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유영효(Young Hyo Yu),박남준(Nam Jun Park),김병오(Byung O Kim),최문정(Moon Jung Choi),심점순(Jeom Soon Shim),강태충(Tae Chung Kang),이재욱(Jae Wook Lee),김대영(Dae Young Kim) 대한약학회 1994 약학회지 Vol.38 No.3
In vitro and in vivo antibacterial activities of DWQ-013(1-cyclopropyl-6,8-difluoro-7-(3-methylthiomethylpyrrolidinyl)-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid), a new fluoroquinolone antibacterial agent, were compared with those of ciprofloxacin, sparfloxacin and ofloxacin against aerobic and anaerobic standard strains and clinical isolates. DWQ-013 had a broad spectrum and potent antibacterial activity against Gram-positive and Gram-negative bacteria. The antibacterial activity of DWQ-013 against Staphylococcus aureus was equal to that of sparfloxacin(SPFX) and superior to those of ciprofloxacin(CPFX). The antibacterial activity against Gram-negative bacteria was slightly lower than those of ciprofloxacin and sparfloxacin. MIC of DWQ-013 against Pseudomonas aeruginosa(0.781- 1.563mcg/ml) was usually equal to that of sparfloxacin(O.781mcg/ml) and was inferior to that of ciprofloxacin(O.098mcg/ml). The number of viable cells was decreased rapidly after addition of DWQ-013 at concentration of 1-2 folds of MIC.
라니티딘을 함유한 새로운 위장질환 치료용 의약조성물(DWP302)의 약물동태
김영만(Young Man Kim),김동오(Dong O Kim),김영도(Young Do Kim),남권호(Kweon Ho Nam),이성원(Sung Won Lee),이주헌(Joo Hun Lee),김학형(Hak Kyoung Kim),유영효(Young Hyo Yu),박명환(Myung Hwan Park) 대한약학회 1993 약학회지 Vol.37 No.5
The pharmacokinetics of DWP302, a new combined ranitidine preparation in rats and dogs was studied using HPLC. DWP302 was composed of ranitidine, sucralfate and tripotassium dicitrato bismuthate. Especially, this study was focused on the possibilities that the concomitant administration of either sucralfate or TDB may affect the absorption of orally administered ranitidine. Ranitidine and DWP302 were orally administered to rats at a dose of ranitidine 10mg/kg. Several rats showed the biphasic peak of plasma concentration. AUCs0-8 of ranitidine and DWP302 group were found to be 1040 +/- 109 and 945 +/- 124ng.hr/ml, respectively, and there was no significant difference between both AUCs. In a cross-over study for dogs, Cmax t1/2 beta and total AUC of ranitidine group were found to be 625.8 +/- 86.7ng/ml, 2.80 +/- 0.28 hr and 1688 +/- 127ng.hr/ml, and those of DWP302 group were 562.6 +/- 120.9ng/ml, 3.05 +/- 0.30 hr and 1673 +/- 123ng.hr/ml, respectively. There was no significant difference between those parameters, but Tmax of DWP302 group (1.69 +/- 0.31 hr) was significantly different from ranitidine group (1.13 +/- 0.26 hr). The results suggest that either sucralfate or TDB may affect the lag-time or rate of absorption of ranitidine but not the extent of absorption.
재조합 인간 상피세포성장인자(DWP401)의 흰쥐에서의 약물동태
정주영(Joo Young Chung),고여욱(Yeo Wook Koh),남권호(Kwon Ho Nam),조재열(Jae Youl Cho),박승국(Seung Kook Park),유영효(Young Hyo Yu),김재환(Jae Hwan Kim),한건(Kun Han),박명환(Myung Hwan Park),심창구(Chang Koo Shim) 대한약학회 1997 약학회지 Vol.41 No.3
Pharmacokinetics of DWP401, a recombinant human epidermal growth factor (rhEGF), was studied using radioimmunoassay (RIA) and 125I-DWP401 in rats. When DWP401 was administered i.v. at doses of 50 and 500 mcg/kg, the plasma DWP401 disappeared biiexponentially with terminal half life of 4.7 and 92.8 min. The Cmax and Tmax after s.c. administration of ti at doses of 50 and 500 mcg/kg were determined to be 23.6 and 17.5 ng/ml at 50 mcg/kg, and 261.4 ng/ml and 36.8 min, respectively. Both the total urinary and biliary recoveries of intact DWP401 2343 very low (<0.4%), probably due to its extensive degradation in the body. the concentration ratio of DWP401 between the organ and plasma decreased especially in the liver and kidney as the dose and time after the dose increased. For example, the liver/plasma and kidney/plasma concentration ratio of DWP401 at 2.5 min after i.v. doses of 50 mcg/kg were comparable and much larger than unity. But, the ratio at 2.5 min after i.v. doses of 500mcg/kg was much larger in the kidney that in than in the liver. These results suggest that the systemic administration of DWP401 might be subject to rapid and extensive clearance from circulation within several hour after main distrbution to liver and kidney.
