• Journal of Pharmaceutical Investigation
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• v.32 no.4
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• pp.327-330
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• 2002

Alginate based polymeric matrices were designed for controlled release and stabilization of cefaclor in gastrointestinal fluid. Cefaclor is known to be acid stable and subjected to be degraded at neutral and alkaline pHs. In order to achieve an effective release profile of cefaclor in gastrointestinal tract, a particular strategy in dosage form design should be required from the view point of maintaining its activity. The amphiphilic nature of cefaclor allowed its controlled release using ionic polymers based on ionic interaction between the drug and polymers. The thrust of this study was to develop a technique that delivers cefaclor keeping effective release rate in the intestinal tract. Considering the fast degradation of cefaclor in the intestinal fluid, the matrices were designed to release surplus amount of cefaclor. The alginate based matrices demonstrated increase in release rate in the simulated intestinal fluid, which was favorable to compensate the degraded portion of cefaclor. In addition, stabilization of cefaclor in the intestinal fluid was obtained by employing citric acid that provides an local acidic environment. The matrices might be valuably used for the development of an oral cefaclor dosage form.

• Environmental Engineering Research
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• v.14 no.2
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• pp.81-87
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• 2009

The decomposition of antibiotics (cefaclor) by gamma irradiation in aqueous solutions was experimentally evaluated. To obtain a mutual interaction between two factors (antibiotics concentrations and radiation doses) and to optimize these factors during the process, experimental design and statistical analysis were employed. The decomposition capability of the gamma radiation was also mathematically described as a function of cefaclor concentration and gamma-ray dose using the statistical analysis. The results showed that the cefaclor concentration ($X_1$) in the response $Y_1$ (Reduction of cefaclor concentration) and gamma-ray dose ($X_2$) in the response $Y_2$ (Removal efficiency (%) of cefaclor concentration) exhibited a significantly positive effect, whereas gamma-ray dose ($X_2$) in the response $Y_1$ showed a significantly negative effect. The estimated ridge of maximum responses and optimal conditions for $Y_1$:($X_1$,$X_2$)=(25 mg/L, 350 Gy) and $Y_2$:($X_1$,$X_2$)=(21 mg/L, 565 Gy) using canonical analysis were 4.37 mg/L of reduction of cefaclor concentration and 98.35% of removal efficiency of cefaclor concentration, respectively. The measurement values agreed well with the predicted ones, thereby confirming the suitability of the model for $Y_1$ and $Y_2$ and the success of the experimental design in optimizing the conditions of the gamma irradiation process.

• YAKHAK HOEJI
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• v.32 no.3
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• pp.182-186
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• 1988

Binding of four cephalosporins(cefaclor, cefpiramide, ceftazidime, ceforanide) to bovine serum albumin was studied. Difference spectrophotometry was employed to evaluate the nature and the degree of association of cephalosporin-albumin complex. 2-(4'-hydroxybenzen azo) benzoic acid was used as the uv spectrophotometric probe for measuring the binding of cephalosporins to bovine serum albumin. Competitive bindings between cephalosporins and probe were observed. For the binding of cephalosporins to bovine serum albumin, three binding sites were identified. The binding constants of cefaclor, ceforanide, ceftazidime and cefpiramide were $12.57\;{\times}\;10^{-2}M^{-1}$, $6.49\;{\times}\;10^{-2}M^{-1}$, $4.70\;{\times}\;10^{-2}M^{-1}$ and $6.20\;{\times}\;10^{-2}M^{-1}$ respectively.

• Journal of Korean Society of Environmental Engineers
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• v.30 no.10
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• pp.1039-1046
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• 2008

The combining process of UV irradiation and H$_2$O$_2$ was used to investigate characteristics of cefaclor decomposition in the aquatic environment. The separate mixing tank was used to minimize the decreasing effective of contact area caused by sampling. Four baffles were installed inside the UV reactor for the complete mixing of the sample and outside of the reactor was wrapped with aluminum foil to protect the emission of photon energy. Production of OH radical was measured using pCBA(p-Chlorobenzoic acid) indirectly and rate constants were withdrawn pseudo-frist order reaction. Optimum condition for the maximum production of OH radical was found to be pH 3, hydrogen peroxide of 5 mmol/L and recirculation rate of 400 mL/min. Pseudo-frist order reaction rate constant was 0.1051 min$^{-1}$. In the optimum condition, cefaclor was completely decomposed within 40 min and rate constant was 0.093 min$^{-1}$. Decomposition by OH radical producted intermediate anions such as chloride, nitrate, sulfite and acetic acid and phenylglycine. After 6 hr most cefaclor was decomposed by UV/H$_2$O$_2$ process and converted to CO$_2$ and H$_2$O, resulting of operation in the decrease of TOC and acetic acid and the disappearance of phenylglycine.

