• 생약학회지
• /
• 제14권4호
• /
• pp.178-192
• /
• 1983

Polygalae Radix was used as diuretics, analgesics and expertorants in oriental medicine. The root of Polygala tenuifolia Willd. (Polygalaceae) is comprised saponin (Onjisaponin A,B,C,D,E,F and G) polygalitol, onsitin and sugars. The pharmacological action of crude Polygala-saponin (PS) obtained from the roots are studied. The following results were obtained; 1) The median lethal dose $(LD_{50})$ of PS in mice is presented 71.1mg/kg s.c. and 694. 5mg/kg p.o.. 2) PS demonstrated diuretic action of relatively long acting duration in mice. 3) The diuretic mechanism of PS was found due to inhibitory effect of renal tubular reabsorption of electrolytes and glomerular vascular dilatation. 4) The group, administered simultaneously PS and cefadroxil monobydrate was significantly increased with PS alone group on diuretic action. Synergistic effect cefadroxil monohydrate on the diuretic action of PS seems due to competitive inhibition of plasma protein binding with PS. 5) PS demonstrated analgesic action by the acetic acid stimulating method and Randall-Selitto test in mice. 6) PS presented antipyretic action against febrile treated with the typhoid vaccine. 7) PS was significantly prolonged against the hypnotic duration of pentobarbital in mice. 8) Onset time convulsion and death induced by picrotoxin and strychnine in mice were not delayed. According to the above results, the PS was identified as a pharmacological active component obtained from roots of Polygala tenuifolia Willd.

• 미생물과산업
• /
• 제20권1호
• /
• pp.42-45
• /
• 1994

아미노산은 식품이나 사료의 첨가물로, 의약품으로 그리고 화학합성에 있어서의 단위구조체(building block)로써 널리 이용되어 왔는데, 위에서 광학적으로 순수한 single enantiomer로서 D- 혹은 L-form의 .alpha.-아미노산은 의약품의 합성에 있어서 그 산업적 중요성이 날로 증대되고 있다. 이중 D-form의 아미노산은 .betha.-lactam계 항생제, peptide hormone, 살충제 등의 합성에서 중간 물질로 사용되고 있는데, 특히 D-p-hydroxyphenylglycine(이하 D-HPG)의 경우 amoxicillin, cefadroxil, cefatrizine, cefaparole, cefaperazone등의 penicillin이나 cephalosporin계의 반합성항생제의 전구체로서 전 세계적으로 널리 사용되고 있다.

• 분석과학
• /
• 제23권2호
• /
• pp.119-127
• /
• 2010

환경 시료중에 잔류하는 베타-락탐계 항생제를 동시에 추출하는 방법을 확립하였다. pH 2 에서 HLB 고체상을 사용하여 추출 및 정제한 후, 7종의 베타-락탐계 항생제(amoxicillin, ampicillin, penicillin G, cefaclor, cefadroxil, cefatrizine 및 cephradine)를 LC/ESI-MS/MS를 사용하여 동시에 분석하였다. 새롭게 확립된 분석법은 하천수중에서 베타-락탐계 항생제의 농도가 0.01~1.0 ng/mL일 때 정량을 위한 검정곡선의 상관계수($r^2$)가 0.9911~0.9995 범위로써 우수한 직선성을 나타내었다. 바탕하천수로부터 구한 검출한계(LOD)와 정량한계(LOQ)는 각각 0.0003~0.0234 ng/mL 와 0.0046~0.0778 ng/mL이었다. 이 분석방법은 물 환경중에 잔류하는 베타-락탐계 항생제를 정성 정량하는데 빠르고 신뢰할 만한 방법이 될 것이다.

