Fosfomycin의 항균효과 및 capillary electrophoresis에 의한 측정법에 관한 연구

윤효인,박승춘,이규승,권진욱,조준형,신광순,김무열,허강준,조명행 충남대학교 수의과대학 동물의과학연구소 1996 動物醫科學硏究誌 Vol.4 No.-

Fosfomycin, a low molecular antibiotic, is to be easily synthesized, therefore to be possibly used in veterinary sectors due to econimic reasons. In this study, we determined the antibacterial activities of fosfomycin against some domestic animal-origin pathogens, and its combined effects with some important antibacterials available. We also compared detection methods of fosfomycin from various measuring instruments. The results obtained through this experiment were as follows: 1. Antibacterial activities of fosfomycin against the pathogens used in this experiment were appeared fairly low. We found the antobacterial activities depanded on the kinds of media and the addition of some material thereins, which suggests the importance of appropriate medium so as to judge the antibacterial activity of fosfomycin. 2. Fosfomycin showed varying antibacterial effects in combination with other antibacterials, which should be taken into consideration when combining other antobacterials especially in the clinical settings. Of the combined antivacterials, fosfomycin had synergistic effects in combination with amoxicillin but antagonistic effects with oxytetracyline. 3. Conventional detection methods using HPLC, GC and spectrophotometer were not appropriate to measure fosfomycin. Capillary electrophoresis by the way of the indirect ultraviolet detection method was good enough to detect fosfomycin in the range of expected concentration in tissues, with the limit of quantitation (LOQ) of 1.25 ㎍/㎖. We recommend the eletrophoresis method could be used to detect fosfomycin, thereby being able to set the optimal dosage for animals and providing the measures in relation with the residual concentration in the meat.

돼지에서 정맥, 근육 그리고 경구 투여시의 enrofloxacin의 약물동태학

윤효인,김무열,박승춘,조준형,박병권,이내경,노상석,장범수,신광순,조명행 충남대학교 수의과대학 동물의과학연구소 1996 動物醫科學硏究誌 Vol.4 No.-

In order to characterize pharmacokinetic profiles according to route of a new enrofloxacin salt form (Enrotil®), it was given to 4 healthy pigs via oral (p.o.), intramuscular (i.m.) or intravenous (i.v.) administrations at a dose rate of 5 ㎎/㎏ body weight. Enrofloxacin (ENFX) in serum was detected by bioassay using E. coli BE1186 as a test organism. The biological elimination half-lives (t_1/2(β)) of ENFX were 6.76±0.99 h (i.v.), 7.16±2.30 h (i.m.) and 11.45±3.90 h (p.o.), Volume of distribution (Vd) of enrofloxacin was 2.20±0.31 L/㎏ (i.v.), 2.52±0.60 L/㎏ (i.m.) and 1.88±0.33 L/㎏ (i.m.). Mean residence time (MRT) was 8.77±1.26 h after i.v. injection and the maximal concentration time (Tmax) following p.o. and i.m. administration was 0.76±0.09 h and 0.60±0.12 h, indicating a rapid absorption from these routes. Bioavailibility (F) was calculated as 64.1% for p.o. administration and 59.71% for i.m. injections. In summary, the newly formulated enrofloxacin salt form has shown a high water solubility, rapid absorption and large tissue distribution, suggesting a potential antibacterials for oral application on a large scale in veterinary sectors.

새로운 개념의 살충제

윤효인 대한수의사회 1991 대한수의사회지 Vol.27 No.9

아드레날린성 β-수용체에 대한 higemamine의 약리학적 특성

윤효인,장기철,이창업,Yun, Hyo-in,Chang, Ki-churl,Lee, Chang-eop 대한수의학회 1992 大韓獸醫學會誌 Vol.32 No.1

Higenamine is an Aconiti tuber derived compound whose chemical structure is 1-(4'-hydroxybenzyl)-6, 7-dihydroxy-1, 2, 3, 4-tetrahydroisoquinoline containing catechol ring and tetrahydroisoquinoline nucleus in its own structure, both of which are well known to have agonistic effects on adrenergic receptors. Using guinea-pig atria(rich in ${\beta}_1$-receptor) and treachea(rich in ${\beta}_2$-receptor), we studied pharmacological actions of higenamine on these organs with special interest of its relevancy of ${\beta}$-receptor selectivity. In order to further clarify its pharmacological characteristics, the influncences of pretreatment of reserpine or cocaine were also investigated. The results were summarized as follows : 1. Higenamine had remarkable chronotropic, inotropic and bronchodilator effects in guinea-pig spontaneously beating right atria, left atria and trachea, in dose-dependent manners. 2. All of above actions were blocked competitively by propranolol, which shows nonselectivity of higenamine on ${\beta}$-receptor. $pA_2$ values of propranolol against higenamine were 7.93, 7.76 and 8.46 in guinea-pig right atria, left atria and treachea, respectively. 3. Reserpine pretreatment(5mg/kg, ip, 24h) did not show my decrease in pharmacological actions of higenamine, which suggests higenamine has direct action on ${\beta}$-receptor not via catecholamine release. 4. Cocaine pretreatment$(1{\mu}M)$ had no influence on pharmacological actions of higenamine in contrast with nor epinephrine, which suggests there is no neuronal uptake mechanism of higenamine in the studied organ preparations.

