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연구논문(硏究論文)(재록(再錄)) : 생명과학 ; 생체이용율이 증가된 cyclosporine A 함유 히알우로닉 미립구의 개발
우종수 ( Jong Soo Woo ),박명관 ( Ming Guan Piao ),이동훈 ( Dong Xun Le ),유동성 ( Dong Sung Ryu ),최준영 ( Jun Young Choi ),김정애 ( Jung Ae Kim ),김정훈 ( Jeong Hoon Kim ),진성규 ( Sung Giu Jin ),김대덕 ( Dae Duk Kim ),류원석 ( W 영남대학교 약품개발연구소 2007 영남대학교 약품개발연구소 연구업적집 Vol.17 No.-
Lim, Soo-Jeong,Lee, Jeong-Hoon,Piao, Ming-Guan,Lee, Mi-Kyung,Oh, Dong-Hoon,Hwang, Du-Hyung,Quan, Qi-Zhe,Yong, Chul-Soon,Choi, Han-Gon 대한약학회 2010 Archives of Pharmacal Research Vol.33 No.7
The purpose of this study was to investigate the effect of sodium carboxymethylcellulose (Na-CMC) and fucidic acid on the gel characterization for the development of sodium fucidate-loaded wound dressing. The cross-linked hydrogel films were prepared with polyvinyl alcohol (PVA) and sodium carboxymethylcellulose (Na-CMC) using the freeze-thawing method. Their gel properties such as gel fraction, swelling, water vapor transmission test, morphology, tensile strength and thermal property were investigated. In vitro protein adsorption test and release were performed. Na-CMC decreased the gel fraction and tensile strength of the hydrogels, but increased the swelling ability, water vapor transmission rate, elasticity and porosity of hydrogels. Thus, the wound dressing developed with PVA and Na-CMC was more swellable, flexible and elastic than that with only PVA because of its cross-linking interaction with PVA. However, the drug had a negative effect on the gel properties of hydrogels but there were no significant differences. In particular, the hydrogel composed of 2.5% PVA, 1.125% Na-CMC and 0.2% drug might give an adequate level of moisture and build up the exudates on the wound area. Thus, this sodium fucidate-loaded hydrogel could be a potential candidate for wound dressing with excellent forming.
Choi, Han-Gon,Kim, Ji-Hyun,Li, Dong-Xun,Piao, Ming-Guan,Kwon, Tae-Hyub,Woo, Jong-Soo,Choi, Young-Wook,Yoo, Bang-Kyu,Yong, Chul-Soon The Korean Society of Pharmaceutical Sciences and 2005 Journal of Pharmaceutical Investigation Vol.35 No.5
A rapid and specific high-performance liquid chromatographic method was developed and validated for the simultaneous determination of prostaglandin $E_{1}\;(PGE_{1})$ and prostaglandin $E_{1}$ ethyl ester $(PGE_{1}-EE)$ in hairless mouse skin homogenate. The sample treatment procedure involved deproteination and precipitation by acetonitrile. $PGE_{1}$ and $PGE_{1}-EE$ in supernatant were separated in a reversed-phase C18 column without being interfered by other components present in hairless mouse skin homogenate. 9-Anthracenecarboxylic acid was used as an internal standard. The retention times of $PGE_{1}$, 9-anthracenecarboxylic acid and $PGE_{1}-EE$ were, 4.5, 9.5 and 18.0 min, respectively. The assay showed linearity from 1 to $40\;{\mu}g/ml$ for both $PGE_{1}$ and $PGE_{1}-EE$. Precision expressed as RSD ranged from 2.3 to 14.1 % for $PGE_{1}$ and 1.6 to 11.0% for $PGE_{1}-EE$. Accuracy ranged from 100.5 to 119.6 % for $PGE_{1}$ and from 98.0 to 103.7% for $PGE_{1}-EE$. This method was employed successfully to follow the time course of concentrations of $PGE_{1}$ and $PGE_{1}-EE$ in hairless mouse skin homogenate for stability study.
