• 한국임상수의학회지
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• 제22권3호
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• pp.175-180
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• 2005

본 연구는 개에서 키토산 비드를 이용한 cefadroxil 방출에 영향을 주는 인자, 약물을 함유한 최적의 키토산 비드의 제조, 그리고 키토산 비드로부터 약물의 방출을 평가하는 것이다. 키토산 비드는 tripolyphosphate (TPP)와 이온결합으로 생성되며 비드의 크기는 1 mm 미만이었다. 비드로부터 cefadroxil 방출은 여러 인자에 영항을 받는다. TPP의 pH가 감소할수록 cefadroxil의 비드내 함유량은 증가하지만, 비드로부터 방출량은 감소한다. Cefadroxil의 방출속도은 TPP 농도가 증가할수록 감소한다. 결합시간이 길어지면, 방출량이 감소한다. Cefadroxil을 함유한 키토산 비드를 50 mg/kg 용량으로 건강한 개 4두의 피하에 이식한 결과, cefadroxil의 혈청내 농도는 1 ${\mu}g/ml$ 이상으로 7일간 유지되었다. 따라서 cefadroxil을 함유한 키토산 비드는 개의 농피증 치료에 유용한 것으로 사료되며 약물방출을 통제할 수 있는 약물수송체가 이용될 수 있다고 사료된다.

• Biomolecules & Therapeutics
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• 제10권4호
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• pp.303-308
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• 2002

A bioequivalence study of Shin II Cefadroxil capsule (Shin II Pharm. Co. Ltd.) to Duricef capsule(Bo Ryung Pharm. Co. Ltd.), each containing 500 mg of cefadroxil, was conducted. Twenty three healthy Korean male subjects administered each formulation at the dose of 1 capsule (500 mg as cefadroxil) in 2 $\times$ 2 cross-over study. There was a I-week washout period between the doses. Plasma concentrations of cefadroxil were monitored for a period of 8 hr after each administration by an LC/UV method. Area under the plasma concentration-time curve up to 8 hr ($AUC_t$) was calculated by a linear trapezoidal method. $C_{max}$ was compiled from the plasma drug concentration-time data. ANOVA test was conducted for logarithmically transformed $AUC_t$ and $C_{max}$ The results showed that there are no significant differences in $AUC_t$ and $C_{max}$ between the two formulations: The differences between d1e formulations in these log transformed parameters were all for less than 20% (i.e., －0.57%, 3.84% for $AUC_t$ and $C_{max}$, respectively). The 90% confidence intervals for the log transformed data were within the acceptance range of log 0.8 to log 1.25 (i.e., log 0.94~log 1.04 and log 0.95~log 1.10 for $AUC_t$ and $C_{max}$, respectively). Based on d1e bioequivalence criteria of KFDA guidelines, the two formulations of cefadroxil were concluded to be bioequivalent.

• Journal of Pharmaceutical Investigation
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• 제34권5호
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• pp.363-368
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• 2004

In order to investigate the effect of bovine serum albumin (BSA), as a pore former, on the controlled release of an antibiotic from a biodegradable polymeric device, polycaprolactone (PCL)-cefadroxil matrices were prepared by the solvent casting method. The amount of cefadroxil released from various formulations at $37^{\circ}C$ was measured by HPLC. The duration of antimicrobial activity of matrices against S. aureus was evaluated by measuring the diameters of the inhibition zone. The morphology of the matrices was investigated by scanning electron microscopy (SEM). The release rate and extent of cefadroxil from PCL matrix increased as the loading dose and particle size of BSA/cefadroxil mixture powder increased. Cefadroxil released from the matrix exhibited antibacterial activity for up to 4 days. SEM of the cross-section of matrix showed the typical channel formation after 3 days of release study. Thus, a biodegradable polymeric matrix loaded with antibiotic/BSA mixture can effectively prevent bacterial infection on its surface, thereby bringing about an enhancement of biocompatibility of biomaterials.

• Journal of Pharmaceutical Investigation
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• 제32권2호
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• pp.135-140
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• 2002

Cefadroxil is a semi-synthetic cephalosporin active against many Gram-positive and Gram-negative bacteria. The drug has been used for the treatment of the urinary and respiratory tract infections when caused by susceptible strains of the designated microorganism. The purpose of the present study was to evaluate the bioequivalence of two cefadroxil capsules, Duricef (Bo Ryung Pharmaceutical Co. Ltd.) and Hanacef (Korean Pharmaceutical Co. Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). The cefadroxil release from the two cefadroxil capsules in vitro was tested using KP VII Apparatus II method with various different kinds of dissolution media (pH 1.2, 4.0, 6.8 buffer solution and water). Twenty four normal male volunteers, $21.58{\pm}2.43$ years in age and $70.74{\pm}10.29$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After one capsule containing 500 mg as cefadroxil was orally administered, blood was taken at predetermined time intervals and the concentrations of cefadroxil in serum were determined using HPLC with UV detector. The dissolution profiles of two cefadroxil capsules were very similar at all dissolution media. 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 using logarithmically transformed $AUC_t\;and\;C_{max}$ and untransformed $T_{max}$. The results showed that the differences in $AUC_t,\;C_{max}\;and\;T_{max}$ between two capsules based on the Duricef were 0.05%, -5.29% and 4.53%. There were no sequence effects between two capsules in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log(0.8) to log(1.25) $(e.g.,\;log(0.95){\sim}log(1.05)\;and\;log(0.87){\sim}log(1.02)$ for $AUC_t\;and\;C_{max}$, respectively). The 90% confidence interval using untransformed data was within ${pm}20%$ $(e.g.,\;-6.75{\sim}15.74\;for\;T_{max})$. All parameters met the criteria of KFDA guideline for bioequivalence, indicating that Hanacef capsule is bioequivalent to Duricef capsule.

