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    • 2005
  • Purpose : S. pneumoniae is one of major pathogens of community-acquired respiratory infections. The rate of antibiotic resistance to this organism has increased, and resistance to multiple antimicrobial agents in a single strain of S. pneumoniae may compromise the efficacy of empiric antimicrobial treatment commonly used for respiratory infections. We did this study to find out the penicillin resistant distributions and oral antibiotics susceptibility patterns against S. pneumoniae, isolated from pediatric patients with community-acquired respiratory infections in Korea. Methods : One hundred fifty six pneumococcal isolates obtained from pediatric patients with community-acquired respiratory infections such as acute otitis media(AOM), sinusitis and pneumonia between May 2000 to June 2003. And MICs of penicillin and oral antibiotics(amoxicillin, amoxicillin-clavulanate, cefaclor) were performed by broth microdilution methods according to the NCCLS(2003a). Results : Seventy eight percent of the isolates were resistant to penicillin. The isolates, collected from AOM patients showed the highest penicillin resistance(92.7%). The resistant rates of amoxicillin (16.7%) and amoxicillin-clavulanate(9.6%), based on susceptibility breakpoints established by the NCCLS, were markedly lower than these of penicillin. But, the resistant rate of cefaclor was very high, above 95%. Conclusion : We concluded that pneumococci isolated from study cases may be one of the world's highest penicillin resistant rates. But, amoxicillin and amoxicillin-clavulanate can be used as a first-line antibiotics. Finally, we hope that a continuous surveillance study to monitor resistant patterns of pneumococcal respiratory infections will be needed for the standard guidelines of empiric antibiotic treatment.

Susceptibility tests of oral antibiotics including cefixime against Escherichia coli, isolated from pediatric patients with community acquired urinary tract infections (소아 원외 요로감염 환아에서 분리된 E. coli에 대한 cefixime을 포함한 경구 항생제의 감수성 연구)

  • Lee, Soo Young;Lee, Jung Hyun;Kim, Jong Hyun;Hur, Jae Kyun;Kim, Sun Mi;Ma, Sang Hyuk;Kang, Jin Han
    • Clinical and Experimental Pediatrics
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    • v.49 no.7
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    • pp.777-783
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    • 2006
  • Purpose : Urinary tract infection(UTI) is one of the most frequent infections in children. E. coli is the most frequent etiological micropathogen in pediatric community UTI, and E. coli has developed resistance to many antibiotics, highlighting the need for regular surveys of this organism resistant patterns in the community. The aim of this study was to determine the oral antibiotic susceptibility patterns of E. coli, isolated from pediatric patients with uncomplicated community acquired UTI. Methods : E. coli isolates, obtained from pediatric patients with uncomplicated community acquired UTI between October in 2004 to September in 2005. And minimal inhibitory concentrations(MICs) of oral aminopenicillins and beta-lactamase inhibnitors(ampicillin, amoxacillin, ampicillin-sulbactam), oral cephalosporins(cefaclor, cefixime) and sulfa drug(trimethoprime-sulfamethoxazole) were performed according to the National Committee for Clinical Laboratory Standards(NCCLS) guide line. Results : Total 211 organisms were isolated from pediatric out-patients with community UTI. E. coli was the most common organism(89 percent), followed by E. fecalis, Proteus species, S. aureus, M. morganii, and P. aeruginosa. The resistant rates of aminopenicillins and beta-lactamase inhibitors, cefaclor and sulfa drug to E. coli were very high. But, the resistant rate of cefixime was markedly low, and ESBL strains were isolated with small rates. Conclusion : Our study results suggest that aminopenicillins, cefaclor and sulfa drug may not be useful as first line empirical antibiotics to treat pediatric patients with community UTI in Korea. But, 3rd generation cephalosporin such as cefixime can be used as effective second line antibiotics after primary treatment failure, also may be useful as an empirical first line antibiotic. Finally, we conclude that a continuous surveillance study to monitor susceptibility patterns of E. coli in community UTI will be needed for the standard guide lines of empirical oral antibiotic treatment.

Synthesis and Antibacterial Activities of New Oral Cephalosporins (새로운 경구용 세파로스포린의 합성 및 항균작용)

  • 나성범;정명희;김완주;지웅길
    • YAKHAK HOEJI
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    • v.37 no.3
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    • pp.295-305
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    • 1993
  • In order to develop oral cephalosporin having a new substituent at 3 position, the synthesis of cephalosporins modified at C-3 and the effect of the substituents on the oral absorption is studied. 7-[(Z)-2-(2-Aminothiazole- 4-yl)-2-methoxyiminoacetamidol-3-[4-(2-pyridyl )piperazinyl] thiocarbonylthiomethyl-3-cephem-4-carboxylic acid (CEN1) and 7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyrimid yl)piperazinylthiocarbonylthiomethyl-3-cephem-4-carboxylic acid (CEN2) were synthesized from 4-(2-piridyl)piperazinyl dithiocarbamate potassium salt or 4-(2-pirimidyl)piperazinyl dithiocarbamate potassium salt and cefotaxime. Also pivaloyloxymethyl esters of CEN1 and CEN2, pivaloyloxymethyl 7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamido]-3-[4-(2-pyridyl )piperazinyllthiocarbonylthiomethyl-3-cephem-4-carboxylate (CENIP) and pivaloyloxymethyl 7-[(Z)-2-(2-aminothiazole-4-yl)-2-methoxyiminoacetamidol-3- [4-(2-pyrimid yl)piperazinyllthiocarbonylthiomethyl-3-cephem-4-carboxylate (CEN2P) were synthesized. The in vitro activities of two new oral cephalosporins, CEN1 and CEN2, were compared with the in vitro activities of cefaclor and cefotaxime against a variety of bacterial species. CEN2 has a broad antibacterial spectrum covering Gram-positive and Gram-negative bacteria, similar to that exhibited by CEN1 and cefotaxime. CEN1 and CEN2 were more active in vitro than cefaclor against Streptococcus pyogenes, Klebsiella aerogenes and Enterobacter cloacae.