Enhanced Bioavailability of Poorly Water-Soluble Clotrimazole by Inclusion with β-Cyclodextrin
Balakrishnan Prabagar,Bong-Kyu Yoo,우종수,Jung-Ae Kim,이종달,Ming Guan Piao,최한곤,용철순 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.2
Clotrimazole, a poorly water-soluble antimycotic agent, is a promising agent for various diseases including cancer and sickle cell anemia. To improve the oral bioavailability of clotrimazole, the inclusion compound of clotrimazole with β-cyclodextrin was prepared by spray-drying method and characterized by phase solubility, differential scanning calorimetry and dissolution. Furthermore, the pharmacokinetics after oral administration in rats was then performed compared with clotrimazole powder. The solubility of clotrimazole increased linearly as a function of β-cyclodextrin concentration, resulting in AL type phase solubility diagram which revealed a formation of inclusion compound in a molar ratio of 1:2, with the apparent association constant of 230.2 M-1. The dissolution rate of clotrimazole in the inclusion compound increased greatly compared to clotrimazole powder in pH 7.4 phosphate buffer solution. The inclusion compound gave significantly higher initial plasma concentrations, Cmax and AUC of clotrimazole than did clotrimazole powder when they were administered as suspension form, indicating that the drug from inclusion compound could be more orally absorbed in rats. Thus, the oral bioavailability of clotrimazole could be improved markedly by inclusion complexation, possibly due to an increased dissolution rate.
Prabagar, Balakrishnan,Yoo, Bong-Kyu,Woo, Jong-Soo,Kim, Jung-Ae,Rhee, Jong-Dal,Piao, Ming Guan,Choi, Han-Gon,Yong, Chul-Soon 대한약학회 2007 Archives of Pharmacal Research Vol.30 No.2
Clotrimazole, a poorly water-soluble antimycotic agent, is a promising agent for various diseases including cancer and sickle cell anemia. To improve the oral bioavailability of clotrimazole, the inclusion compound of clotrimazole with ${\beta}$-cyclodextrin was prepared by spray-drying method and characterized by phase solubility, differential scanning calorimetry and dissolution. Furthermore, the pharmacokinetics after oral administration in rats was then performed compared with clotrimazole powder. The solubility of clotrimazole increased linearly as a function of ${\beta}$-cyclodextrin concentration, resulting in A$_L$ type Phase solubility diagram Which revealed a formation of inclusion compound in a molar ratio of 1:2, with the apparent association constant of 230.2 M$^{-1}$. The dissolution rate of clotrimazole in the inclusion compound increased greatly compared to clotrimazole powder in pH 7.4 phosphate buffer solution. The inclusion compound gave significantly higher initial plasma concentrations, Cmax and AUC of clotrimazole than did clotrimazole powder when they were administered as suspension form, indicating that the drug from inclusion compound could be more orally absorbed in rats. Thus, the oral bioavailability of clotrimazole could be improved markedly by inclusion complexation, possibly due to an increased dissolution rate.
( Yi Dong Yan ),( Jun Ho Sung ),( Dong Won Lee ),( Jung Su Kim ),( Eun Mi Jeon ),( Dae Duk Kim ),( Dong Wuk Kim ),( Jong Oh Kim ),( Ming Guan Piao ),( Dong Xun Li ),( Chul Soon Yong ),( Han Gon Choi ) 영남대학교 약품개발연구소 2012 영남대학교 약품개발연구소 연구업적집 Vol.22 No.0
Various amide prodrugs of salicylic acid were synthesised, and their physicochemical propertiesincluding lipophilicity, chemical stability and enzymatic hydrolysis were investigated. In vivo skinpermeation and accumulation profiles were also evaluated using a combination of common permeationenhancing techniques such as the use of a supersaturated solution of permeants in an enhancer vehicle, a lipophilic receptor solution, removal of the stratum corneum and delipidisation of skin. Their capacity factor values were proportional to the degree of carbon-carbon saturation in the side chain. All these amides were highly stable in acetonitrile and glycerine. Amide prodrugs were converted tosalicylic acid both in hairless mouse liver and skin homogenates. N-dodecyl salicylamide (C12SM) showed the lowest permeation of salicylic acid in skin compared to the other prodrugs, probably due to its low aqueous solubility. It had a high affinity for the stratum corneum and its accumulation was restricted to only the uppermost layer of skin. Thus, this amide prodrug could be a safer topicalsunscreen agent with minimum potential for systemic absorption.ⓒ2011 Elsevier B.V.All rights reserved.