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Kim Gwan-Young,Kim Jin-Ho,Lee Taeho,Bae Byoung-Chan,Baik Hyejeong,김태헌,Kim Junsik,Kang Dong Wook,Kim Ju Hee,Kim Dahan,Cho Hea-Young,김대덕 한국약제학회 2022 Journal of Pharmaceutical Investigation Vol.52 No.1
Purpose The aim of this work was to evaluate a new polylactic acid microsphere depot formulation (Leuprolide Depot 3 M) prepared by a water-in-oil-in-water emulsion/solvent evaporation method. Methods The physical properties of the microspheres, including particle size and drug encapsulation efficiency, were characterized. The accelerated and long-term in vitro release profiles were examined. Pharmacokinetic and pharmacodynamic studies were conducted in male beagle dogs after a single subcutaneous injection of the microspheres at 11.25 mg/animal leuprolide acetate by measuring the plasma leuprolide and testosterone levels, respectively. Results Leuprolide Depot 3 M was spherical in shape with a smooth surface and showed an average diameter of 17.83 μm and a drug loading content of 7.58% (w/w). These properties were comparable to those of Lupron Depot 30 mg, a commercial product. In vitro release of leuprolide at 37 °C from both formulations was sustained for up to 126 days and showed a similarity factor (f2) of 51.0. In the pharmacokinetic study, the plasma leuprolide concentration after subcutaneous injection of Leuprolide Depot 3 M or Lupron Depot 30 mg remained at approximately 0.1 ng/mL for up to 98 days. There were no significant differences in the pharmacokinetic parameters between the two formulations. Moreover, the plasma testosterone level was effectively suppressed to less than 0.5 ng/mL until the end of the evaluation. Conclusion These results suggest that Leuprolide Depot 3 M and Lupron Depot 30 mg are expected to have comparable efficacy profiles in clinical settings, which should be confirmed in further clinical studies.
Kim Tae-Kwang,Lee Jeong-Eun,Jeong Kyuho,Baek Min-Jun,Kim Dahan,Jeon Jun-Young,Lee Sangyoung,김대덕 한국약제학회 2024 Journal of Pharmaceutical Investigation Vol.54 No.1
Purpose The objective of this study was to design a fixed-dose combination (FDC) tablet with minimal interaction of valsartan, amlodipine, rosuvastatin and ezetimibe to improve medication compliance in patients with hypertension and dyslipidemia and to evaluate its feasibility for development through in vitro dissolution test and pharmacokinetic assessment in humans. Methods The formulation was designed as a bilayer FDC tablet to minimize the interaction of the four drugs based on the results of drug‒drug interaction evaluations in which the drugs were mixed and exposed at 50 °C for 4 weeks. The FDC tablet was then evaluated against the reference listed drug (RLD) products, Exforge® tablet 10/160 mg and Rosuzet® tablet 10/20 mg, through in vitro dissolution studies and in vivo pharmacokinetic studies in humans. Results The in vitro release profiles of valsartan, rosuvastatin and ezetimibe were similar to those of the RLD products. Although the Cmax of ezetimibe in the FDC tablet was slightly higher, there were no significant differences in the area under the plasma drug concentration–time curve (AUC). There were also no notable discrepancies in the Cmax and AUC of the other three drugs. Furthermore, the absence of statistically significant variations in the frequency of adverse events and the lack of serious adverse reactions indicate a comparable safety profile between the FDC and RLD tablets. Conclusion The feasibility of bilayer FDC tablet formulation to improve medication compliance in patients with hypertension and dyslipidemia was demonstrated.
