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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.
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.
간장질환 치료용 의약조성물 ( DWP 305 ) 의 이반약리작용
심점순(Jeom 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),박명환(Myung Hwon Park),연제덕(Je Duk Yeon),김병오(Byung O Kim),강진석(Jin Seok K 한국응용약물학회 1994 Biomolecules & Therapeutics(구 응용약물학회지) Vol.2 No.2
The general and some pharmacological actions of DWP 305 were investigated in animals and the following results were obtained. In central nervous system, DWP 305 had no effects on the pentobarbital induced anaesthesia, locomotor activity, rotarod test, traction test, analgesic action in mice and body temperature in rat. DWP 305 showed no depressive action on convulsion induced by strychnine, electronic shock and pentylenetetrazole. From these results, DWP 305 was considered to have no pharmacological effect on the central nervous system. Furthermore, DWP 305 had no influences on the normal blood pressure and heart rate. In the isolated ileum of guinea pig, DWP 305 inhibited contrastive effects against the acetylcholine (10^(-6)g/㎖), histamine (10^(-6)g/㎖), 5-hydroxytryptamine (10^(-6)g/㎖) and BaCl₂ (10^(-4)g/㎖) at a concentration of 2.15 X 10^(-4)g/㎖ in bath. In the isolated trachea and vas deference, DWP 305 showed no effect on the contractions produced by histamine and norepinephrine, respectively. DWP 305 showed inhibitory effect on the contractions produced by acetylcholine and oxytocin at a concentration of 2.15 X 10^(-4)g/㎖ on the isolated nonpregnant rat uterus. DWP 305 had no effect on the isolated right atrium of guinea pig, bile excretion urine volume, pH, gastrointestinal motility, gastric secretion and blood aggregation.
Formaldehyde 가스 흡입에 의한 마우스의 급성독성 및 소핵 유발성에 관한 연구
김충용,김균,심점순,김용화,노정구,Kim, Choong-Yong,Kim, Kyun,Shim, Jeom-Soon,Kim, Yong-Hwa,Roh, Jung-Koo 한국독성학회 1991 Toxicological Research Vol.7 No.1
The acute and genetic effect of formaldehyde on mice through inhalation route was studied. The Riley's chamber with one stack of cage was used for the exposure and the micronucleus test was performed under unprecedently maximum exposure concentration. LC50's of formaldehyde in mice by whole body exposure for 4 hours were 105.5 ppm with 95% confidence interval of 72.6 ppm and 143.2 ppm for male, and 159.2 ppm with 95% confidence interval of 116.5 ppm and 272.7 ppm for female. Cinicial symptoms by acute exposure were salivation, lacrimation, and abnormal respiration.
플로오로퀴놀론계 항생제인 DWP20373의 in vitro 항균작용
김지연,최문정,한승희,김병오,심점순,정연의,이재욱,유영호,박명환,Kim, Ji-Yeon,Choi, Moon-Jung,Han, Seung-Hee,Kim, Byung-O,Shim, Jeom-Soon,Jung, Yeon-Eui,Lee, Jae-Wok,Yu, Young-Hyo,Park, Myung-Hwan 대한약학회 1996 약학회지 Vol.40 No.3
The in vitro antibacterial activity of a novel fluoroquinolone, DWP20373(1-Cyclopropyl-6-fluoro-8-methoxy-7-(2,7-diazabicyclo[3,3,0]oct-4-ene-7-yl)-1,4-dihydro-4 oxoquino line-3carboxylic acid) was compared with those of ciprofloxacin (CPFX), sparfloxacin (SPFX) and ofloxacin (OFLX). DWP20373 was more active than SPFX and OFLX but was less potent than CPFX against gram-negative bacteria. DWP20373 showed an excellent activity against L-MRSA and H-MRSA ($MlC_{90}=0.781{\sim}1.563{\mu}g/ml$).The activity of DWP20373 decreased moderately in the presence of 5mM $Mg^{2+}$. However, pH and serum had no effect on the activity of DWP20373. DWP20373 possessed a rapid bactericidal activity against gram-positive and gram-negative strains.
신합성 플로로퀴놀론계 항생물질인 DWP20367의 In vitro 항균효과
김지연(Ji Yeon Kim),최문정(Moon Jung Choi),한승희(Seung Hee Han),심점순(Jeom Soon Shim),정연의(Yeon Eui Jung),손호정(Ho Jung Son),이재욱(Jae Wook Lee),유영효(Young Hyo Yu),박명환(Myung Hwan Park) 대한약학회 1997 약학회지 Vol.41 No.2
The in vitro antibacterial activity 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 new broad-spectrum fluoroquinolone, was compared with those of ciprofloxacin (CPFX), sparfloxacin (SPFX) and ofloxacin (OFLX). DWP20367 was showed antibacterial activity much higher than CPFX, SPFX and OFLK against gram-positive bacteria, while it was slightly more superior to quinolones against gram-negative bacteria. DWP20367 was particularly effective against MRSA, and its MlC90 against clinical isolates of methicillin-susceptible S. aureus, low methicillin-resistant S. aureus and high methicillin-resistant S. aureus were 0.098, 0.781 and 1.563 micro g/ml, respectively. Against S. pneumoniae, MIC90 of DWP20367 was 2- to 8-fold higher than those of CPFX. With a view of MIC90, DWP20367 showed slightly more potent activity against P. aeruginosa and E. coli isolates than the control quinolones. DWP20367 activity was not affected by inoculum size and medium pH. But addition of Mg2+, Ca2+ or horse serum (25%) decreased its antibacterial activity. DWP20367 was showed rapidly bactericidal activity within 2 to 4 h, and regrowth was not observed even after 24 h incubation at concentrations near the 4-fold of MIC.