• Korean Journal of Clinical Pharmacy
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• v.7 no.1
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• pp.17-21
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• 1997

Cefaclor is a second generation cephalosporin antibiotic that shows a potent antibacterial activity against both Gram-positive and Gram-negative bacteria, when it is orally administered. Due to its patent expiration, a number of generic drugs have been marketed, but not yet elucidated to ensure therapeutic equivalence. In this study, cefaclor capsules manufactured by Chong Kun Dang were bioequivallently assessed by comparing with $Ceclor^{TM}$ introduced originally by Daewoong Lilly. A total of 16 healthy male volunteers were evaluated in a randomized crossover manner with a 2-week washout period. Concentrations of cefaclor in plasma were measured upto 6 hours following a single oral administration of two capsules (500 mg of cefaclor) by high-performance liquid chromatography with UV detection. Although the plasma concentration at 6 hours was not detected, the computed half-life of cefaclor was approximately 0.5 hours. The area under the concentration-vs-time curve from 0 to 4 hours $(AUC_{0-4h})$ was calculated by the trapezoidal summation method. The differences in mean values of $AUC_{0-4h}$, peak plasma concentration $(C_{max})$, and time to peak concentration $(T_{max})$ between the two products were $4.63\%,\;1.84\%,\;and\3.28\%$, respectively. The least significant differences at $\alpha4= 0.05 for $AUC_{0-4h},\;C_{max},\;and\;T_{max}\;were\;6,53\%,\;4.05\%,\;and\;6.47\%$, respectively. In conclusion, the test drug was bioequivalent with the reference drug.

• Journal of Pharmaceutical Investigation
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• v.35 no.2
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• pp.117-122
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• 2005

After establishing improved HPLC analytical method of cefaclor in human plasma samples, a bioavailability study of cefaclor capsules was conducted according to the guidelines of Korea Food and Drug Administration (KFDA). The standard calibration curve using an HPLC with UV detector was constructed in a range of $0.0324{\sim}16\;{\mu}g/ml$. The 6% perchloric acid instead of 6% trichloroacetic acid was used to precipitate plasma protein. The HPLC chromatograms were precisely and accurately resolved when spiked with human plasma spiked with cefaclor and cephalexin (internal standard). Twenty healthy male Korean volunteers received two commercial cefaclor capsules, $Neocef^{\circledR}$ capsule (Jinyang Pharm. Co., Ltd) or $Ceclor^{\circledR}$ capsule (Lilly Korea. Co., Ltd.) at the 250 mg cefaclor in a $2{\times}2$ crossover study. There was a one-week washout period between the doses. Plasma concentrations of cefaclor were monitored for 8 hours after oral drug administration. $AUC_t$ the area under the plasma concentration-time curve from time zero to 8 hr (13 points), was calculated by the linear trapezoidal rule method. $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{max}$) were compiled from the plasma concentration-time data. Analysis of variance was carried out using logarithmically transformed $AUC_t$ and $C_{max}$. No significant sequence effect was found for all of the bioavailability parameters indicating that the cross-over design was properly performed. The 90% confidence intervals of the $AUC_t$ ratio and the $C_{max}$ ratio for $Neocef^{\circledR}/Ceclor^{\circledR}$ were $0.9049{\leq}{\delta}{\leq}1.226$, respectively. These values were within the acceptable bioequivalence intervals of 0.80-1.25. Thus, our study demonstrated the bioequivalence of $Neocef^{\circledR}/Ceclor^{\circledR}$ with respect to the extent of absorption.

• Journal of Pharmaceutical Investigation
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• v.30 no.3
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• pp.201-205
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• 2000

Three new polymorphic modifications were prepared by recrystallization under various conditions and characterized by DSC and X-ray crystallography. In pH 4.0 buffer at $37{\pm}0.5^{\circ}C$, the polymorphic modifications showed significant differences in the dissolution rate. The dissolution rate of Mod. 4, amorphous form, was faster than that of marketed cefaclor (Mod. 1). When all modifications were stored at 52% RH, 95% RH and in silica gel desiccator, any polymorphic transformation was not observed.

