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부자(附子) Butanol fraction의 강심작용(强心作用)에 관한 연구(硏究)
홍사악(Hong S.A.),박찬웅(Park C.W.),김명석(Kim M.S.),신상구(Shin S.G.) 대한약리학회 1975 대한약리학잡지 Vol.11 No.1
In Chinese medicine, it is said that Aconiti tuber has cardiotonic, diuretic and analgesic effects. Kim et al reported that alkaloid free part of Aconiti tuber, CHCl<sub>3</sub> insoluble fraction, showed inotropic effect on isolated frog heart and inotropic effect is potenciated by n-butanol fractionation. To investigate the effect of Aconiti tuber butanol fraction on the mechanical and electrical properties of heart, change of active tension, excitability and refractory period of isolated rabbit atrium in the presence of butanol fraction were measured and the comparison with that of ouabain and quinidine was done. The observed results are as follows. 1. 5 X 10<sup>-4</sup>g/ml concentration of Aconiti tuber butanol fraction showed approximately same effect with therapeutic concentration of ouabain on the increment of contractile force, and the effect of 2 X 10<sup>-3</sup>g/ml was greater than that of 1 X 10<sup>-5</sup>g/ml of ouabain. 2. Acceleration of rate of contractile force increment in the presence of Aconiti tuber butanol fraction was greater than in ouabain, and the time to maximum tension was shorter in Aconiti tuber butanol fraction than in ouabain. 3. The excitability of isolated atrium was slightly increased at low concentration of Aconiti tuber butanol fraction, while decreased at higher concentration. 4. Aconiti tuber butanol fraction slightly prolonged refractory period of isolated right atrium at the concentration of 2 X 10<sup>-3</sup>g/ml.
인삼(人蔘)사포닌의 동물행동(動物行動)에 대(對)한 작용(作用)
홍사악(Hong, S.A.),박찬웅(Park, C.W.),김재훈(Kim, J.H.),홍순근(Hong, S.K.),장현갑(Chang, H.K.),김명석(Kim, M.S.) 대한약리학회 1974 대한약리학잡지 Vol.10 No.2
Results of an experiment on the behavior of rats and mice in order to explore the possible pharmacological actions of Panax ginseng upon the central nervous system can be summarized as follows: 1. Spontaneous motor activity. In the case of mice, those groups who were administered 2.5 mg and 5.0mg of ginseng saponin per kilogram of body weight were observed to have increased their activity compared with the control group, while the 50.0 mg and 100.0 mg per kilogram body weight groups demonstrated lower levels of activity, with the peak of activity appearing at 30 minutes after administration of drugs. In the case of rats, those groups of animals who were given injections in the dosage of 2.5 mg, 5.0 mg and 50.0 mg per kilogram body weight demonstrated higher activity than the control group, while the 100.0 mg per kilogram group appeared to have decreased in their activity, with the peak action appearing 30 minutes after the administration of ginseng saponin. The 50.0 mg per kilogram group demonstrated no significant differential. 2. General behavior analysis. In the case of mice, decrease in sleeping component of behavior and increase in the walking and roaring components, compared those with the control group, turned out to be a common phenomenon among the groups who were administered 2.5 mg, 5.0 mg and 50.0 mg of ginseng saponin per kilogram body weight, with the 5.0 mg per kilogram group standing out of all the other groups in terms of their reactions. In the case of rats, ginseng saponin appeared to reduce sleeping component with 2.5 mg, 5.0 mg and 50.0 mg per kilogram body weight groups, while increased the walking and rearing components. It was observed that administratoin of ginseng saponin in a dose of 2.5 mg per kilogram appeared to markedly increase the lying and grooming components of animal behavior. 3. Open-field exploratory behavior. Adminstration of ginseng saponin to mice in doses of 5.0 mg, 50.0 mg and 100.0 mg per kilogram body weight decreased activity, but increased their exploratory behavior. In the case of rats, however, administration of ginseng saponin in the doses of 2.5 mg and 5.0 mg per kilogram body weight markedly increased their activities, while decreased activities with the 50.0 mg per kilogram and 100.0 mg per kilogram groups. The exploratory behavior of rats appeared to have decreased, while grooming increased ramarkably. 4. The above findings from a series of experiment appear to suggest a stimulating effect on the central nervous system when ginseng saponin is administered in small doses, but that larger doses might result in an inhibitory effect, though differential results can be anticipated with modification of experimental conditions.