• 한국어병학회지
• /
• 제31권1호
• /
• pp.23-34
• /
• 2018

세파드록실 (CDX)의 수온에 따른 잔류 약동학적 특성을 알아보기 위해 평균 660 g의 넙치를 비교수온 ($13{\pm}3^{\circ}C$) 및 적정수온 ($22{\pm}3^{\circ}C$)에서 7일간 임상용량 (45 mg/kg b.w.)과 임상용량의 5배에 해당하는 양 (225 mg/kg b.w.)으로 연속 경구투여 후 시간에 따른 근육, 혈장, 위-장관, 조혈조직 (신장+비장) 및 간장에서 잔류농도를 HPLC-MS/MS로 분석하였다. CDX의 농도 측정을 위해 근육에서는 투여종료 후 0.25, 0.5, 1, 3, 7, 14 및 28일에 분석하였고, 혈장, 위-장관, 조혈조직 및 간장에서는 1, 3, 7, 14 및 28일에 분석하였다. 경시적 잔류농도를 바탕으로 PKSolver program의 non-compartmental model로 최고농도 ($C_{max}$), 최고농도 도달시간 ($T_{max}$), 배설반감기 ($T_{1/2}$) 등의 약물동태학적 매개변수(parameter)를 계산하였다. 근육, 혈장, 위-장관, 조혈조직 및 간장에서 최고농도 및 최고농도 도달시간은 각각 $985.98-5,032.86{\mu}g/kg$ (1일), $5,670.99-38,922.23{\mu}g/l$ (1일), $2,457.27-10,192.78{\mu}g/kg$ (1일), $886.04-3,070.87{\mu}g/kg$ (1일) 및 $1,188.15-3,814.33{\mu}g/kg$ (1일)으로 계산되었다. 평균체류시간 ($MRT_{0-{\infty}}$)과 배설반감기 ($T_{1/2}$)는 각각 1.51-4.74일 (1.08-3.47일), 2.12-3.06 (1.14-5.42일), 4.25-13.18일 (3.56-10.99일), 1.37-18.66일 (1.17-14.93일) 및 1.78-29.76일 (1.25-28.55일)로 계산되었다.

• 한국물환경학회지
• /
• 제29권3호
• /
• pp.409-419
• /
• 2013

In this study, the analytical method for 27 residual pharmaceuticals in raw water was developed. Online sample preconcentration/extraction and analysis with high resolution Orbitrap mass spectrometry (LC-ESI/Orbitrap MS) were performed. The calibration curves showed good linearities (above $r^2$ = 0.998) in the range of 5 ~ 1,000 ng/L. The method detection limit and the limit of quantification were 1.1 ~ 10.0 ng/L and 3.4 ~ 31.7 ng/L, respectively. Recoveries of the target compounds were between 70.1% and 115.8% (except cefadroxil, cefradine, vancomycin, and iopromide (50.2 ~ 67.0%)). The optimized analytical method can be useful to determine the residual pharmaceuticals in raw water.

• 약학회지
• /
• 제38권2호
• /
• pp.114-122
• /
• 1994

A study on the absorption mechanism of cefixime(CF), an oral ${\alpha}-amino$ group deficient cephalosporin antibiotic, has been undertaken through the rat jejunum and nasal cavity using an in situ simultaneous perfusion technique developed in our laboratory. CF was well absorbed in the jejunum and nasal cavity of rats at pH 5.0, but not at pH 7.0. CF absorption was studied over four orders of magnitude in concentration to determine saturability. Disappearance of CF in the perfusate followed first-order kinetics at all tested concentrations. The apparent first-order absorption rate constant was found to be dependent on the concentration over the range of $0.1\;mM{\sim}3\;mM$ in the jejunum and nasal cavity of rats. Inhibitors were added to determine the competitive inhibition of CF absorption. The presence of L-tyrosine, L-phenylalanine, alanine-alanine, glycine-glycine and cefadroxil produced the significant inhibition of CF absorption in the nasal cavity and jejunum. However, there was no evidence of the inhibition in the presence of cefazolin. In addition, The CF absorption in the nasal cavity and jejunum was inhibited significantly by ouabain and 2,4-dinitrophenol(DNP). This study suggested that CF is absorbed across the rat nasal cavity and jejunum by carrier-mediated transport mechanism and energy consuming system.

• 한국임상약학회지
• /
• 제5권2호
• /
• pp.13-16
• /
• 1995

The Minimum Inhibitory Concentration (MIC) of a first-generation cephalosporin derivative, Cefazedone (CZD; $PAZERON^R$ inj.) was determined by the two-fold serial agar dilution method. The in-vitro antibacterial activity of CZD against a wide variety of clinical isolates was compared with those of other first generation cephalosporins such as Methylol Cephalexin (CEX), Cefazolin (CEZ), Cefadroxil (CDX), Cephradine (CED), Ceftezol (CTZ) and one of second generation cephalsporin antibiotics, Cefotaxime (CTX). CZD had the most potent inhibitory effect against Gram-positive strains, when compared to the first-generation cephalosporin antibiotics tested in this study and CTX. The geometric MIC mean of CZD for Gram-positive strains was calculated as 0.386 kg/m{\ell}$, and those of CEX, CEZ, CDX, CTZ, CED, and CTX were 6.073, 0.894, 3.399, 0.748, 7.884 and 1.502 $kg/m{\ell}$, respectively. In addition, the geometric mean of CZD for staphylococclJs aureus strains was obtained as 0.340 $kg/m{\ell}$ and those of CEX, CEZ, CDX, CTZ, CED, and CTX 6.145, 0.534, 4.126, 0.442, 10.51, and 2.500 $kg/m{\ell}$, respectively. Against Gram-negative strains, CZD showed better antibacterial activity than CEZ, CDX, CTZ, and CED.