Lee, Hyeyoung,Oh, Il-Nam,Kim, Jungeun,Jung, Dahan,Cuong, Nguyen Phu,Kim, Younmi,Lee, Jongcheol,Kwon, Oha,Park, Sang Un,Lim, Yongpyo,Kim, Byungjoo,Park, Jong-Tae Elsevier 2018 FOOD SCIENCE AND TECHNOLOGY -ZURICH- Vol.90 No.-
<P><B>Abstract</B></P> <P>In previous study, red Chinese cabbages which satisfy the morphological characteristics of traditional Chinese cabbages were developed by crossing Chinese cabbage and red cabbage, with subsequent backcrossing. In this study, we evaluated the phenolic compound profiles of two newly developed red-phenotype Chinese cabbages in comparison with three typical cultivars. Anthocyanidins (cyanidin), phenolic acids (caffeic acid, <I>p</I>-coumaric acid, ferulic acid, and sinapic acid), and flavonols (quercetin and kaempferol) were identified and quantified by HPLC, LC/MS and LC/MS/MS analyses. The new cultivars contained significantly increased levels of phenolic compounds, except for kaempferol. Their contents drastically varied by sowing season. The spring-sown red Chinese cabbages contained significantly higher levels of phenolic acids (11,530 and 12,437 μg/g dry wt.) and cyanidin (1830 μg/g dry wt.) but lower levels of flavonols than their fall-sown counterparts. Correlation analysis exhibited a significant positive correlation between cyanidin and phenolic acids but a negative correlation between phenolic acids and flavonols in red Chinese cabbages. Principal component analysis could differentiate red Chinese cabbages and typical cultivars with different sowing seasons based on their phenolic compound profiles. This study provides information regarding the selection of appropriate Chinese cabbage cultivars rich in phenolic compounds that may benefit human health.</P> <P><B>Highlights</B></P> <P> <UL> <LI> Newly developed red Chinese cultivars contained significantly increased levels of phenolic compounds. </LI> <LI> Spring-sown red Chinese cabbages contained higher levels of phenolic acids and cyanidin than their fall-sown counterparts. </LI> <LI> Developed red cultivars can be used as raw materials for further industrial application. </LI> </UL> </P>
Kim, Cheol-Eui,Park, Sangjune,Eom, Dahan,Seo, Boram,Lee, Phil Ho American Chemical Society 2014 ORGANIC LETTERS Vol.16 No.7
<P>A method for synthesis of substituted pyrroles has been developed. 1-Sulfonyl-1,2,3-triazoles generated from terminal alkynes gave α-imino rhodium carbene complexes, which when reacted with alkenyl alkyl ethers afforded substituted pyrroles. The method can be efficiently applied to a one-pot sequential reaction starting from terminal alkynes.</P><P><B>Graphic Abstract</B> <IMG SRC='http://pubs.acs.org/appl/literatum/publisher/achs/journals/content/orlef7/2014/orlef7.2014.16.issue-7/ol500718s/production/images/medium/ol-2014-00718s_0008.gif'></P><P><A href='http://pubs.acs.org/doi/suppl/10.1021/ol500718s'>ACS Electronic Supporting Info</A></P>
Eom, Dahan,Mo, Juntae,Lee, Phil Ho,Gao, Zhiming,Kim, Sunggak WILEY‐VCH Verlag 2013 European Journal of Organic Chemistry Vol.2013 No.3
<P><B>Abstract</B></P><P>A synthetic method was developed for the preparation of vinyl sulfides and vinylamines from arylalkynyl phenyl sulfides and sulfonamides. Under mild conditions, a catalytic intramolecular hydroarylation reaction was carried out in the presence of FeCl<SUB>3</SUB> and AgOTf (OTf = trifluoromethanesulfonate) in 1,2‐dichloroethane. A variety of 1,2‐dihydronaphthalenes, 2<I>H</I>‐chromenes, and 1,2‐dihydroquinolines containing a phenylsulfenyl or <I>N</I>‐phenyl‐<I>N</I>‐tosyl group on the sp<SUP>2</SUP>‐hybridized benzylic carbon were prepared in good to excellent yields. The present method could be extended to the preparation of dihydropyrano[2,3‐<I>g</I>]chromenes through a twofold Fe‐catalyzed hydroarylation by a selective 6‐<I>endo</I> mode.</P>