Fluoroquinolone계 항생제인 DWQ-217의 in vitro와 in vivo 항균작용
김병오(Byung O Kim),최문정(Moon Jung Choi),한승희(Seung Hee Han),김지연(Ji Yeon Kim),심점순(Jeom Soon Shim),박남준(Nam Jun Park),손호정(Ho Jung Son),이재욱(Jae Wook Lee),유영효(Young Hyo Yu),박명환(Myung Hwan Park) 대한약학회 1995 약학회지 Vol.39 No.4
The in vitro and in vivo antibacterial activities of DWQ-217 (1-cyclopropyl-6-fluoro-8-chloro-7-(3-amino-4-methylthiomethylpyrrolidinyl)-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid) were compared with those of ciprofloxacin (CPFX) and vancomycin(VCM). DWQ-217 was superior to those of CPFX and VCM against gram positive bacteria. DWQ-217 showed excellent activity against MRSA (MIC of methicilline; >or= 12.5mcg/ml), MIC90=0.013. DWQ-217 possessed strong bactericidal action against gram positive and gram negative strains by MIC/MBC test and killing curve. DWQ-217 and CPFX were administered orally and subcutaneously to mice infected systemically with S. aureus and S. pyogenes. DWQ-217 was >or= 5-16 fold(p.o.) and >or= 3-5 fold(s.c.) more active than CPFX.
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.
C7-이환체 구조를 갖는 새로운 플루오르퀴놀론계 항생제의 in vitro와 in vivo 항균작용
한승희(Seung Hee Han),최문정(Moon Jung Choi),김지연(Ji Yeon Kim),김병오(Byung O Kim),심점순(Jeom Soon Shim),강진석(Jin Seok Kang),손호정(Ho Jung Son),이재욱(Jae Wook Lee),유영효(Young Hyo Yu),박명환(Myung Hwan Park) 대한약학회 1996 약학회지 Vol.40 No.4
The in vitro and in vivo antibacterial activities of a new fluoroquinolone, DWP20364(1-cyclopropyl-5-amino-6,8-difluoro-7-(2,7-diazabicyclo[3.3.0]oto-4-ene-7-yl)-1,4-di-hydro-4-oxoquinoline-3-carboxylic acid) were evaluated in comparison with those of ciprofloxacin(CPFX), sparfloxacin(SPFX) and ofloxacin(OFLX). DWP20364 was more potent than CPFX and OFLX against Staphylococcus spp., Streptococcus spp. and Enterococcus faecium MD8b and it was similarly or slightly less active than CPFX against Escherichia spp. and Pseudomonas spp.. For MRSA and OFLX resistant strains (Staphylococcus spp.(14),Enterococcus spp.(4), Acinetobacter spp.(2), Pseudomonas spp.(9), Klebsiella spp.(2) and Serratia spp.(6)),DWP20364(MICs for 90% of strains,0.025 and 12.5mcg/ml, respectively) was 4 to 32 folds more potent than SPFX and CPFX. The activity of DWP20364 decreased moderately in the presence of 5mM Mg2+. However, various pHs and the concentrations of various serum had no effect on the activity of DWP20364. DWP20364 possessed a bacteriocidal effect at the 1MIC against gram positive and gram negative strains. The protective effect of DWP20364 against systemic infections in mice caused by S. aureus Smith or S. aureus L2379 was superior to that of CPFX and SPFX but it was less active than that of CPFX against infection by P. aeruginosa E-2.
신규 세파로스포린 항생제 DWC-751 의 in vitro 항균작용
심점순,최응칠,최문정,유영효,박남준,김병오 한국응용약물학회 1993 Biomolecules & Therapeutics(구 응용약물학회지) Vol.1 No.2
We compared in vitro antibacterial activity of DWC-751, a new parenteral cephalosporin antibiotic, with those of cefpirome (CPR), cefotaxime (CTX) and ceftazidime (CAZ). DWC-751 showed a broad antimicrobial spectrum against Gram-positive and negative bacteria The antibacterial activity of DWC-751 against Stapylococcus aureus was equal to that of CPR and superior to those of CTX and CAZ. The activity of it against Escherichia coli was more potent than those of CPR, CTX and CAZ. Against Pseudomonas aeruginosa, DWC-751 was slightly inferior to that of CAZ and superior to those of CPR and CTX. The antibacterial activity of DWC-751 was superior to those of CPR, CTX and CAZ against clinical isolates and ofloxacin resistant strains. DWC-751 showed bactericidal action against Escherichia coli at concentrations close to the MIC and induced the formation of filament and burge and lysis of Escherichia coli in a microscopic examination.