• Journal of Pharmaceutical Investigation
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• v.31 no.1
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• pp.37-41
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• 2001

Various characteristics of polyethylene oxide (PEO) are useful for drug delivery systems. In this study, PEO was used as a sustained release matrix system containing cefatrizine propyleneglycol (Cefa-PG) which is a new semi-synthetic broad-spectrum and orally active cephalosporin. Five kinds of sustained release matrix tablets were formulated with various content of PEO and other ingredients. And three types of matrix tablets were formulated of which compositions were the same but the hardness was different. It was found that PEO content influenced drug release rate. Increasing PEO content, the drug release rate from matrix tablets was decreased. In addition, Avicel, one of the ingredients of matrix components, changed the drug release from the sustained release PEO matrix tablets. With increasing Avicel content, the rate of drug release was increased. For the effect of hardness of matrix tablets, the rate of drug release is decreased with increasing hardness. In comparison of bioavailability parameters after oral administration of Cefa-PG PEO matrix tablets and general Cefa-PG capsule in beagle dog, the sustained release PEO matrix tablets is more useful than a general dosage form. $AUC^{0-12}$ of the sustained release PEO matrix tablet and the general dosage form was 1.16 and 0.644 respectively.

• The Journal of Internal Korean Medicine
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• v.34 no.3
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• pp.278-288
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• 2013

Objectives : Methicillin-resistant Staphylococcus aureus (MRSA) has a cephalosporin and beta-lactam antibiotic-resistant strains. MRSA is one of the major pathogens causing hospital infection and the isolation ratio of MRSA has gradually increased. Consequently, increased resistance to antibiotics is causing serious problems in the world. Therefore, there is a need to develop alternative antimicrobial drugs for the treatment of infectious diseases. Methods : The antibacterial activities of Ipyo-san were evaluated against 2 strains of MRSA and 1 standard Methicillin-susceptible staphylococcus aureus (MSSA) strain by using the disc diffusion method, minimal inhibitory concentrations (MIC) assay, colorimetric assay using MTT test, checkerboard dilution test and time-kill assay performed under dark. Results : The MIC of Ipyo-san water extract against S. aureus strains ranged from 1000 to $2,000{\mu}g/ml$, so we confirmed that it had a strong antibacterial effect. Also, the combinations of Ipyo-san water extract and conventional antibiotics exhibited improved inhibition of MRSA with synergy effect. We suggest that Ipyo-san water extract against MRSA has antibacterial activity so it has potential as alternatives to antibiotic agents. For the combination test, we used Triton X-100 (TX) and DCCD for measurement of membrane permeability and inhibitor of ATPase. As a result, antimicrobial activity of Ipyo-san water extract was affected by the cell membrane. Conclusions : We suggest that the Ipyo-san water extract lead the treatment of bacterial infection to solve the resistance and remaining side-effect problems that are the major weak points of traditional antibiotics.

• Korean Journal of Veterinary Research
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• v.47 no.4
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• pp.475-478
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• 2007

A 4-year-old spayed female, Yorkshire terrier dog with a history of petechial and ecchymotic hemorrhages on the face, trunk and hind limb was referred to Veterinary Medical Teaching Hospital, Cheju National University. The complete blood count revealed a marked thrombocytopenia ($96{\times}10^3/{\mu}l$). The biochemical profile showed only slightly increased glucose. The coagulation profile such as prothrombin time and activated partial thromboplastin time, was within the reference range. In Giemsa staining, there were no endoparasites like as Babesia spp. on the RBC. This case was diagnosed as a idiopathic thrombocytopenia in a Yorkshire terrier dog. She was treated with prednisone (1 mg/kg BW, IM q 12 h) and cephalosporin (10 mg/kg BW, IM, q 12 h). When rechecked on day 6, the platelet was within reference range ($507{\times}10^3/{\mu}l$) and also petechial and ecchymotic hemorrhages on the body were gradually improved without any complications. The dose of prednisone was decreased to 0.5 mg/kg BW, q 24 h. On day 17, we finished treatment because all the clinical signs, blood and serum chemistry were reference range and platelet count was dramatically increased.

• Biomolecules & Therapeutics
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• v.15 no.3
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• pp.182-186
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• 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.).

