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흰쥐의 배양 간세포를 이용한 세포독성시험에 있어서 뉴트랄레드 및 젖산 탈수소효소법의 비교
이경태,서성훈 ( Kyung Tae Lee,Seong Hoon Seo ) 한국약제학회 1995 Journal of Pharmaceutical Investigation Vol.25 No.4
The acute cytotoxicities of chloroquine sulfate, propranolol, ascorbic acid, acetylsalicylic acid and acrylamide on cultured adult rat hepatocytes were evaluated by the use of LDH leakage and NR uptake test. On the basis of IC_(50) values, the rank order of cytotoxicities of these drugs in both tests was chloroquine sulfate > propranolol > acetylsalicylic acid > ascorbic acid. The IC_(50) of LDH test was very similar to that of NR uptake test. Thus, we concluded that both tests are reliable and sensitive methods in detecting toxicity in adult cultured rat hepatocytes.
이경태,서성훈,Lee, Kyung-Tae,Seo, Seong-Hoon 한국약제학회 1995 Journal of Pharmaceutical Investigation Vol.25 No.4
The acute cytotoxicities of chloroquine sulfate, propranolol, ascorbic acid, acetylsalicylic acid and acrylamide on cultured adult rat hepatocytes were evaluated by the use of LDH leakage and NR uptake test. On the basis of $IC_{50}$ values, the rank order of cytotoxicities of these drugs in both tests was chloroquine sulfate > propranolol > acetylsalicylic acid > ascorbic acid. The $IC_{50}$ of LDH test was very similar to that of NR uptake test. Thus, we concluded that both tests are reliable and sensitive methods in detecting toxicity in adult cultured rat hepatocytes.
새로운 백금 착체(II) 화합물의 흰쥐 혈장에서 대사체 확인
김종환,조요나,노영수,서성훈,정지창,장성구,이규홍,이주한,이경태,Kim, Jong-Whan,Jo, Yo-Na,Rho, Young-Soo,Seo, Seong-Hoon,Jung, Jee-Chang,Chang, Sung-Goo,Lee, Kyoe-Heung,Lee, Joo-Han,Lee, Kyung-Tae 한국약제학회 1998 Journal of Pharmaceutical Investigation Vol.28 No.3
KHPC-002 $[(trans-l-diaminocyclohexane-bis-l,2(diphenylphosphinoethane)platinum)\;{\cdot}2NO_3]$ and $KHPC-006[(cis-diaminocyclohexane-bis-1,2(diphenylphosphinoethane)platinum)\;{\cdot}2NO_3]$ were synthesized as candidates for third platinum antitumor agent. Before their pharmacokinetic study, we optimized the analytical condition with HPLC and identified the major metabolites in the rat plasma. HPLC analysis by $C_{18}$ reverse-phase column showed that standard peak of both compounds appeared rapidly at around 1 minutes, whereas metabolites of KHPC-002 and KHPC-006 which were extracted from plasma after single I.V. administration in rats or incubation for 24 hr at $37^{\circ}C$ showed retention time of $10{\sim}11$ minutes. These metabolites were identified as the major compound by Matrix Associated Laser Deposition/Ionization (MALDI), which only lose the 2 molecules of $NO_3$. Based on these results, we suggest that the major metabolites of KHPC-002 and KHPC-006 were [trans-l-diamino-cyclohexane-bis-l,2(diphenylphosphinoethane)platinum] and [cis-diaminocyclohexane-bis-l.2(diphenylphosphinoethane)platinum], respectively.
박재훈,김종환,김주일,김승조,서성훈,이경태,Park, Jae-Hoon,Kim, Jong-Hwan,Kim, Joo-Il,Kim, Seung-Jo,Seo, Seong-Hoon,Lee, Kyung-Tae 한국약제학회 1997 Journal of Pharmaceutical Investigation Vol.27 No.1
This laboratory has recently reported the solubility and in vivo absorption enhancement of diclofenac sodium by ${\beta}-cyclodextrin$ complexation. The acute gastroduodenal mucosa injury provoked by administration of 34 mg/kg and 68 mg/kg of a diclofenac sodium (DS) and equivalent dose of new formulation [diclofenac sodium-beta-cyclodextrin complexation$(DS-{\beta}-CD)$] was evaluated and compared. Microscopic examinations, performed after 18-hrs treatment, demonstrated that $DS-{\beta}-CD$ was less gastrolesive than DS. The drop in gastrophy after a single dose of the assigned drug was considerably greater for DS than for $DS-{\beta}-CD$, which registered similar values to control. Since gastrophy is an expression of the anatomy-functional integrity of the gastric barrier, the results indicate that $DS-{\beta}-CD$ exerts less direct acute damage on the gastric mucosa. Therefore, when administered short-term, $DS-{\beta}-CD$ appears to be less gastrolesive than the standard DS formulation.
