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Hepatic Targeting of Acyclovir Using Asialofetuin as a Drug Carrier
용철순,손성호,전철수,오두만,Yong, Chul-Soon,Son, Sung-Ho,Jun, Chul-Soo,Oh, Doo-Man 한국약제학회 1994 Journal of Pharmaceutical Investigation Vol.24 No.4
With the purpose of improving the therapeutic index of $[^3H]$ acyclovir (ACV) in the treatment of chronic hepatitis B infection, asialofetuin (AF) which after selective interaction with Ashwell's receptor specifically enters into hepatocytes, was chosen as a carrier system for hepatic targeting. This drug was first converted to its monophosphate (ACVMP), which was subsequently activated by water soluble carbodiimide to conjugate with ${\varepsilon}-NH_2$ groups of Iysine residues of AF. The molar ratio of ACVMP to AF in the conjugate was 3.9. In rats, elimination of ACVMP-AF conjugate after i.v. injection showed two phase elimination kinetics. Initial apparent elimination rate constant in rats was $0.191\;min^{-1}$ which was greater than that of ACV. The elimination rate constant from terminal phase was $0.021\;min^{-1}$. Area under the total radioactivities versus time curve was found to be several times larger in liver than in other organs (spleen, intestine, lung and kidney) after i.v. administration of the conjugate labelled in the drug moiety. The above results suggested that ACVMP-AF conjugate was rapidly taken up by hepatocytes and could be a useful hepatic targeting system.
헬리코박터 파이로리 균 진단용 <sup>13</sup>C-요소 캅셀의 개발
용철순,김용일,김지만,강성훈,권기철,이종달,김종국,사홍기,최한곤,Yong, Chul-Soon,Kim, Yong-Il,Kim, Chi-Man,Kang, Sung-Hoon,Quan, Qi-Zhe,Rhee, Jong-Dal,Kim, Chong-Kook,Sah, Hong-Kee,Choi, Han-Gon 한국약제학회 2002 Journal of Pharmaceutical Investigation Vol.32 No.1
The purpose of this study was to develop a new $^{l3}C-urea-containing$ capsule for diagnosis of H. pylori. The urea-containing capsules were prepared with various diluents such as polyethylene glycol (PEG), microcrystalline cellulose, sodium lauryl sulfate and citric acid. The dissolution test, $^{l3}C-urea$ breath test and stability test were then performed on the capsules. Microcrystalline cellulose and sodium lauryl sulfate retarded the initial dissolution rates of urea. However, PEG increased the initial dissolution rates of urea. Furthermore, two formulae composed of PEG, [$^{l3}C-urea/PEG$ (38/1.9 mg/cap)] and [$^{l3}C-urea/PEG/citric$ acid (38/1.9/1.9 mg/cap)] had the maximum DOB value, about 16 at 20 mim, while the formula composed of only 38 mg $^{l3}C-urea$ had the maximum DOB value at 30 min. The results indicated that PEG improved the, sensitivity of $^{l3}C-urea$ in the human volunteers. The capsule [$^{l3}C-urea/PEG$ (38/1.9 mg/cap)] was stable for at least six months in 25 and $37^{\circ}C$. Thus, a PEG-containing capsule, [$^{l3}C-urea/PEG$ (38/1.9 mg/cap)] would be a more economical, sensitive and stable preparation for diagnosis of H. pylori.
The Effect of Physicochemical Properties of Salicylate Analogs on Binding to Bovine Serum Albumin
용철순,Yong, Chul-Soon 한국약제학회 1993 Journal of Pharmaceutical Investigation Vol.23 No.3
The protein binding of salicylate analogs has been investigated by equilibrium dialysis. A series of binding experiments were performed in order to elucidate the effects of physicochemical properties of salicylate analogs on the binding with bovine serum albumin. Attempts to correlate affinity constants with capacity factor, steric factor and Hammett ${\sigma}$ values suggested hydrophobic forces to be involved in the binding of salicylate analogs. Steric factor contributes to binding process partly, whereas electronic interaction appears to be insignificant.