신규 플르오로퀴놀론계 항생물질인 DWP20373 의 흰쥐 및 개에서의 체내동태와 조직분포
심점순(Jeom Soon Shim),유영효(Young Hyo Yu),남권호(Kweon Ho Nam),박명환(Myung Hwan Park),공재양(Jae Yang Kong),조재열(Jae Youn Cho),한승희(Seung Hee Han),김병오(Byoung O Kim),김지연(Ji Yeon Kim),유은숙(Eun Sook Yoo),정대영(Dae Young 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.2
The pharmacokinetics and tissue distribution of DWP20373, a novel fluoroquinolone, were examined in rats and beagle dogs after a single intravenous and oral administration. Analysis of DWP20373 in plasma, tissue, and urine was performed by both HPLC and microbiological assay. The plasma drug concentration declined biexponentially both rats and beagle dogs. In the rats, the terminal drug elimination half-life (t_(½β)) was 64 min (IV) and 57 min (PO) by bioassay, and 76 min (IV) and 77 min (PO) by HPLC. Whereas, in beagle dogs, t_(½β) was 196 min (IV) and 350 min (PO). The volume of distribution at steady-state (Vd_(ss)) was 811 ml/kg (bioassay) and 2061 ml/kg (HPLC) in rats, and 2738 ml/kg (bioassay) in beagle dogs. The total body clearance (Cl₁) of DWP20373 was 10 ml/min/kg (bioassay) and 7 ml/min/kg (HPLC) in rats, and 11 ml/min/kg (bioassay) in beagle dogs. The extent of bioavailability after oral administration was 49% (bioassay) and 67% (HPLC) in rats, and 84% (bioassay) in beagle dogs. The 24-h urinary recovery, measured by bioassay, was 2.7% after oral dosing and 5.5% after intravenous dosing in rats. Serum protein binding ratio determined at 2 ㎍/㎖ was 78%. This drug was also distributed in tissues in the decreasing order of liver, kidney, spleen, lung, heart, and muscle determined at 30 min after oral administration.
7-[3-히드록시-(4-메틸티오 또는 4-메틸티오메틸)피롤리디닐]퀴놀린-3-카르복실산의 합성과 항균작용
이재욱,손호정,이규삼,유영효,윤길종,Lee, Jae-Wook,Son, Ho-Jung,Lee, Kyu-Sam,Yu, Young-Hyo,Yoon, Geal-Jung 대한약학회 1994 약학회지 Vol.38 No.6
A number of 7-[3-hydroxy-(4-methylthio or 3-methylthiomethyl)pyrrolidinyl]quinoline-3-carboxylic acids were synthesized by condensation of 7-fluoro substituted quinoline-3-carboxylic acid with 3-hydroxy-4-methylthiopyrrolidine or 3-hydroxy-4-methylthiomethylpyrrolidine. The in vitro antimicrobial activity of them were tested against twenty species of Gram-positive or Gram-negative microorganisms. It showed remarkable antibacterial activity, particularly against Gram-positive microorganisms. Among those 1-cyclopropyl-5-amino-6,8-difluoro 7-(3-hydroxy-4-methylthiomethylpyrrolidinyl)-1,4-dihyd ro-4-oxo-3-quinolinecarboxylic acid(12d) and 1-cyclopropyl-6-fluoro-8-methoxy-7-(3-hydroxy-4-methylthiometby1pyrrolinyl)-1,4-dihydro-4-oxo-3-quinolinocarboxylic acid(12g) showed the most potent in vitro antibacterial activity, and 12d showed better antibacterial activity against MRSA compared to ciprofloxacin and sparfloxacin.