임정규,홍사악,박찬웅,김명석,서유헌,신상구,김용식,김혜원,이정수,장기철,이상국,장우현,김익상,Lim J.K.,Hong S.A.,Park C.W.,Kim M.S.,Suh Y.H.,Shin S.G.,Kim Y.S.,Kim H.W.,Lee J.S.,Chang K.C.,Lee S.K.,Chang K.C.,Kim I.S. 대한약리학회 1980 대한약리학잡지 Vol.16 No.2
The pharmacological and microbiological studies of Cefoperazone (T-1551, Toyama Chemical Co., Japan) were conducted in vitro and in vivo. The studies included stability and physicochemical characteristics, antimicrobial activity, animal and human pharmacokinetics, animal pharmacodynamics and safety evaluation of Cefoperazone sodium for injection. 1) Stability and physicochemical characteristics. Sodium salt of cefoperazone for injection had a general appearance of white crystalline powder which contained 0.5% water, and of which melting point was $187.2^{\circ}C$. The pH's of 10% and 25% aqueous solutions were 5.03 ana 5.16 at $25^{\circ}C$. The preparations of cefoperazone did not contain any pyrogenic substances and did not liberate histamine in cats. The drug was highly compatible with common infusion solutions including 5% Dextrose solution and no significant potency decrease was observed in 5 hours after mixing. Powdered cefoperazone sodium contained in hermetically sealed and ligt-shielded container was highly stable at $4^circ}C{\sim}37^{\circ}C$ for 12 weeks. When stored at $4^{\circ}C$ the potency was retained almost completely for up to one year. 2) Antimicrobial activity against clinical isolates. Among the 230 clinical isolates included, Salmonella typhi was the most susceptible to cefoperazone, with 100% inhibition at MIC of ${\leq}0.5{\mu}g/ml$. Cefoperazone was also highly active against Streptococcus pyogenes(group A), Kletsiella pneumoniae, Staphylococcus aureus and Shigella flexneri, with 100% inhibition at $16{\mu}g/ml$ or less. More than 80% of Escherichia coli, Enterobacter aerogenes and Salmonella paratyphi was inhibited at ${\leq}16{\mu}/ml$, while Enterobacter cloaceae, Serratia marcescens and Pseudomonas aerogenosa were somewhat less sensitive to cefoperagone, with inhibitions of 60%, 55% and 35% respectively at the same MIC. 3) Animal pharmacokinetics Serum concentration, organ distritution and excretion of cefoperazone in rats were observed after single intramuscular injections at doses of 20 mg/kg and 50 mg/kg. The extent of protein binding to human plasma protein was also measured in vitro br equilibrium dialysis method. The mean Peak serum concentrations of $7.4{\mu}g/ml$ and $16.4{\mu}/ml$ were obtained at 30 min. after administration of cefoperazone at doses of 20 mg/kg and 50 mg/kg respectively. The tissue concentrations of cefoperazone measured at 30 and 60 min. were highest in kidney. And the concentrations of the drug in kidney, liver and small intestine were much higher than in blood. Urinary and fecal excretion over 24 hours after injetcion ranged form 12.5% to 15.0% in urine and from 19.6% to 25.0% in feces, indicating that the gastrointestinal system is more important than renal system for the excretion of cefoperazone. The extent of binding to human plasma protein measured by equilibrium dialysis was $76.3%{\sim}76.9%$, which was somewhat lower than the others utilizing centrifugal ultrafiltration method. 4) Animal pharmacodynamics Central nervous system : Effects of cefoperazone on the spontaneous movement and general behavioral patterns of rats, the pentobarbital sleeping time in mice and the body temperature in rabbits were observed. Single intraperitoneal injections at doses of $500{\sim}2,000mg/kg$ in rats did not affect the spontaneous movement ana the general behavioral patterns of the animal. Doses of $125{\sim}500mg/kg$ of cefoperazone injected intraperitonealy in mice neither increased nor decreased the pentobarbital-induced sleeping time. In rabbits the normal body temperature was maintained following the single intravenous injections of $125{\sim}2,000mg/kg$ dose. Respiratory and circulatory system: Respiration rate, blood pressure, heart rate and ECG of anesthetized rabbits were monitored for 3 hours following single intravenous inje