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SB-31ⓡ 의 일반약리작용 ( General Pharmacology of SB-31ⓡ )
공재양(Jae Yang Kong),박우규(Woo Kyu Park),천혜경(Hyae Gyeong Cheon),권경자(Kyoung Ja Kwon),윤여생(Yeo Saeng Yoon),신화섭(Hwa Sup Shin) 한국응용약물학회 1997 Biomolecules & Therapeutics(구 응용약물학회지) Vol.5 No.4
General pharmacological effects of SB-31^R the extracts of Pulsatilla koreana, were investigated in mice, rats and guinea-pigs. Intravenous injection of SB-31 (3 and 6 ml/kg) produced almost no effect on central nervous system; no effects on the general symptom and behaviors of mice, spontaneous locomotor activity, pentobarbital-induced sleeping time, rotarod performance, electroshock and pentylenetetrazole-induced seizures, acetic acid-induced writhing and normal body temperature in mice. SB-31 showed little effects on the spontaneous movement of the isolated ileum and contraction induced by agonists in isolated ileum, suggesting no influence on autonomic nervous system. Administration of SB-31 also did not show any effect on blood pressure in conscious rats. However, a slight decrease in heart rate was observed at high doses (6 and 10 ml/kg) of SB-31 in conscious rats. Similarly, a slight increase in respiratory rate was observed at 6 ml/kg of SB-31 in anesthetized rats. SB-31 did not produce any effect at the dose of 3 ml/kg, but showed a tendency to increase the urinary volume at 6 ml/kg, and produced a decrease in urinary excretions of Na^+ and K^+ at 6 ml/kg. However, transport capacity within the gastrointestinal tract and the secretion of the gastric juice were not influenced by 6 ml/kg of SB-31. In conclusion, these results suggest that SB-31 did not produce any acute effects on the central nervous system, autonomic nervous system, respiratory and circulatory systems, digestive system and kidney function at the dose of below 3 ml/kg.
세팔로스포린 3′-퀴놀론의 물리화학적 성질, 안정성 및 체내약물동태
나성범,공재양,김완주,지웅길 충남대학교 약학대학 의약품개발연구소 1993 藥學論文集 Vol.9 No.-
A cephalosporin with an aminothiazolylmethoxyimino-type side chain at the 7 position and bicyclic quinolone dithicarbamate at the 3' position was synthesized. It has broad and potent antivacterial activity in vitro. The antibacterial spectrum reflects contributions of both the cephalosporin moiety and the quinolone moiety. Thus, this compound was named DACD implying a dual-action cephalosporin derivative. In this paper, the physicochemical properties (lipid-water partition, pKa), stability and pharmacokinetics of DACD were determined and compared with cefotaxime 3'-norfloxacin dithiocarbamate (CENO). Stability tests were studied in pH 1.20, 6.80 and 8.00 buffers and in the presence of AB type human plasma, rat liver homogenate and its β-lactamase. The pharmacokinetic paramaters of DACD were evaluated in mice after a single intravenous dose of 40 ㎎/㎏. The results are as follows. The lipid-water partition coefficient of DACD was higher than that of CENO. The calculated pKa values of CENO and DACD, were 6.82±0.03, 7.53±0.21, respectively. In the hydrolysis test, half-lives (t^1/2) of CENO and DACD was 66.0 hr and 80.0 hr in pH 6.80 buffer, 190 hr and 91.4 hr in pH 8.00 buffer. CENO and DACD were rapidly hydrolyzed in human plasma and in rat liver homogenate. Half-lives (t_1/2) of CENO and DACD were 1.29 hr and 1.15 hr in human plasma, 0.62 hr and 0.71 hr rat liver homogenate. In β-lactamase stability test, CENO and DACD were very stable to the β-lactamase obtained from three different strains. Half-life (t_1/2) and areas under the curve (AUC) in mice were 2.33 hr and 15.97 (㎎·h/I), respectively.
세팔로스포린 3'-퀴놀론의 물리화학적 성질, 안정성 및 체내약물동태
나성범,공재양,김완주,지웅길 대한약학회 1993 약학회지 Vol.37 No.6
A cepfialosporin with an aminothiazoiylmethoxyimino-type side chain at the 7 position and bicyclic quinolone dithicarbamate at the 3' position was synthesized. It has broad and potent antivacterial activity in vitro. The antibacterial spectrum reflects contributions of both the cephalosporin moiety and the quinolone moiety. Thus, this compound was named DACD implying a dualaction cephalosporin derivative. In this paper, the physicochemical proper-ties (lipid-water partition, pKa), stability and pharmacokinetics of DACD were determined and compared with cefotaxime 3'-norfloxacin dithiocarbamate (CENO). Stability tests were studied in pH 1.20, 6.80 and 8.00 buffers and in the presence of AB type human plasma, rat liver homogenate and its .betha.-lactamase. The pharmacokinetic parameters of DACD were evaluated in mice after a single intravenous dose of 40 mg/kg. The results are as follows. The lipid-water partition coefficient of DACD was higher than that of CENO. The calculated pKa values of CENO and DACD, were 6.82$\pm$0.03, 7.53$\pm$0.21, respectively. In the hydrolysis test, half-lives (t$^{1/2}$) of CENO and DACD was 66.0 hr and 80.0 hr in pH 6.80 buffer, 190 hr and 91.4 hr in pH 8.00 buffer. CENO and DACD were rapidly hydrolyzed in human plasma and in rat liver hornogenate. Half-lives (t$_{1/2}$ of CENO and DACD were 1.29 hr and 1.15 hr in hyman plasma, 0.62 hr and 0.71 hr rat liver homogenate. In $\beta$-lactamase stability test, CENO and DACD were very stable to the .betha.-lactamases obtained from three different strains. Half-life (t$_{1/2}$) and areas under the curve (AUC) in mice were 2.33 hr and 15.97 (mg.h/1), respectively.