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로나졸락 초산에스테르 및 로나졸락 알지니네이트의 생물약제학적 연구
이완하,함광수,양재헌 한국약제학회 1991 Journal of Pharmaceutical Investigation Vol.21 No.2
Two new prodrugs of lonazolac, lonazolac acetic acid ester and lonazolac argininate, were prepared and examined for physicochemical properties and biopharmaceutical characteristics. The prodrugs were stable in solid state and lonazolac argininate showed higher dissolution rate than lonazolac-Ca in both artificial gastric and intestinal juices. These prodrugs have higher analgegic effect than that of lonazolac-Ca in mice, and increased anti-inflammatory activities in rats. In addition, ulcerogenic effects and acute toxicity of these prodrugs were lower than those of lonazolac-Ca. Lonazolac acetic acid ester showed larger area under the plasma concentration-time curves (AUC) than that of lonazolac. Therefore, it was suggested that these prodrugs of lonazolac have advantages over lonzolac-Ca for not only enhanced bioavailability but also decreased ulcerogenic and toxic effects.
李琬夏,智雄吉,咸光洙 成均館大學校 1982 論文集 Vol.31 No.-
The absorption of salicylamide from the everted intestine of a rabbit in combination with ephedrine, and salicylamide alone and chlropheniramine, was examined. This examination was taken to method of cannulated everted sac technique and used to the Crane and Wilson appartus. The results were as follows: 1. The absorption of salicylamide in the everted intestine were incresed by the compound of ephedrine. 2. Also, the compound of chlorpheniramine was increased to the absorption of salicylamide. 3. Moreover, the compounds of chlorpheniramine and ephedrine were increased to the absorption of salicylamide. 4. In the region of intestine, the absorption of salicylamide showed most increased absorption in the middle region of intestine. 5. The intestinal transfer rate of salicylamide was 2.29 and the intestinal transfer rate of salicylamide of compound with chlorpheniramine and ephedrine was 3.42.
오우용(Woo Yong Oh),주상섭(Sang Sup Jew),박형근(Hyeung Geun Park),함광수(Kwang Su Ham),조장섭(Jang Sup Cho),이선미(Sun Mee Lee) 한국응용약물학회 2000 Biomolecules & Therapeutics(구 응용약물학회지) Vol.8 No.3
(R)-JG-381, a R form of alkylglycidic acid derivative, was examined for mutagenicity in the reverse mutation test on bacteria, chromosomal aberration test on cultured mammalian cells and micronucleus test in mice. In the reverse mutation test on bacteria using Salmonella typhimurium strain TA98, TA100, TA102, TA1535, TA1537 with or without a metabolic activation system (S9 mix), (R)-JG-381 did not affect the revertant colonies but significantly increased revertant colonies in one test strain, TA98, compared with the vehicle control. In the chromosomal aberration (CA) test using cultured Chinese Hamster Lung fibroblast(CHL) cells, the number of aberrant cells was not increased in the presence or absence of S9 mix at concentration of the (R)-JG-381 0.025㎕/㎖ to 0.1 ㎕/㎖, compared with vehicle control. In the micronucleus (MN) test, micronucleated polychromatic erythrocytes in the (R)-JG-381-treated mice were not different from those of the vehicle-treated mice.
SD 랫드에서 ( R ) - JG - 381 의 단회경구독성시험
오우용(Woo Young Oh),주상섭(Sang Sup Jew),함광수(Kwang Su Ham),이상호(Sang Ho Lee),김종춘(Jong Chun Kim),박형근(Hyeung Geun Park),조장섭(Jang Sup Cho),이선미(Sun Mee Lee) 한국응용약물학회 2002 Biomolecules & Therapeutics(구 응용약물학회지) Vol.10 No.1
N/A A single administration toxicity of (R)-JG-381 was studied in Sprague-Dawley rats of both sexes. In this study, rats were administered orally with dose of 50, 100, 200, 400 and 800 ㎎/㎏ of (R)-JG-381. We daily examined number of deaths, clinical signs, body weights and gross findings for 14 days after (R)-JG-381 administration. When we administered different doses of 100, 200, 400 and 800 ㎎/㎏, we found 5, 3, 5 and 5 male rats and 1, 4, 4 and 5 female rats dead within 1 day after administration, respectively. Some clinical signs(decrease of locomotor activity, decreased respiration rate, lacrimation, prone position) were observed during the experimental period. Our findings suggest that oral LD_50s(95% confidence limit) for male and female rats are 93.8 ㎎/㎏ (28.8∼161.6 ㎎/㎏) and 166.3 ㎎/㎏ (89.1∼284.8 ㎎/㎏), respectively.
오우용(Woo Yong Oh),이상호(Sang Ho Lee),주상섭(Sang Sup Jew),박형근(Hyeung Geun Park),함광수(Kwang Su Ham),조장섭(Jang Sup Cho),이선미(Sun Mee Lee) 한국응용약물학회 2001 Biomolecules & Therapeutics(구 응용약물학회지) Vol.9 No.1
N/A General pharmacological properties of (R)-JG-381 were examined in laboratory animals to investigate its safety profile. Administration of (R)-JG-381 (50 and 100 mg/kg) in mice and rats had no effects of general behaviors, central nervous system of the animals in test systems of pentobarbital-induced sleeping time, writhing syndromes induced by 0.7% acetic acid, chemo-shock produced by pentylenetetrazole, and, however, had mild effects on motor coordination. Heart rate and blood pressure were not changed by (R)-JG381 treatment. (R)-JG-381 also showed mild effects on intestinal propulsion and gastric secretion. These results suggest that (R)-JG-381 dose not exert serious pharmacological effects.
오우용(Woo Young Oh),이상호(Sang Ho Lee),김형진(Hyung Jin Kim),주상섭(Sang Sup Jew),박형근(Hyeung Geun Park),함광수(Kwang Su Ham),조장섭(Jang Sup Cho),이선미(Sun Mee Lee) 한국응용약물학회 2001 Biomolecules & Therapeutics(구 응용약물학회지) Vol.9 No.3
N/A The single oral toxicity of JG-381 was studied in Sprague-Dawley rats of both sexes. In this study, rats were administrated orally with dosages of 267, 400, 600, 900 and 1350 ㎎/㎏ of JG-381. We daily examined number of deaths, clinical signs, body weights and gross findings for 14 days after JG-381 administration. When we administered different doses of 267, 400, 600, 900 and 1350 ㎎/㎏, we found 1, 4, 4, 5 and 5 male rats died and 3, 5, 4, 5 and 5 female rats died within 1 day after administration, respectively. Some clinical signs (decrease locomotor activity, salivation, soft stool, prone position, lacrimation, crouching position, convulsion, ataxic gait, incontinence of urine) were also observed during the experimental period. Our findings suggest that oral LD_(50s) (95% confidence limit) for male and female rats are 327 ㎎/㎏ (270∼396 ㎎/㎏) and 250 ㎎/㎏ (236∼264 ㎎/㎏), respectively.