Effect of gender on the pharmacokinetics and metabolite formation of sulfamethazine in the rabbit

윤효인,박일현,Yun, Hyo-in,Park, Il-hyun The Korean Society of Veterinary Science 1992 大韓獸醫學會誌 Vol.32 No.1

Sulfamethazine(SMZ)은 수의임상에서 감염증 치료 및 예방목적으로 많이 사용되고 있을 뿐 아니라 가축의 생산성 향상을 위해 남용되고 있는 주요한 항균제의 하나이다. SMZ의 생체내 대사 및 약물동태학적 특성은 동물의 종차에 따라 상이함이 잘 알려져 있으나 주요 실험동물 및 경제동물인 토끼에서 조사된 바는 매우 드물다. 한편 성차에 따른 약물대사의 차이는 rat를 비롯한 여러 동물에서 인정되고 있는데 대체로 숫컷이 암컷에 비해 대사능이 활발한 것으로 알려져 있다. 그러나 산양에서의 SMZ의 대사는 오히려 암컷이 더 활발하다는 보고도 있어, 여러 동물종에서 일률적으로 성차에 따른 약물대사를 설명할 수가 없다. 초식성의 습성을 가지고 있는 토끼에 있어 성차에 따른 SMZ의 대사 및 약물동태학적 특성이 다른 초식성 동물인 산양의 경우와 동일한 경향을 보이는지는 매우 흥미 있다할 것이다. New Zealand White 토끼에 SMZ을 이정맥에 35mg/kg를 주사한 후 미리 정해진 시간에 수거된 혈장 및 뇨(24시간)를 HPLC를 이용하여 분석하여 아래와 같은 약물동태학 및 대사적 특성을 얻었다. 1. 토끼에서의 SMZ의 주요 대사경로는 아세틸화$(N_4AcSMZ)$이었다. 두개의 수산화 대사산물(50HSMZ, $6CH_2OHSMZ$)도 생성되어 수산화 경로가 있음을 확인하였으나 양적인 관심에서 주요하지 않았다. 2. 토끼에서의 SMZ의 각 대사산물의 생성은 암수간의 성차에 따른 차이가 인정되지 않았다. 3. SMZ을 토끼의 이정맥에 투여(35mg/kg)하였을 때의 약물동태학적 특성은 1구1차 지수형 배설형태로 설명이 가능하였으며 암수에 따른 성차가 인정되지 않았다. 4. SMZ는 신속하게 $N_4AcSMZ$로 대사되었으며, $N_4AcSMZ$의 체외배설은 SMZ에 비해 매우 느렸으며 성차에 따른 배설속도의 차이를 인정할 수 없었다. SMZ is one of the most widely used antibacterial agents in veterinary medicine. It is also used as a growth promotant in many species of domestic animals There are marked species differences in its metabolism and pharmacokinetics. However, its pharmacokinetic and metabolism in rabbits. which are ragarded not only as good laboratorty animals hut also as good economical animals in its own, are lacking. Sex-differences in drug metabolism are well recognized in wide range of animal species including rats. Males are known to he more active than females. It is also know that there are Significant differences in the direction of metabolic pathways. But recently, female goats are reported to be more active in the metabolie capacity of SMZ than the other sex by Dutch researchers at Utrecht. Therefore, it is not easy to make general conclusicn of having higher SMZ metal-die capacity in the male compared to the opposite sex in every animal species. In this regard, the study on metabolic pattern of SMZ in rabbits, which are regarded as hervivorous, is of interest because the dietary habbits of rabbit are comparable to thai of goal, NEW Zealand White rabbits of each sex were given SMZ(35mg/kg) as a bolus injection into the marginalean, vein in order to study its pharmacokinetic profiles(using plasma) anc metabolic pattem(24h urine) as specified in the methods anc materials. 1. In the rabbit, the major metabolic pathway of SMZ was the acetylation(the formation of $N_4AcSMZ$). There were hydroxylation pathways(50HSMZ, $6CH_2OHSMZ$) as well, in the metabolism of SMZ in the rabbit, but minor pathways. 2. No sex differences in the metabolic direction of SMZ and its metabolites formation were found from the urinary excreted metabolites of SMZ out of 24h collected urine. 3. The concentration-time curves of SMZ(35mg/kg, iv) in the plasma compartment were fitted to a one-compartment open model when using a computer program(NONLIN). There was also no difference in the pharmacokinetic pattem of SMZ between two sexes. 4. The emergence of $N_4AcSMZ$ metabolized from SMZ was very fast in the plasma of the rabbit The elimination of $N_4AcSMZ$ was prolonged as compared to that of the parent drug Vie found no sex difference in the elimination pattern of $N_4AcSMZ$ in the rabbit.