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Outcome of Regenerative Endodontic Treatment for an Avulsed Immature Permanent Tooth: A Case Report (완전 탈구된 미성숙 영구치의 치수재생치료 증례 보고)

  • Park, Nakyoung;Song, Jihyun
    • Journal of the korean academy of Pediatric Dentistry
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    • v.45 no.2
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    • pp.250-256
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    • 2018
  • Dental avulsion, defined as the complete displacement of a tooth from the alveolar bone with consequent loss of the blood and nerve supply, was reported as one of the most severe dental injuries. Avulsion can cause tissue ischemia, which leads to pulp necrosis. Apexification is a conventional treatment method that induces an apical calcified barrier in immature roots with pulp necrosis. However, root development characterized by an increase in the root thickness and length cannot be achieved by apexification. The purpose of this case report was to describe the radiographic and clinical outcomes of regenerative endodontic treatment for the avulsed and necrosed permanent tooth with an immature root after replantation in a 5-year-old girl; the treatment was performed using a mixture of ciprofloxacin, metronidazole and cefaclor, CollaTape and Biodentine.

Simultaneous analysis of β-lactam antibiotics in surface water (하천수중 잔류 베타-락탐계 항생제의 동시분석법)

  • Huh, Min-Jeong;Myung, Seung-Woon
    • Analytical Science and Technology
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    • v.23 no.2
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    • pp.119-127
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    • 2010
  • An effective method for the simultaneous analysis of ${\beta}$-lactams from surface water was established. After solid-phase extraction with HLB (Hydrophilic Lipohilic Balance) cartridge at pH 2, seven ${\beta}$-lactams (amoxicillin, ampicillin, penicillin G, cefaclor, cefadroxil, cefatrizine and cephradine) were determined using LC/ESI-MS/MS. In this newly established method, correlation coefficients ($r^2$) of calibration curves for seven ${\beta}$-lactams in blank surface water appeared to be 0.9911~0.9995 in the concentration range of 0.01~1.0 ng/mL. The limits of detection (LODs) and the limits of quantificaiton (LOQs) in spiked surface water were shown to be 0.0003~0.0234 ng/mL and 0.0046~0.0778 ng/mL, respectively. The developed method is believed to serve as a rapid and reliable method for the qualitative and quantitative analysis of residual ${\beta}$-lactam antibiotics from aquatic environment.

Causative Pathogens and Therapeutic Assessment of Cefprozil in Acute Otitis Media (급성 중이염의 원인 병원균과 Cefprozil 치료의 임상적 평가)

  • Kang, Jin-Han;Kim, Jong Hyun;Park, Yong-Soo;Choi, Young-Chul;Noh, Heil;Yang, Hoon Shik;Kim, Kyu Sung;Moon, Yeon Sook;Hong, Young Jin
    • Clinical and Experimental Pediatrics
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    • v.46 no.5
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    • pp.459-466
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    • 2003
  • Purpose : AOM is the most common bacterial URI in children. The bacteriology and antibiotic Tx of AOM in children has been studied in many countries. But, there is few study of causative pathogens and antibiotic Tx of AOM in our country. In this aspect, we performed prospective clinical study to confirm the causative pathogens and assess the clinical responses of cefprozil in AOM patients. Methods : Thirty three AOM patients enrolled in this study. Tympanocentesis for isolation of causative pathogens were performed before Tx of cefprozil. The study patients received cefprozil with dose of 15 mg/kg/bid.po/day for 10-12 days, and initially assessed the clinical response at 4-5 days after receiving cefprozil and finally at the end visit. In vitro susceptibility tests of cefprozil to isolated pathogens were done by disc diffusion method, and in vitro susceptibility tests of cefaclor and cefixime to isolated pathogens were simultaneously performed. Results : Bacterial pathogens[S. pneumoniae(10), H. influenzae(5), S. aureus(2), M. catarrhalis(1) and Group A stretococcus(1)] were isolated from 19 patients. Clinically, all patients had history of abrupt high fever except one. Tympanic perforation was dominant in pathogens isolated cases, and otalgia was significantly developed in non-pathogens isolated cases. The ages of pathogens isolated cases were usually below 2 years. Eighty four point nine percent of the patients including two cases with isolation of intermediate resistant S. pneumoniae were clinically improved. Antimicrobial in vitro activity to S. pneumoniae of cefprozil were superior than that of cefacor and cefixime. Conclusion : We confirm that bacteria has the causative role in about 60% cases, and S. pneumoniae is the most common pathogen. Clinically, there were some differences in symptoms, signs and ages between pathogens isolated and non-pathogens isolated cases. The clinical responses of cefprozil in our patients revealed similar outcomes to other countries. And we reconfirm that cefprozil may be clinically effective in cases of AOM due to intermediate resistant S. pneumoniae.