7-[(3-메틸티오 또는 3-메틸티오메틸)-3-피롤리닐]퀴놀론-3-카르복실산의 합성과 항균작용
이재욱,손호정,이규삼,유영효,김대영,Lee, Jae-Wook,Son, Ho-Jung,Lee, Kyu-Sam,Yu, Young-Hyo,Kim, Dae-Young 대한약학회 1994 약학회지 Vol.38 No.5
A number of 7-[(3-methylthio or methylthiomethyl)-3-pyrrolinyl] quinolone-3-carboxylic acids were synthesised by condensation of 7-fluoro substituted quinolone-3-carboxylic acid with 3-methylthio-3-pyrroline or 3-methylthiomethyl-3-pyrroline. The in vitro antimicrobial activity of them were tested against twenty species of Gram-positive or Gram-negative microorganisms. It showed remarkable antibacterial activity, particularly against Gram-positive microoganisms. Among those 1-cyclopropyl-6,8-difluoro-7-[(3-methylthiomethyl) -3-pyrrolinyl]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid(12a) and 1-cycl opropyl-6-fluoro-8-chlore-7-[(3-methylthiomethyl)-3-pyrrolinly]-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid(12b) showed the most potent in vitro antibacterial activity.
신규 플루오로퀴놀론계 DWP20367 의 흰쥐 및 개에서의 체내동태와 조직분포
심점순(Jeom Soon Shim),유영효(Young Hyo Yu),남권호(Kweon Ho Nam),박명환(Myung Hwan Park),공재양(Jae Yang Kong),조재열(Jae Youl Cho),한승희(Seung Hee Han),김병오(Byoung O Kim),정대영(Dae Young Jeong),이재욱(Jae Wook Lee),손호정(Ho Jun 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.3
The pharmacokinetics and tissue distribution of DWP20367 (1-cyclopropyl-6-fluoro-8-chloro-7-(2,7-diazabicyclo[3,3,0]oct-4-ene-7-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid), a novel fluoroquinolone, were examined in rats and beagle dogs after a single intravenous and oral administration. Analysis of DWP20367 in plasma, tissue, and urine was determined by both HPLC and microbiological assay (bioassay). The plasma concentration-time curves of the drug in rats and beagle dogs were biexponentially declined. The terminal halflife (t_(½β)) of the drug in rats was about 60.1 ±7.3 min (i.v.) and 61.3 ±12.4 min (p.o.) in bioassay, and 86.3 ±19.8 min (i.v.) and 50.9±14.9 min (p.o.) in HPLC. In beagle dogs, half-life of the drug determined by bioassay was about 121.8±6.2 min (i.v.) and 111.0±7.6 min (p.o.). The volume of distribution at steady-state (Vd_(ss)) was 243.8±74.1 ml/kg (bioassay) and 339.2±84.3 ml/kg (HPLC) in rats, and 1587.5±536.9 ml/kg (bioassay) in beagle dogs. The total body clearance (Cl₁,) of DWP20367 was 3.4±0.4 ml/min/kg (bioassay) and 2.4±0.4 ml/min/kg (HPLC) in rats, and 12.3±1.0 ml/min/kg (bioassay) in beagle dogs, respectively. The extent of bioavailability after oral administration was 89.1 %(bioassay) and 79.9% (HPLC) in rats, and 78.7% (bioassay) in beagle dogs. Urinary recovery (24-h) assayed by bioassay was 0.7% (p.o.) and 1.2% (i.v.) in rats, and 0.8% (p.o.) and 1.0% (i.v.) in beagle dogs. In rats, 24-h fecal recovery determined by bioassay was 11.2% (p.o.) and 0.1% (i.v.). Rat and human serum protein binding ratios at 2 ㎍/ml were about 90∼91%. This drug determined by bioassay was also distributed by the order of liver, kidney, lung, heart, spleen and muscle 30 min after oral administration.
