• Archives of Pharmacal Research
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• v.17 no.1
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• pp.51-53
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• 1994

• Health Policy and Management
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• v.10 no.3
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• pp.50-67
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• 2000

This study aims to estimate the consumption of antibiotics in Korea and to suggest the further studies. To measure the amount of antibiotics consumption, we referred to the statistic of NFHI(National Federation of Health Insurance) and a private institute of pharmaceutical information(Korea Intercontinental Medical Statistics; IMS Korea). There were 1,563 antibiotics produced in Korea in 1997. The total amount of antibiotics production was 1,197 billion won in 1997. Antibiotics accounted for 17.6% of the total pharmaceutical productions in 1997. Cephalosporins have taken the largest part of antibiotics production since 1992. The estimation using NFHI data showed that the total expenditure of antibiotics used in health facilities was 268 billion won, 608 billion won, 911 billion won in 1990, 1994, 1997 respectively. Tertiary hospitals spent 246 billion won, general hospitals 287 billion won, hospitals 78 billion won, clinics 300 billion won in 1997. The amount of expenditure and the intensity of antibiotics consumption in hospitals have increased more steeply than any other health facilities. The total expenditure of antibiotics consumption in health facilities and pharmacies was 778 billion won when estimated using the data from IMS Korea, and 999 billion won from NFHI. Cephalosporins was the fast growing antibiotics group in all of the market- hospitals, clinics, pharmacies since 1991. To measure the amount and patterns of antibiotics consumption more precisely, a pharmaceutical monitoring or surveillance system is needed.

• YAKHAK HOEJI
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• v.25 no.4
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• pp.161-165
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• 1981

The binding of two cephalosporins, cephalothin and cefazoline to human serum albumin(HSA) was studied by difference spectrophotometry using a spectrophotometric probe, 2-(4'-hydroxybenzeneazo) benzoic acid. The probe is strong visible absorbing material which interacts with serum albumin to give characteristic spectrophotometric peaks and provides the basis for a convenient assay to measure free and bound amounts in the presence of serum albumin and competitive drugs. The results obtained showed that the probe and cephalosporin compete for the same binding site on human serum albumin; thus the probe can be used to gauge the displacement of cephalosporins from human serum albumin. The data were interpreted on the basis of theory of multiple equilibria. The number of binding sites of human serum albumin for 2-(4'-hydroxybenzeneazo) benzoic acid(HBAB), cephalothin and cefazoline appears to be 4. By using this technique the binding constants were found as follows: HSA-HBAB, $7.89{\times}10^{4}M^{-1}$; HSA-cephalothin, $1.09{\times}10^{3}M^{-1}$ ; HSA-cefazoline, $1.21{\times}10^{3}M^{-1}$.

• Journal of Pharmaceutical Investigation
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• v.29 no.3
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• pp.205-210
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• 1999

To formulate the parenteral delivery of a new cephalosporin derivative, 7-${\beta}$-[(2)-2-(2-arninothiazol-4-yl)-2methoxyiminoacetamido]- 3- [(2,3-cyclopenteno-4-carbamoyl-l-pyridinium)methyl]- 3-cephem-4-carboxylate sulfate( CKD604), the stability and solubility of CKD-604 in various aqueous media were investigated. The degradation kinetics of CKD-604 in aqueous solutions (ionic strength 0.1, pH 1-8) were studied at $37^{\circ}C$. The observed degradation rates followed pseudo first order kinetics. The pH-rate profile exhibited a minimum degradation rate at pH 5. The Arrhenius activation energy was 14.2 kcal/mol in pH 5 buffer solution. Excellent agreement between the cephalosporins' theoretical pH-rate profile and the experimental data indicated that the degradation pathway of CKD-604 could be predicted according to the general pathway of cephalosporins. The solubility of CKD-604 was 8.16 mg/ml at $25^{\circ}C$. To enhance the solubility and adjust the suitable pH, CKD-604 was solubilized by using sodium ascorbate, ascorbic acid and urea. The compositions were obtained to satisfy optimum pH and concentration, and the total amount of additives was several times of the active ingredient, CKD-604.

• Proceedings of the Korean Society for Applied Microbiology Conference
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• 1977.10a
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• pp.192-193
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• 1977

It is certainly a difficult work to find out novel-type "practical" antibiotic from natural sources. In fact, chemically modified antibiotics, such as synthetic penicillins, cephalosporins, derivatives of tetracycline, lincomycin, rifamycin and kanamycin are most widely used in medical practice at present. However, as the possibility of success gained by chemical modification is limited, it would be the buty of our applied microbiologists to offer novel antibiotics to chemist and physician without interruption. In this lecture, some practical problems in new antibiotic research will be discussed.(중략)

• Archives of Pharmacal Research
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• v.21 no.5
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• pp.559-564
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• 1998

Preparation and biological activity of prodrug-type 3-methoxymethyl cephalosporins were described. From the mixtures, R- and S-prodrugs were separated and their absolute configurations were determined, and also their bioavailability was investigated.

• Archives of Pharmacal Research
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• v.20 no.3
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• pp.288-290
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• 1997

An efficient synthesis of 3-(E)-hydroxy- and 3-(E)-acetoxypropenylcephem derivatives, key intermediates for the synthesis of 3-(E)-propenylcephalosporins was achieved via Stille coupling reaction of 3-trifloxycephem with 3-(E)-tributylstannylallylic alcohol.

• Bulletin of the Korean Chemical Society
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• v.14 no.1
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• pp.32-38
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• 1993

3-(3-Bromotetrahydrofuran-2-yl)-3-cephem 7 was obtained from 3-(2-hydroxyethyl)vinyl-3-cephem 6 by the cyclization reaction using N-bromosuccinimide. Compound 5 was prepared by Wittig reaction, namely a coupling of cephem-derived triphenylphosphonium salt 3 with aldehyde component 4 in the presence of base.

• YAKHAK HOEJI
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• v.28 no.1
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• pp.25-27
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• 1984

Some $\betha$-lactam antibiotics-penicillins and cephalosporins-were determined by gas chromatography (GC) with flame photometric detector (FPD) which was selective and sensitive to sulfur-containing compounds. Methyl ester derivatives of carboxyl group in $\betha$-lactam antibiotics were prepared using 0.5Mmethyl iodide in methylene chloride and were taken for gas chromatography with 0.9% or 0.6% QF-1 on Chromosorb WAW-DMCS. We have found that it is possible to determine methyl esters of $\betha$-lactam antibiotics by GC/FPD.

• Proceedings of the PSK Conference
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• 2000.04a
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• pp.161.2-161.2
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• 2000