• Journal of Pharmaceutical Investigation
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• 제30권2호
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• pp.93-98
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• 2000

In order to evaluate the effect of fabrication methods on the controlled release of an antibiotic from a polymeric device, two types of polyurethane-cefadroxil matrix were prepared by the solvent casting method or the freeze drying method, using bovine serum albumin as a pore former. The amount of cefadroxil released from various formulations at $37^{\circ}C$ was measured by HPLC. The duration of antimicrobial activity of matrices against S. aureus was evaluated by measuring the diameters of the inhibition zone. The morphology of the matrices was investigated by scanning electron microscopy (SEM). Changing the fabrication method could alter the release rate of cefadroxil from the matrix. The matrix fabricated by the freeze drying method had more porous inner structure and showed higher release rate than that prepared by the solvent casting method. However, the duration of antimicrobial activity was shorter when the matrix was fabricated by the freeze drying method.

• Bulletin of the Korean Chemical Society
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• 제29권6호
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• pp.1185-1189
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• 2008

Two HPLC methods such as cefadroxil and cefalexin methods were compared in their performance for the quantitative analysis of the content and purity of $\beta$ -lactamic antibiotic, cefradine, for six bulk drug samples. Between the two methods, the cefadroxil method prescribed by the European Pharmacopoeia (EP) for the determination of impurities in cefradoxil was superior to the cefalexin method prescribed by the EP and by the United States Pharmacopeia (USP) for the determination of cefalexin impurity in cefradine in terms of the greater stability of the chromatogram baselines and the higher precision, i.e., the lower % relative standard deviation (RSD). Based on the comparison of the two HPLC methods, the cefadroxil method was recommended to replace the TLC method, which has been prescribed by the EP as the official method for determination of extraneous impurities in cefradine.

• 한국미생물·생명공학회지
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• 제17권3호
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• pp.193-197
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• 1989

Spanner chain의 탄소수가 2,4 또는 6개의 alkylene diisothiocyanate를 합성 후 cefadroxil-2DMF와 반응시켜 spanner chain의 탄소수 2, 4 또는 6개로 연결되어 있고 양쪽에 thioureido group과 $\beta$-lactam ring을 가진 bivalent ligand 구조의 alkylene bisdithioureido $\beta$-lactam 유도체를 합성하고 그 화합물들의 항균작용에 대하여 연구하였다. 그 유도체의 I식 화합물은 $C_{36}$H$_{38}$N$_{8}$O$_{10}$S$_4$, II식 화합물은 $C_{38}$H$_{42}$N$_{8}$O$_{10}$S$_4$, III식 화합물은 $C_{40}$H$_{46}$N$_{8}$O$_{10}$S$_4$의 분자식이다. $\beta$-lactam 감수성 균주에 대한 항균력은 spnner chain의 탄소수가 많을수록 감소하였다.

• The Korean Journal of Physiology and Pharmacology
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• 제7권4호
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• pp.247-250
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• 2003

A simple and sensitive assay method was developed for cefepime in human plasma using high performance liquid chromatography (HPLC). Cefepime and cefadroxil (the internal standard) were extracted from heparinized human plasma by simple deproteination with perchloric acid. The extract was injected into an Atlantis dC18 column ($250{\times}4.6$ mm; particle size $5{\mu}m$, Waters) and the column was eluted with methanol and 0.01 M dihydrogen phosphate at pH 3.0 (15：85 v：v) as a mobile phase at a flow rate of 0.7 mL/min. Linearity was confirmed for the range 0.25 to $200{\mu}L/mL$ and the limit of quantitation was $0.25{\mu}L/mL$. The retention times were 10.2 min and 13.4 min for cefepime and cefadroxil, respectively. This method was successfully applied to a pharmacokinetic study of cefepime in plasma from bone marrow transplant patients.

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 NEW STRATEGY FOR DRUG DEVELOPMENT IN POST-GENOMIC ERA(대한약학회)
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• pp.263.1-263.1
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• 2000

• 대한약학회:학술대회논문집
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• 대한약학회 2000년도 춘계총회 및 학술대회
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• pp.207.1-207.1
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• 2000