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최재묵(Jae-Mook Choi),이성학(Sung-Hak Lee),김일환(Il-Hwan Kim),박지은(Jie-Eun Park),김덕열(Deog-Yeor Kim),노현정(Hyun-Jung Noh),김택로(Taekrho Kim),최광도(Do-Gwang Choi),김영훈(Young-Hoon Kim),김진완(Jin-Wan Kim),장준환(Joon-Hwan Jan 한국독성학회 2004 Toxicological Research Vol.20 No.1
Safety pharmacological properties of CJ-11555, an anti-cirrhotic agent, were investigated in experimental animals and in vitro test system. CJ-11555 had no effects on normal body temperature in rats, motor coordination, chemoshock induced by pentetrazol, electric shock induced by electric shocker and writhing syndromes in mice at dose levels of 100, 300 and 1,000 mg/kg. CJ-11555 inhibited intestinal activity and prolonged hexobarbital-induced sleeping time in mice at the dose level of 1,000 mg/kg. CJ-11555 affected on general activity and behaviour tests in SD rats, such as lacrimation, ptosis, piloerection, decreased body tone, abnormal dispersion within the cage, diarrhoea, red colored faeces, slight hypothermia and decreased grooming, at the dose level of 1,000<br/> mg/kg in rats. CJ-11555 was effected on cardiovascular and respiratory system in anesthetized beagle dogs, such as tachycardia, increase of mean blood pressure and decrease of PR interval, decrease of respiratory rate and minute volume, at dose levels of 10 and 30 mg/kg. However, these effects were also observed in vehicle treated anesthetized beagle dogs. In in vitro experiments, CJ-11555 inhibited agonists (histamine, acetyl-choline or BaCl2) induced contraction of isolated guinea-pig at the concentration of 30×10-6 M. CJ-11555 was weekly inhibited hERG channel current at concentrations of 10 and 30×10-6 M, and IC50 was estimated to be higher than 30×10-6 M. Based on these results, it was concluded that CJ-11555 affected on cardiovascular and respiratory system, general activity and behaviour and hexobarbital-induced sleeping time at the dose level of 1,000 mg/kg and contraction of the smooth muscle and hERG channel current at the concentration of 30×10-6 M.
최재묵(Jae Mook Choi),이성학(Sung Hak Lee),김일환(Il Hwan Kim),박지은(Jie Eun Park),김덕열(Deog Yeor Kim),노현정(Hyun Jung Noh),김택로(Taekrho Kim),최광도(Do-Gwang Choi),김영훈(Young Hoon Kim),김진완(Jin Wan Kim),장준환(Joon Hwan Jan 한국독성학회 2004 Toxicological Research Vol.20 No.2
Safety pharmacological properties of CJ-11555, an anti-cirrhotic agent, were investigated in experimental animals and in vitro test system. CJ-11555 had no effects on normal body temperature in rats, motor coordination, chemoshock induced by pentetrazol, electric shock induced by electric shocker and writhing syndromes in mice at dose levels of 100, 300 and 1,000 mg/kg. CJ-11555 inhibited intestinal activity and prolonged hexobarbital-induced sleeping time in mice at the dose level of 1,000 mg/kg. CJ-11555 affected on general activity and behaviour tests in SD rats, such as<br/> lacrimation, ptosis, piloerection, decreased body tone, abnormal dispersion within the cage, diarrhoea, red colored faeces, slight hypothermia and decreased grooming, at the dose level of 1,000mg/kg in rats. CJ-11555 was effected on cardiovascular and respiratory system in anesthetized beagle dogs, such as tachycardia, increase of mean blood pressure and decrease of PR interval, decrease of respiratory rate and minute volume, at dose levels of 10 and <br/> 30mg/kg. However, these effects were also observed in vehicle treated anesthetized beagle dogs. In in vitro experiments, CJ-<br/> 11555 inhibited agonists (histamine, acetyl-choline or BaCl2) induced contraction of isolated guinea-pig at the concentration of 30x10-6 M. CJ-11555 was weekly inhibited hERG channel current at concentrations of 10 and 30x10-6 M, and IC50 was estimated to be higher than 30x10-6 M. Based on these results, it was concluded that CJ-11555 affected on cardiovascular and respiratory system, general activity and behaviour and hexobarbital-induced sleeping time at the dose level of 1,000 mg/kg and contraction of the smooth muscle and hERG channel current at the concentration of 30x10-6 M.