• The Journal of the Korean Society for Microbiology
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• v.18 no.1
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• pp.39-46
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• 1983

We collected three hundred thirty-five strains of Salmonella typhi isolated from human sources during the period January to December 1982 Korea. Most of them were from general hospitals and city health center, the remaining one hundred sixtyone strains were obtained from other 12 provincial health centers among 335 testing strains. We used ninety-nine Vi-phages as distributed from International Center for Enteric phage Typing(ICEPT) in London. We found nine phage types among 335 strains of Salmonella typhi in this study. Additionally, I+IV, degraded Vi-positive and Vi negative strains were presented. This study documented the occurrence of the new $B_2$ type in Korea for the first time. The present basic phage type formula in Korea appeared to be A, $B_2,\;D_1,\;D_2,\;D_4,\;D_6,\;D_8,\;D_{12},\;E_1,\;E_9,\;D_1,\;M_1$, 40 and plus I+IV and degraded vi strains(Table 2). The current phage types of Salmonella typhi isolated in Korea 1982 were A, $B_2,\;D_1,\;D_2,\;D_6,\;D_8,\;E_1,\;M_1$ and 46 $M_1$ type was widely distributed all over the country, and E type was next predominant. Antibiotic susceptibility test were performed by means of Kirby-Bauer disc diffution method using 12 kind of antibiotics such as Ampicillin, Carbenicillin, Cephalosporin, Chloramphenicol, Colistin, Gentamicin, Kanamycin, Nalidix acid, Neomycin, Polymyxin-B, Streptomycin and Tetracycline. The sensitivity pattern to antibiotics of Salmonelia typhi cultures were summarized.

• The Journal of the Korean Society for Microbiology
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• v.19 no.1
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• pp.55-64
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• 1984

The clinical specimens used in this study were collected during the period from March 4, to December 30, 1983, from children's hospitals in Seoul area. They came from clinically apparent cases of diarrheal disease in hospitals. Many specimens were taken from rectal Swabs. During this period, 2166 stool cultures were streaked onto MacConkey plate and were them deposited in selenite broth. Colonies resembling pathogens on MacConkey medium were picked to KIA, Urea agar, malonate broth, ONPG broth, SIM. Reaction on those media cultures were identified biochemically with using API 20E test kit and confirmed serologically with commercially avabile Salmonella antisera(Difco) or Shigella antisera(Denka, Japan). The sensitivity of Salmonella and Shigella tested to ampicillin cephalosporin, chloramphenicol, colistin, gentamicin, tetracycline, streptomycin, nalidixic acid, neomycin, polymyxin B was performed by means of disc diffusion method recommended by Bauer-Kirby, using the discs prepared in BBL Laboratory. 1. There were 34 (1.6%) isolations of Salmonella cultures and 52(2.4%) isolations of Shigella from the 2,116 specimens. Only 53%of Salmonella were isolated by direct streaking on MacConkey plating media, by contrast, 80% of the Shigella were isolated directly. 2. Shigella flexneri types comprised 56% of the Shigellae isolate from 52 Shigellae identified 24% of Salmonella enteritidis ser typhimurium were identified. 3. Concerning to Salmonella and Shigella occurance according to month and sex, They shows relatively higher for the male than in case of female, and 2-3 age were shown the highest group. 4. October is the month with highest incidences. 5. In the sensitivity patterns of Shigellae, most of them were appeared to be resistant ampicillin, streptomycin, tetracycline, in case of Salmonella, 15% of them were resistant to chloramphenicol.

• YAKHAK HOEJI
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• v.27 no.3
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• pp.185-205
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• 1983

Penicillins and cephalosporins are biosynthesized from L-.alpha.-aminoadipic acid, L-cysteine and L-valine. A tripeptide, LLD-$\delta$-($\alpha$-aminoadipyl)cysteinylvaline(LLD-ACV) was isolated from fermentation broths of Cephalosporium acremonium as well as of Penicillium chrysogenum and it was proved that the LL-$\delta$-($\alpha$-aminoadipyl cysteine was formed first in mycelia, to which valine would be connected to give LLD-ACV. However, several points are still unsolved; first, what mechanism is involved in the configurational change from L-valine to D-valine, second, what kind of cyclization mechanism gives a $\betha$-lactam ring and a thiazolidine ring and third, what is the pathways for the ring expansion from penicillins to cephalosporins. At present, it seems clear that LLD-ACV is cyclized to give isopenicillin N, which is transformed to penicillin N and further to cepbalosporin C. Other hydrophobic penicillins, including benzyl penicillin and penicillin V, are formed from isopenicillin N by acyl-exchange reactions catalyzed by penicillin transferase, rather than by acylation reaction on 6-aminopenicillanic acid(6-APA), which was isolated from the fermentation broth of P. chrysogenum and which would be formed by hydrolysis of $\delta-(\alpha$-amincadipyl)amido moiety at the C-6 position in isopenicillin N or penicillin N by penicillin acylase. Acylation of 6-APA is catalyzed also by penicillin acylase, but the reaction is proved not to be involved in penicillin biosynthesis. Understanding the biosynthesis of penicillins and cephalsoporins would provide solutions to increase in fermentation yields of penicillins, especially of cephalosporins and a solution to biological production of 7-aminocepbalosporanic acid (7-ACA) which is of importance in pharmaceutical industry. Still regulation mechanisms in penicillin and cephalosporin biosynthesis are unveiled at all.