Rat에서 설파메타진의 대사 및 약물동태학

윤효인,박승춘,박종명,조준형,이문한,Yun, Hyo-in,Park, Seung-chun,Park, Jong-myung,Cho, Joon-hyoung,Lee, Mun-han 대한수의학회 1995 大韓獸醫學會誌 Vol.35 No.4

We used rats as the experimental animal for the elucidation of metabolic patterns and pharmacokinetic profiles of SMZ in the rat, by use of the urine and plasma from predetermined intervals, respectively. Information herefrom would give some insight into species differences and sex differences in the metabolism and pharamcokinetics of drugs, at least SMZ in particular. Results would be summarized as follows: 1. There were two hydorxy metabolites(5-hydroxysulfamethazine and 6-hydroxyethylsulfamethazine) and an acetyl derivative($N_4$-acetyl sulfamethazine) in the 24h-collected urine, on confirmation with each standard materials. There were also two unknown metabolites therein. 2. In the viewpoint of quantitative aspect, $N_4$-acetylsulfamethazine was the largest, hence it is assumed that the acetyl pathway is the major one in the metabolism of SMZ in the rat. 3. As regards sex difference in the rat, the male had more metabolic capacity than the female in metabolism of SMZ. 4. The concenteration-time curves of sulfamethazine(20mg/kg, po) in the plasma compartment were fitted to a one-compartment open model by use of a computer program(NONLIN). 5. There were significant differences(P<0.05) in the pharmacokinetics of sulfamethazine between two sexes in the rat, with higher disposition rate in the male. 6. The emergence of $N_4AcSMZ$ metabolized from SMZ was fast in the plasma of the rat. Half-life of $N_4AcSMZ$ was also. significantly different(P<0.05) between two sexes, suggesting differences in the eliminatory capacity of $N_4AcSMZ$.

양파외피 추출물의 어류 병원성세균에 대한 항균성 검색

윤효인,배순이 충남대학교 수의과대학 동물의과학연구소 1998 動物醫科學硏究誌 Vol.6 No.-

The objective of the study was to evaluate the antibacterial activity of onion shells, which are discarded as industrial wastes, against fish pathogenic bacteria using various extractants such as water, ethanol, ethyl acetate and butanol. Water onion extracts did not show any antibacterial activity in the tested bacteria but butanol onion extracts showed antibacterial activity against Bacillus subtilis and Escherichia coli BE 1186. Ethyl acetate and ethanol onion extracts showed antibacterial activity for all the test bacteria. Ethanol, an edible stuff, was possible to use as an extractant of onion shells in industrial process to make marketed products. We further studied the effects of heat and PH on the antibacterial activity of ethanol onion extract against fish pathogenic bacteria. Heating did not change the antibacterial activity of the ethanol extract. However, ethanol extract showed a decreasing antibacterial activity toward alkaline (pH 11). These results indicate that the ethanol onion extracts is suitable for use as supplementary antibacterials.

Higenamine의 Guinea pig 기관 평활근 이완작용

윤효인,장기철,홍성근,이창업,Yun, Hyo-in,Chang, Ki-chorl,Hong, Seong-geun,Lee, Chang-eop 대한수의학회 1987 大韓獸醫學會誌 Vol.27 No.1

Higenamine, a benzyltetrahydroisopuinoline analog isolated from aconite tuber, has potent isotropic action. Recent studies suggest it may have beta receptor agonistic property in that its inotropic action is blocked by propranolol in isolated rabbit heart. However, no study has been carried out on other organs than heart. Higenamine is expected to have pharmacological actions on smooth muscle on the ground that it has catecholamine moiety and tetrahydrosioquinoline nucleus in its chemical structure, both of which are well known to have smooth muscle relaxation effects. Therefore present study was aimed at determining whether higenamine has bronchodilating effect in isolated guinea pig trachea smooth muscle rich in adrenergic beta receptor and if any, it has agonistic effect on beta receptor. The results were summarized as follows : 1. Higenamine had remarkable bronchodilating effect in guinea pig tracheal smooth muscle in a dose-dependent manner. 2. Bronchodilator effect of higenamine in isolated guinea pig tracheal smooth muscle was blocked competitively by propranolol. The $pD_2$ value of higenamine in isolated guinea pig tracheal smooth muscle was 5.65 and the $pA_2$ value of propranolol against higenamine in the same preparation was 7.97.

Thermodynamic properties and structural geometry of KMgCl3·6H2O single crystals

윤효인,임애란 한국자기공명학회 2015 Journal of the Korean Magnetic Resonance Society Vol.19 No.3

The thermodynamic properties and structural geometry of KMgCl3·6H2O were investigated using thermogravimetric analysis, differential scanning calorimetry, and nuclear magnetic resonance. The initial mass loss occurs around 351 K (=Td), which is interpreted as the onset of partial thermal decomposition. Phase transition temperatures were found at 435 K (=TC1) and 481 K (=TC2). The temperature dependences of the spin–lattice relaxation time T1 for the 1H nucleus changes abruptly near TC1. These changes are associated with changes in the geometry of the arrangement of octahedral water molecules.

고추 작물 중 oxytetracycline 및 oxolinic acid의 반감기 산출

윤효인,류송희,이지원,윤지현,송아름 한국농약과학회 2022 한국농약과학회 학술발표대회 논문집 Vol.2022 No.4