• Korean Journal of Clinical Pharmacy
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• v.15 no.1
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• pp.21-26
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• 2005

A bioequivalence study of CKD $Cefaclor^{(R)}$ capsule (Chong Kun Dang Pharm Co., Ltd) to $Ceclor^{(R)}$ capsule (Lilly Korea Co., Ltd.) was conducted according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty four healthy male Korean volunteers received each medicine at the cefaclor dose of 250 mg in a $2{\times}2$ crossover study. There was a one-week washout period between the doses. An improved high-performance liquid chromatorgraphy (HPLC) analytical method with UV detection was used to determine plasma cefaclor concentration in human volunteers for 8 hr after oral drug administration. The area under the plasma concentration-time curve from time zero to 8 hr ($AUC_{0-8hr}$) was calculated by the linear trapezoidal rule. the $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{max}$) were compiled from the plasma concentration-time data. Analysis of variance was carried out using logarithmically transformed $AUC_{0-8hr}\;and\;C_{max}$. No significant sequence effect was found for all of the bioavailability parameters indicating that the cross-over design was properly performed. The $90{\%}$ confidence intervals of the $AUC_{0-8hr}$ ratio and the $C_{max}$ ratio for CKD $Cefaclor^{(R)}$ and $Ceclor^{(R)}$ were $0.9400{\leq}{\delta}{\leq}1.0345$ and $0.8858{\leq}{\delta}{\leq}1.1021$, respectively. These values were within the acceptable bioequivalence intervals of 0.80-1.25. Thus, our study demonstrated the of CKD $cefaclor^{(R)}$ capsule was bioequivalent to $Cefaclor^{(R)}$ capsule with respect to its bioavailability.

• Journal of Pharmaceutical Investigation
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• v.35 no.1
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• pp.39-44
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• 2005

The purpose of the present study was to evaluate the bioequivalence of two cefaclor capsules, Ceclor (Lilly Korea Co., Ltd.) and Kyongbocefaclor (Kyongbo Pharm. Co., Ltd.), according to the guidelines of the Korea Food and Drug Administration (KFDA). The release of cefaclor from the two cefaclor formulations in vitro was tested using KP VIII Apparatus II method with various dissolution media (pH 1.2, 4.0, 6.8 buffer solution and water). Twenty four healthy male subjects, $22.96{\pm}1.52$ years in age and $67.03{\pm}7.90$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ crossover study was employed. After one capsule containing 250 mg of cefaclor was orally administered, blood was taken at predetermined time intervals and the concentrations of cefaclor in serum were determined using HPLC method with UV detector. The dissolution profiles of two formulations were similar at all dissolution media. In addition, 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 $AUC_t$, $C_{max}$ and untransformed $T_{max}$. The results showed that the differences between two formulations based on the reference drug, Ceclor, were -1.90%, 2.68% and -7.60% for $AUC_t$, $C_{max}$ and $T_{max}$, respectively. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals using logarithmically transformed data were within the acceptance range of log 0.8 to log 1.25 $(e.g.,\;log0.91{\sim}log\;1.06\;and\;log0.92{\sim}log\;1.18\;for\;AUC_t\;and\;C_{max}$, respectively). Thus, the criteria of the KFDA bioequivalence guideline were satisfied, indicating Kyongbocefaclor capsule was bioequivalent to Ceclor capsule.

• YAKHAK HOEJI
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• v.41 no.1
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• pp.30-37
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• 1997

In order to formulate a controlled release system for oral drug delivery, the microcapsules were prepared in w/o emulsion containing cefaclor as a water-soluble model drug by th e method of interfacial polycondensation. Gelatin wis selected as a suitable polymer for interfacial polycondensation. Gelatin solution containing drug was emulsified in an organic phase under mechanical stirring. After emulsification, terephthaloyl chloride was added as cross linking agent, followed by mechanical stirring, washing and drying. Physical characteristics of microcapsules were investigated by optical microscopy, scanning electron microscopy and particle size analysis. Mean particle sizes of gelatin microcapsules were, in the range, of about 20~50 ${\mu}$m. The microcapsules were in good apperance with spherical shapes before washing, but were destroyed partially after washing and drying, even though some microcapsules were still maintained in their shapes. Contents of cefaclor in the microcapsules were calculated by UV spectrophotometry after 3 days extraction with pH 4 carbonate buffer solution. The effects of cross linking time. pH. concentration of cross-linking agent, and temperature on drug release kinetics have been discussed extensively.