• YAKHAK HOEJI
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• v.46 no.4
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• pp.290-294
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• 2002

Cephradine is an orally absorbed cephalosporin with a broad spectrum of activity against gram-positive and gram-negative bacteria and is highly resistant to beta-lactamase degradation. The purpose of the present study was to evaluate the bioequivalence of two cephradine capules, Cephradine capsule (Donggu Pharmaceutical Co., reference drug) and Cephradine capsule (Shinpoong Pharmaceutical Co., test drug), according to the guidelines of Korea Food and Drug Administration. Twenty-six normal volunteers, 24.6 $\pm$ 3.70 years in age and 62.4 $\pm$ 8.99 kg in body weight, were divided into two groups and a randomized 2 $\times$ 2 cross-over study was employed. After one capsule containing 250 mg of cephrdine was orally administered, blood was taken at predetermined time intervals and the concentrations of cephrdine in serum were determined using HPLC with UV detector. The pharmacokinetic parameters such as AU $C_{t}$ to $C_{max}$ and $T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters. The results showed that the differences in AUCt, $C_{max}$ and $T_{max}$ between two products were 2.89％, 1.05％ and 1.06％, respectively, when calculated against the reference drug. The 90％ confidence intervals were within log0.8 $\leq$ $\delta$ $\leq$ log1.25 (e.g., log0.9803 $\leq$ $\delta$ $\leq$ log1.0734 and log0.9674 $\leq$ $\delta$ $\leq$ log1.220 for AU $C_{t}$, and $C_{max}$, respectively). Two parameters met the criteria of KFDA for bioequivalence, indicating that Cephradine capsules (Shinpoong Pharmaceutical Co.) is bioequivalent to Cephradine capsules (Donggu Pharmaceutical Co.).o.).o.).).o.).

• Archives of Pharmacal Research
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• v.26 no.1
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• pp.83-88
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• 2003

KR-984055 is a new oral cephalosporin antibiotic with activity against both gram-positive and gram-negative bacteria. Lipophilic ester-type prodrugs of KR-984055, i.e., KR-999001 and KR-999002, have been synthesized in an attempt to increase the oral bioavailability of this broad-spectrum antibiotic agent. In this study we determined the oral bioavailability of KR-984055 and its prodrugs in the rat, and evaluated the pharmacokinetic model that best describes the plasma concentration behavior following single intravenous (IV) and oral single dose. In addition, concentrations in plasma as well as biliary and urinary recovery of KR-984055 were determined. Also, protein binding of KR-984055 in plasma was examined in vitro. The degree of protein binding of KR-984055 was in the range of 92.09~94.77%. KR-984055 exhibited poor oral bioavailability (7.02$\pm$1.58%). The observed oral bioavailabilities of KR-984055 from KR-999001 and KR-999002 were 38.77$\pm$2.81 % and 39.81$\pm$5.25%, respectively. These data were calculated from the levels of free KR-984055 in plasma. Oral KR-999001 and KR-999002 were not recovered from plasma, suggesting that it was readily cleaved to free KR-984055. KR-999001 and KR-999002 appear to be an efficient oral prod rug of KR-984055 that deserved further clinical evaluation in human.

• Journal of Korean Academy of Nursing
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• v.50 no.4
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• pp.621-630
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• 2020

Purpose: This study was aimed to evaluate the external validity of a carbapenem-resistant Enterobacteriaceae (CRE) acquisition risk prediction model (the CREP-model) in a medium-sized hospital. Methods: This retrospective cohort study included 613 patients (CRE group: 69, no-CRE group: 544) admitted to the intensive care units of a 453-beds secondary referral general hospital from March 1, 2017 to September 30, 2019 in South Korea. The performance of the CREP-model was analyzed with calibration, discrimination, and clinical usefulness. Results: The results showed that those higher in age had lower presence of multidrug resistant organisms (MDROs), cephalosporin use ≥ 15 days, Acute Physiology and Chronic Health Evaluation II (APACHE II) score ≥ 21 points, and lower CRE acquisition rates than those of CREP-model development subjects. The calibration-in-the-large was 0.12 (95% CI: - 0.16~0.39), while the calibration slope was 0.87 (95% CI: 0.63~1.12), and the concordance statistic was .71 (95% CI: .63~.78). At the predicted risk of .10, the sensitivity, specificity, and correct classification rates were 43.5%, 84.2%, and 79.6%, respectively. The net true positive according to the CREP-model were 3 per 100 subjects. After adjusting the predictors' cutting points, the concordance statistic increased to .84 (95% CI: .79~.89), and the sensitivity and net true positive was improved to 75.4%. and 6 per 100 subjects, respectively. Conclusion: The CREP-model's discrimination and clinical usefulness are low in a medium sized general hospital but are improved after adjusting for the predictors. Therefore, we suggest that institutions should only use the CREP-model after assessing the distribution of the predictors and adjusting their cutting points.