박지은(Jie-Eun Park),이성학(Sung-Hak Lee),최재묵(Jae-Mook Choi),김일환(Il-Hwan Kim),김덕열(Deog-Yeor Kim),노현정(Hyun-Jung Noh),김택로(Taekrho Kim),김영훈(Young-Hoon Kim),임지웅(Lim Jee Woong),김진환(Jin-Wan Kim),장준환(Jun-Hwan Chan 한국독성학회 2004 Toxicological Research Vol.20 No.2
To evaluate the genotoxicity of CJ-11555, an anti-cirrhotic agent, the reverse mutation test, chromosomal aberration test and in vivo micronucleus test in rats were performed. In the reverse mutation test, the treatment of CJ-11555 at doses of 33.3, 100, 333, 1000, 3330 and 5000 mg/plate with and without S9 did not induce mutagenicity in Salmonella typhimurium TA98, TA100, TA1535, TA1537, and Escherichia coli ( E. coli) WP2 uvrA. In chromosomal aberration test, CJ-11555 did not induce structural a chromosomal aberration in Chinese hamster ovary (CHO) cells with and without metabolic activation at all doses. In micronucleus test, CJ-11555 did not induce any statistically significant increases in micronucleated polychromatic erythrocyte (MNPCE) at doses of 500, 1000, and<br/> 2000 mg/kg. These results suggest that CJ-11555 might not have a mutagenic potential under the conditions in this study.
박지은(Jie-Eun Park),이성학(Sung-Hak Lee),최재묵(Jae-Mook Choi),김일환(Il-Hwan Kim),김덕열(Deog-Yeor Kim),노현정(Hyun-Jung Noh),김택로(Taekrho Kim),김영훈(Young-Hoon Kim),임지웅(Lim Jee Woong),김진완(Jin-Wan Kim),장준환(Jun-Hwan Chan 한국독성학회 2004 Toxicological Research Vol.20 No.1
To evaluate the genotoxicity of CJ-11555, an anti-cirrhotic agent, the reverse mutation test, chromosomal aberration test and in vivo micronucleus test in rats were performed. In the reverse mutation test, the treatment of CJ-11555 at doses of 33.3, 100, 333, 1000, 3330 and 5000 mg/plate with and without S9 did not induce mutagenicity in Salmonella typhimurium TA98, TA100, TA1535, TA1537, and Escherichia coli ( E. coli) WP2 uvrA. In chromosomal aberration test, CJ-11555 did not induce structural a chromosomal aberration in Chinese hamster ovary (CHO) cells with and without metabolic activation at all doses. In micronucleus test, CJ-11555 did not induce any statistically significant increases in micronucleated polychromatic erythrocyte (MNPCE) at doses of 500, 1000, and 2000 mg/kg. These results suggest that CJ-11555 might not have a mutagenic potential under the conditions in this study.
Effects of bile salts on the lovastatin pharmacokinetics following oral administration to rats
Kyunghee, Kim,Hye Sun, Gwak,Inkyung, Yoon,Inkoo, Chun,Nayoung, Lee,Taekrho, Kim 이화여자대학교 약학연구소 2012 藥學硏究論文集 Vol.- No.22
This study aimed to examine the effects of bile salts on pharmacokinetics of lovastatin, which has low bioavailability. Lovastatin solid dispersions were prepared using sodium deoxycholate (NaDC) and sodium glycholate (NaGC) at ratios of 1:19, 1:49, and 1:69. The formulated solid dispersions and control (commercial tablet) were administered to rats and plasma concentrations were determined by a validated LC-MS/MS method. Statistically significant differences were found in C(max), AUC₀₋₁₀, and AUC₀₋∞ values among lovastatin formulations (p < 0.05). NaDC-containing formulations revealed higher bioavailabilities than NaGC-containing solid dispersions at ratios of 1:19 and 1:49. Especially, NaDC-containing formulation at a ratio of 1:19 (NaDC19) showed the highest bioavailability. The AUC (both AUC₀₋₁₀ and AUC₀₋∞) of NaDC19 was statistically higher than control and NaDC69 (p < 0.05). The AUC values decreased as bile salt concentrations increased. Overall, formulations containing bile salts showed higher AUC values than control, even though all formulations did not show significantly higher AUC. In conclusion, the addition of bile salts to lovastatin could enhance drug bioavailabilities. However, too high concentrations of bile salts could decrease bioavailabilities of lovastatin.