레니텍<sup>®</sup> 정(말레인산 에날라프릴, 10 mg)에 대한 에나레이스 정의 생물학적 동등성
조성희,하용화,홍성제,서성훈,류재환,김동현,이경태,Cho, Sung-Hee,Ha, Yong-Hwa,Hong, Sung-Je,Seo, Seong-Hoon,Rew, Jae-Hwan,Kim, Dong-Hyun,Lee, Kyung-Tae 한국약제학회 2003 Journal of Pharmaceutical Investigation Vol.33 No.3
The purpose of the present study was to evaluate the bioequivalence of two enalapril maleate tablets, $Renitec^{TM}$ (MSD Korea Ltd.) and $Enalace^{TM}$ (Welfide Korea Ltd.), according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty-four normal male volunteers, $22.33{\pm}2.55$ year in age and $66.54{\pm}8.30$ kg in body weight, were divided into two groups and a randomized $2{\times}2$ cross-over study was employed. After two tablets containing 10 mg of enalapril maleate per tablet were orally administered, blood was taken at predetermined time intervals and concentrations of enalapril in plasma were determined using LC-MS-MS. Pharmacokinetic parameters such as $AUC_t,\;C_{max}\;and\;T_{max}$ were calculated and ANOVA test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t,\;and\;C_{max}$ untransformed $T_{max}$. There were no sequence effects between two formulations in these parameters. The 90% confidence intervals for the log transformed data were acceptance range of log0.8 to log1.25$(e.g.,\;log1.02{\sim}log1.14\;and\;log1.03{\sim}log1.19\;for\;AUC_t\;and\;C_{max},\;respectively)$. The major parameters, $AUC_t,\;and\;C_{max}$, met the criteria of KDFA for bioequivalence indicating that $Enalace^{TM}$ tablet is bioequivalent to $Renitec^{TM}$ tablet.
당귀와 천궁 및 시호의 병용 경구 투여에서 흰쥐 혈중 Decursinol 농도의 비교 검토
박노정,김남재,이경태,서성훈,Park, Roh-Jeong,Kim, Nam-Jae,Lee, Kyung-Tae,Seo, Seong-Hoon 한국생약학회 2001 생약학회지 Vol.32 No.1
This study was performed to elucidate the influence on the plasma decursinol concentration after administration of combined decursin and Cnidii Rhizoma or decurisin and Bupleuri Radix extracts in comparison with single decursin administration. The identification of decursinol isolated from Angelica gigas was carried out by GC/MS and the concentration of decursinol in the plasma after oral administration was determined by HPLC. The value of area under the plasma concentration (AUC) and the maximal concentration (Cmax) of decursinol after administration of methanol and ether Angelicae Gigantis Radix extract was higher than those of single decursin-treated group. It was also found that the AUC and the Cmax of decursinol after combined administration with decursin and Cnidii Rhizoma were higher than those of decursin administration, whereas those of combined with decursin and Bupleuri Radix was lower. Moreover, the studies were performed with decursinol only or with combined decursinol and Cnidii Rhizoma/Bupleuri Radix, both of combined treatment increased the plasma decursinol concentrations compared with decursinol-treated group in rats. On the basis of these results, it is concluded that co-existing substances or co-administration with other drugs may influence the plasma levels of decurisinol after oral administration.
디클로페낙나트륨 디클로페낙나트륨과 β - 시클로덱스트린 포접물의 흰쥐 위 점막 손상 비교
박재훈,김종환,김주일,김승조,서성훈,이경태 ( Jae Hoon Park,Jong Hwan Kim,Joo Il Kim,Seung Jo Kim,Seong Hoon Seo,Kyung Tae Lee ) 한국약제학회 1997 Journal of Pharmaceutical Investigation Vol.27 No.1
N/A This laboratory has recently reported the solubility and in vivo absorption enhancement of diclofenac sodium by β-cyclodextrin complexation. The acute gastroduodenal mucosa injury provoked by administration of 34 ㎎/㎏ and 68 ㎎/㎏ of a diclofenac sodium (DS) and equivalent dose of new formulation [diclofenac sodium-beta-cyclodextrin complexation(DS-β-CD)] was evaluated and compared. Microscopic examinations, performed after 18-hrs treatment, demonstrated that DS-β-CD was less gastrolesive than DS. The drop in gastrophy after a single dose of the assigned drug was considerably greater for DS than for DS-β-CD, which registered similar values to control. Since gastrophy is an expression of the anatomy-functional integrity of the gastric barrier, the results indicate that DS-β-CD exerts less direct acute damage on the gastric mucosa. Therefore, when administered short-term, DS-β-CD appears to be less gastrolesive than the standard DS formulation.
양이온교환수지복합체에 의한 페닐프로판올아민염산염의 제조 및 평가
김인규(In Kyu Kim),이경태(Kyung Tae Lee),서성훈(Seong Hoon Seo),김종국(Chong Kook Kim),김동현(Dong Hyun Kim),노영수(Young Soo Rho) 한국약제학회 1999 Journal of Pharmaceutical Investigation Vol.29 No.4
This study was prepared to develop the sustained release dosage form of phenylpropanolamine hydrochloride (PPA) by complexation with cation exchange resin(CER). The PPA-CER complex was confirmed by differential scanning calorimetry(DSC) thermogram, indicating a relative shift of an endometric peak of PPA to higher temperature. The loading efficiency was increased as the amount of PPA was increased as well as the time of fractional exchange was advanced as the temperatures were increased. Loading efficiency, fractional exchange, reaction rate constant and activation energy were highly dependent on the temperature and drug : resin ratio. The optimal ratio of PPA and resin was estimated to be 10:10 for the sustained release.