용철순(Chul Soon Yong),이종달(Jong Dal Rhee),김종국(Chong Kook Kim),최한곤(Han Gon Choi) 한국약제학회 2001 Journal of Pharmaceutical Investigation Vol.31 No.2
N/A The purpose of this study was to investigate the effect of additives on the powder characteristics of peonja dry elixir. Peonja dry elixirs were prepared with various amounts of dextrin using a spray-dryer, and their powder characteristics such as flow, cohesion and compressibility were evaluated as an angle of repose, cohesion index and compressibility index, respectively. Their powder characteristics were not significantly different from one another, indicating that the hydrophilic dextrin, a base of dry elixir hardly affected their powder characteristics. Peonja dry elixirs were prepared with 10% dextrin and various amounts of additives such as mannitol (hydrophilic excipient), sodium lauryl sulfate (surfactant), colloidal silica (hydrophobic excipient) and HPMC (polymer), respectively, and their angle of repose, cohesion index and compressibility index were measured. The powder characteristics of peonja dry elixirs prepared with mannitol were not significantly different from one another, indicating that the mannitol scarcely improved the powder characteristics of peonja dry elixirs. The angle of repose and cohesion index of peonja dry elixirs significantly decreased with increasing amount of sodium lauryl sulfate to 0.3% followed by no significant changes in them. The cohesion index of peonja dry elixir significantly decreased with increasing amount of colloidal silica. The angle of repose and cohesion index of peonja dry elixir significantly decreased with increasing amount of HPMC to 0.3% followed by an abrupt increase in them. However, the compressibility index of peonja dry elixir significantly increased with increasing amount of HPMC to 0.3% followed by an abrupt decrease in them. Our results suggested that a small amount of sodium lauryl sulfate, colloidal silica and HPMC improved markedly the powder characteristics of peonja dry elixirs due to forming stronger and less hygroscopic shell of peonja dry elixirs. Among the peonja dry elixirs studied, the peonja dry elixir prepared with 0.3% sodium lauryl sulfate and 0.3% HPMC had the lowest angle of repose of 27˚ and cohesion index of 37.8%, and the highest compressibility index of 38.7%, respectively. Thus, sodium lauryl sulfate and HPMC appear to be promising additives for peonja dry elixir, if used in adequate amounts.
약학박사 정 시련 교수 정년퇴임 기념호 : 연구논문(재록) ; 생명과학 : 폴록사머와 프로필렌글리콜을 사용한 클로트리마졸함유 좌제의 항암효능 증대 및 간 독성 감소 효과
용철순 ( Chul Soon Yong ),현경희 ( Jing Ji Xuan ),백승환 ( Seung Hwan Paek ),오유경 ( Yu Kyoung Oh ),우종수 ( Jong Soo Woo ),최한곤 ( Han Gon Choi ),김정애 ( Jung Ae Kim ),( Mann Hyung Lee ) 영남대학교 약품개발연구소 2006 영남대학교 약품개발연구소 연구업적집 Vol.16 No.-
연구논문 : 생명과학 ; 인간에서의 경구흡수를 촉진하는 투명 아세클로페낙 연질캅셀의 개발
용철순 ( Chul Soon Yong ),오유경 ( Yu Kyoung Oh ),이경희 ( Kyung Hee Lee ),박상만 ( Sang Man Park ),길영식 ( Young Sig Gil ),유창훈 ( Chang Hun Yu ),김종오 ( Jong Oh Kim ),유봉규 ( Bong Kyu Yoo ),이종달 ( Jong Dal Rhee ),김종국 ( 영남대학교 약품개발연구소 2005 영남대학교 약품개발연구소 연구업적집 Vol.15 No.-
연구논문 : 생명과학 ; 폴록사머 188 및 멘톨에 의한 쥐에서의 이부프로펜의 직장 생체이용율의 증가
용철순 ( Chul Soon Yong ),양재하 ( Chae Ha Yang ),이종달 ( Jong Dal Rhee ),이범진 ( Beom Jin Lee ),김동출 ( Dong Chool Kim ),김대덕 ( Dae Duk Kim ),김종국 ( Chong Kook Kim ),최진석 ( Jun Shik Choi ),최한곤 ( Han Gon Choi ) 영남대학교 약품개발연구소 2004 영남대학교 약품개발연구소 연구업적집 Vol.14 No.-