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신규 Carbapenem 유도체 CRB 529 및 CRB 550의 생체내 항균효과와 약물동태의 비교
김준겸(Joon Kyum Kim),민관기(Kwan Kee Min),이주몽(Ju Mong Lee),이홍우(Hong Woo Lee),김정우(Jung Woo Kim) 대한약학회 1995 약학회지 Vol.39 No.4
1-beta-Methyl carbapenem-2-substituted pyrrolidine derivatives, CRB 529 and CRB 550, were synthesized as investigational carbapenem derivatives. It has been reported that the in vitro antibacterial activities of the compounds against G(+) and G(-) bacteria were almost the same or more effective than those of imipenem (IPM) and meropenem (MEPM), and also showed better in vivo efficacy than MEPM and imipenem/cilastatin (IPM/CS) against representative G(-) organisms, P. aeruginosa and MRSA organisms, S. aureus. The antibacterial activities, pharmacokinetics and protective efficacy of IPM/CS and CRB 529 and CRB 550 were conducted after subcutaneous or intravenous administration to mice and rats. The pharmacokinetic parameters of CRB 529 and CRB 550 in mice were as follows; the observed maximal serum concentrations (CMAX) following I.V. administration were 87.5 and 101mcg/ml for CRB 529 and CRB 550, respectively, and 63.6mcg/ml for IPM/CS. The half-lives (t1/2) were 14.0 and 12.0 min for CRB 529 and CRB 550, respectively, and 14.8 min for IPM/CS. In rats, CMAX after I.V. administration were 74.0 and 91.8mcg/ml for CRB 529 and CRB 550, respectively, and 41.2mcg/ml for IPM/CS. The tissue levels of CRB 529 and CRB 550 and IPM/CS after I.V. administration at a dose of 20mg/kg decreased by the following order; lung, heart, kidney, liver and spleen for CRB 529, kidney, liver, lung, heart and spleen for CRB 550 and kidney, lung, liver, heart, spleen and brain for IPM/CS. In systemic infection, CRB 529 and CRB 550 showed excellent efficacies against P. aeruginosa and S. aureus (MRSA) at a dose of 5mg/kg. The PD50s were 0.80, 0.36mg/kg for CRB 529 and CRB 550, respectively, and 3.22mg/kg for IPM/CS against P. aeruginosa. The corresponding values against S. aureus (MRSA) were 76.0, 55.3mg/kg for CRB 529 and CRB 550, respectively, and 146mg/kg for IPM/CS. In local infection, the antibacterial activities of CRB 529 and CRB 550 were more effective than those of IPM/CS against intrarenal infection with E. coli and P. aeruginosa and also showed as effective as IPM/CS against respiratory tract infection with E. coli and P. aeruginosa at a dose of 5mg/kg.
신규 Carbapenem 유도체 CRB 529, 535, 538, 545, 550의 시험관내 항균력 평가
민관기(Kwan Kee Min),김준겸(Joon Kyum Kim),이홍우(Hong Woo Lee),김정우(Jeong Woo Kim) 대한약학회 1995 약학회지 Vol.39 No.3
The in vitro antibacterial activities of new carbapenem, CRB 529, 535, 538. 545 and 550 with meropenem and imipenem were compared. CRB 529, 535, 538, 545 and 550 proved to have a broad antibacterial spectrum. Its in vitro activity against standard 20 strains was almost the same as that of imipenem and slightly higher than that of meropenem. However, against clinical isolated P. aeruginosa, CRB 529. 535, 538, 545 and 550 showed significantly higher activity than imipenem, and also CRB 529, 535, 538, 545 and 550 showed almost the same activity than imipenem and meropenem against 82 clinical isolated strains including S. aureus (MRSA), S. aureus (MSSA), E. faecalis, E. facium, E. coli, P. aeruginosa, K. pneumonia, P. mirabiris, P. stuartii, M. morganii, C. freundii, E. cloacae, S. marcescens and A. calcoaceticus var. anitratus. The stability of CRB 529, 535, 538, 545 and 550 against porcine renal dehydropeptidase-I (DHP-I) was 10 folds higher than that of imipenem and was 3 folds higher than that of meropenem.
흰쥐 hepatocyte에서 알파 및 베타 아드레날린 수용체의 자극에 의한 글리코겐분해에 있어서 칼슘과 니페디핀의 작용
이영희(Young Hee Lee),김준겸(Joon Kyum Kim),김미영(Mie Young Kim) 대한약학회 1988 약학회지 Vol.32 No.6
The effects of calcium and calcium antagonist, nifedipine on the adrenergic receptor- stimulated glycogenolysis were investigated in isolated rat hepatocytes. The hepatic glycogenolysis induced by alpha-adrenergic receptor stimulation depended on calcium ions, and beta-adrenergic activation was unrelated to calcium ions. Nifedipine decreased the alpha-adrenergic agonist-induced glucose release significantly and the decrease was depended on calcium ions. The glucose release induced by beta-adrenergic agonist was not inhibited by nifedipine.
신규 캄토테신계 항암제 CKD-602의 약물동태 : 분포, 대사 및 배설
이주몽(Ju Mong Lee),이준희(Jun Hee Lee),김준겸(Joon Kyum Kim),신희종(Hee Jong Shin),이형기(Hyung Ki Lee),이상준(Sang Joon Lee),홍청일(Chung Il Hong) 大韓藥學會 1998 약학회지 Vol.42 No.4
The distribution, metabolism and excretion of CKD-602{20(S)-7-[2-(N-Isopropylamino)ethyl]camptothecin HCI), a new camptothecin derivative, were investigated in rats after a single administration of CKD-602. 1. The tissue levels of CKD-602 given to mice by the intravenous route at a dose of 20mg/kg were the highest in intestine, followed in descending order by kidney, liver, stomach,lung, heart, spleen and plasma. The concentrations of CKD-602 after 24hrs decreased to less than 2% of the peak level in most tissues except the skin. The urinary and fecal excretion of CKD-602 were 47.6% and 44.4% of the administered dose, respectively, with 0.7% remaining in the rinse. 2. After administration of CKD-602 at 10mg/kg in rats, metabolism of this compound was examined in plasma, urine, and feces. The plasma samples were collected for 24hr, urinary and fecal samples for 72hr. While any peak of CKD-602 in HPLC chromatograms was not detected from plasma and urine it was detected in feces (peaks, 9.8 min). However, additional peak area was about 0.5% of the peak area of parent CKD-602. Therefore, CKD-602 may be eliminated with the parent form and rarely metabolized in the body. 4. After I.v. administration of CKD-602 at 10mg/kg in rats, urinary and fecal excretions were examined for 72hrs post dose period. 87% of total urinary excretion of CKD-602 was excreted within 8hr after administration, 53%, and 32% of total fecal excreted amounts were determined in 0-24 hr and 24-48hr periods, respectively. The total excretion amounts of CKD-602 into urine and feces were 94% of the administered dose.