Bae, Soo K.,Lee, Shin J.,Kim, Taekrho,Kim, Jin W.,Lee, Inchul,Kim, Sang G.,Lee, Myung G. Wiley Subscription Services, Inc., A Wiley Company 2006 journal of pharmaceutical sciences Vol.95 No.5
<P>Pharmacokinetics and therapeutic effects of oltipraz were evaluated after consecutive (once per day at 30 mg/kg/day for 7 and 14 days) or intermittent (once per week at 100 mg/kg/week for 1–3 weeks) oral administration to rats with liver cirrhosis induced by dimethylnitrosamine. The AUC of oltipraz was significantly greater in cirrhotic rats than controls (890 compared with 270 µg · min/mL) due to impaired liver function in cirrhotic rats. However, the AUC values after consecutive 7 (421 compared with 753 µg · min/mL) and 14 (309 compared with 821 µg · min/mL) days oral administration of oltipraz in cirrhotic rats were significantly smaller than those in respective vehicle-treated cirrhotic rats. Moreover, the AUC values after intermittent 2 and 3 weeks in cirrhotic rats were also significantly smaller than that in 1 week vehicle-treated cirrhotic rats (2370 and 1690 compared with 4760 µg · min/mL). This could be due to induction of CYP isozymes and considerably greater numbers of normal liver cells in cirrhotic rats by oral administration of oltipraz. Improved liver function by oltipraz in cirrhotic rats was proved by liver microscopy; livers are free of significant fibrosis, although evidence of bridging necrosis is still present in many rats. © 2006 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 95:985–997, 2006</P>
Pharmacokinetics of oltipraz in mutant Nagase analbuminemic rats
Bae, Soo K.,Kang, Hee E.,Kang, Min K.,Kim, Jin W.,Kim, Taekrho,Lee, Myung G. Wiley Subscription Services, Inc., A Wiley Company 2006 journal of pharmaceutical sciences Vol.95 No.5
<P>Pharmacokinetic parameters of oltipraz were compared after intravenous (10 mg/kg) and oral (50 mg/kg) administration to control male Sprague–Dawely rats and mutant Nagase analbuminemic rats (NARs). In NARs, the expression and mRNA level of CYP1A2 increased, and oltipraz was mainly metabolized via CYP1A1/2, 2B1/2, 2C11, 201, and 3A1/2 in male rats. Hence, it may be expected that the CL of oltipraz would be significantly faster in NARs. This was proven by the following results. After intravenous administration, the CL of oltipraz was significantly faster in NARs (125% increase) than controls due to significantly greater free fractions (unbound to plasma proteins) of oltipraz (197% increase) and significantly faster CL<SUB>int</SUB> for the disappearance of oltipraz (11.4% increase) in NARs, since oltipraz is an intermediate hepatic extraction ratio drug in rats. The V<SUB>ss</SUB> was significantly larger in NARs (109% increase) and this could be due to significant increase in free fractions of oltipraz in NARs. After oral administration, the AUC of oltipraz was also significantly smaller in NARs (61.9% decrease). This could also be due to significant increase in free fractions of oltipraz and significantly faster CL<SUB>int</SUB> in NARs. However, this was not due to decrease in absorption in NARs. © 2006 Wiley-Liss, Inc. and the American Pharmacists Association J Pharm Sci 95:998–1005, 2006</P>