• 한국환경보건학회지
• /
• 제32권5호
• /
• pp.462-468
• /
• 2006

Antibiotics are manufactured and used for specific physiological functions, hence they may exert adverse ecological consequences when they are in contact with nontarget organisms. In the last decade, many reports have been made on the occurrences of various antibiotic compounds in surface water, and their potential impact to the environment has become an increasing concern. This study was conducted to prioritize antibiotic substances with potential environment risk in Korea. Human use antibiotics with an EIC (Expected Introduction Concentration) value greater than $1{\mu}g/l$, US FDA's action limit criteria, were selected. In order to calculate a worst-case EIC for each substance, annual production volume (in kg) of each antibiotic substance was derived using the Korea Pharmaceutical Manufacturers Association (KPMA)'s monetary database. Sixteen substances were preliminarily selected. The EICs of the 16 antibiotic substances were refined with the excretion rate of the parent substances. Ten antibiotic substances were identified to have EIC-corrected greater than $1{\mu}g/l$, which include Amoxicillin ($15.8{\mu}g/l$), Cefaclor ($10.1{\mu}/l$), Roxithromycin ($4.2{\mu}g/l$), Cephradine ($4.5{\mu}g/l$), Cefatrizine ($2.6{\mu}g/l$), Cefadroxil ($3.3{\mu}g/l$), Aztreonam ($2.3{\mu}g/l$), Ceftazidime ($2.8{\mu}g/l$), Ribostamycin ($1.3{\mu}g/l$), and Ceftezole ($1.3{\mu}g/l$). Additional risk assessments for these antibiotic substances are suggested.

• Biomolecules & Therapeutics
• /
• 제20권1호
• /
• pp.36-42
• /
• 2012

Baicalin, a main constituent of the rhizome of Scutellaria baicalensis, is metabolized to baicalein and oroxylin A in the intestine before its absorption. To understand the role of intestinal microflora in the pharmacological activities of baicalin, we investigated its anti-inflammatory effect in mice treated with and without antibiotics. Orally administered baicalin showed the anti-inflammatory effect in mice than intraperitoneally treated one, apart from intraperitoneally administered its metabolites, baicalein and oroxylin A, which potently inhibited LPS-induced inflammation. Of these metabolites, oroxylin A showed more potent anti-inflammatory effect. However, treatment with the mixture of cefadroxil, oxytetracycline and erythromycin (COE) significantly attenuated the anti-inflammatory effect of orally administered baicalin in mice. Treatment with COE also reduced intestinal bacterial fecal ${\beta}$-glucuronidase activity. The metabolic activity of human stools is significantly different between individuals, but neither between ages nor between male and female. Baicalin was metabolized to baicalein and oroxylin A, with metabolic activities of $1.427{\pm}0.818$ and $1.025{\pm}0.603$ pmol/min/mg wet weight, respectively. Baicalin and its metabolites also inhibited the expression of pro-inflammatory cytokines, TNF-${\alpha}$ and IL-$1{\beta}$, and the activation of NF-${\kappa}B$B in LPS-stimulated peritoneal macrophages. Of them, oroxylin A showed the most potent inhibition. Based on these findings, baicalin may be metabolized to baicalein and oroxylin A by intestinal microflora, which enhance its anti-inflammatory effect by inhibiting NF-${\kappa}B$ activation.

• 분석과학
• /
• 제23권6호
• /
• pp.572-578
• /
• 2010

본 연구에서는 하천수 중 6종의 의약물질(cephradine, cefadroxil, penicillin G, vancomycin, iopromide, and fenbendazole)에 대한 전처리법과 분석 방법을 확립하였다. 하천수 중의 분석물질을 HLB(Hydrophilic-Lipophilic Balanced) 카트리지를 사용하여 추출/정제 및 농축하였다. HPLC/ESI-MS/MS를 이용하여 6종의 물질들을 동시에 분석하였다. Fenbendazole을 제외한 의약물질은 71.1~92.6% 범위의 양호한 회수율을 나타내었고, 상대표준편차는 11.2% 이하로 나타났다. 정량분석을 위해서 0.007~1.2 ng/mL 범위에서 $r^2$=0.99 이상의 높은 직선성을 나타내는 검량선을 얻었다. 검출한계(LOD)와 정량한계(LOQ)는 각각 7.2~128.7 pg/mL, 23.8~429.1 pg/mL로 나타났다. 이 분석 방법은 하천수 중 의약품에 대한 모니터링에 유용하며, 하천수 중 iopromide과 fenbendazole은 높은 농도로 검출되었다.