신규 합성 퀴놀론계 항생물질(DWQ-013)의 일반 약리 작용 -중추신경계에 대한 작용-
임승욱(Seung Wook Lim),김영만(Young Man Kim),유영효(Young Hyo Yu),이재욱(Jae Wook Lee) 대한약학회 1994 약학회지 Vol.38 No.5
The general pharmacological effects of DWQ-013, a new synthetic quinolone antibacterial agent, were examined on the central nervous system in experimentral animals and the following results were obtained. Drug interaction of DWQ-013 with theophylline, fenbufen and nonsteroidal antiinflammatory drugs was also examined. DWQ-013 decreased touch escape effect on the general behavior and decreased body temperature at a concentration of 1000 mg/kg in mice. But DWQ 013 had no effect on the locomotor activity, rotarod perfomance and traction test in mice. Furthermore, DWQ-013 increased pentobarbital-induced sleeping time and affected the onset time in acetic acid-induced writhing test in mice. DWQ-013 reduced onset time and death time on strychnine-induced convulsions and death time on pentylenetetrazole-induced convulsions at a concentration of 1000mg/kg in mice. But, the drug had no effect on the electroshock. DWQ-013 did not interact with fenbufen and any other NSAIDs but it did interact with theophylline. From these results, it could be suggested that DWQ-013 had less pharmacological effect than other quinolones on the central nervous system.
위장질환 치료용 의약조성물 ( DWP 301 ) 의 일반약리작용
심점순(Jeon Soon Shim),박남준(Nam Jun Park),유영효(Young Hyo Yu),임승욱(Seung Wook Lim),염제호(Je Ho Yeom),김영만(Young Man Kim),장병수(Byeong Su Jang),연제덕(Je Duk Yeon),김병오(Byung O Kim),강진석(Jin Seok Kang),유은주(Eun Joo Yu) 한국응용약물학회 1994 Biomolecules & Therapeutics(구 응용약물학회지) Vol.2 No.4
The general and some pharmacological actions of DWP 301 were investigated in animals and the following results were obtained. In central nervous system, DWP 301 had no effects on the pentobarbital induced anaesthesia, rotarod test, traction test, analgesic action, anticonvulsant action in mice and body temperature in rat. But DWP 301 showed a little decrease of locomotor activity at a dose of 3,000 mg/kg. From these results, DWP 301 was considered to have little pharmacological effect on the central nervous system. Furthermore, DWP 301 had no influences on the normal blood pressure and heart rate. DWP 301 showed no effect on the isolated guinea pig ileum, trachea, right atrium, and nonpregnant rat uterus. But, in the isolated guinea pig vas deference, DWP 301 had showed inhibitory effect on the contractions produced by norepinephrine. DWP 301 showed rise of gastric juice pH and decrease of urine volume. Also, DWP 301 had no effect on the gastrointestinal motility and blood aggregation. From these results, it is concluded that the general pharmacological effect of DWP 301 are similar to or weaker than M and AGA.
남석우(Suk Woo Nam),박승희(Seung Hee Park),유세근(Se Geun Yu),서동완(Dong Wan Seo),김형식(Hyung Sik Kim),이병무(Byung Mu Lee),심점순(Jeon Soon Shim),유영효(Young Hyo Yu),박명환(Myung Hwan Park),이향우(Hyang Woo Lee) 한국응용약물학회 1994 Biomolecules & Therapeutics(구 응용약물학회지) Vol.2 No.3
The acute toxicity of DWP305 (Ursodeoxycholic acid : Silymarin : Fursulthiamine : Riboflavin tetrabutyrate=1 : 1 : 0.1 : 0.05) was evaluated in both sexes of Sprague-Dawley rats, 6 weeks old by the oral route of administration. DWP305 was not considered to induce any toxic effect on the rats in mortalities, clinical findings, body weights and gross findings. It is suggested that LD_(50) value in rats would be above 5 g/㎏ in the oral administration. Subacute toxicity of DWP305 was examined in Sprague-Dawley rats. Four groups of rats were administered orally at doses of 0, 0.32, 0.8, and 2.0 g/㎏/day of DWP305 for one month. Any significant toxic clinical symptom was not observed in the treated rats during the experimental period. Macroscopic examination on the organs of tested animals showed no abnormal findings. On autopsy, no significant changes were found in organs examined. Maximum tolerated dose of DWP305 for the rat was estimated to be above 2 g/㎏ in this study.