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      • SCOPUSKCI등재

        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.

      • SCOPUSKCI등재

        아시클로버 - 아시알로페투인 접합체의 간 포획 및 안정성

        손성호,허근,이영대,오두만,용철순 ( Sung Ho Son,Keun Huh,Young Dae Lee,Doo Man Oh,Chul Soon Yong ) 한국약제학회 1997 Journal of Pharmaceutical Investigation Vol.27 No.1

        N/A For the purpose of improving the chemotherapeutic index of acyclovir(ACV), it was conjugated with asialofetuin(AF), which has been reported to enter into hepatocytes. When [H³] acyclovir in itself or its conjugate were administered to rats, the latter was taken up more selectively by the liver than any other tissues. The stability of ACVMP-AF conjugate in phosphate buffer (pH 5.0) and rat liver homogenate showed a pseudo-first order profile. ACVMP-AF, however, was relatively stable in pH7.4 phosphate buffer and rat plasma. The conjugate was added to the isolated rat hepatocyte and cellular uptake was monitored by scintillation counting for up to 6 hours at 37℃. Hepatocytes incubated with the conjugate exhibited radioactivities significantly enhanced over control levels dose-dependently, i.e., a 3-40 fold increase in radioactivities was observed over controls at the conjugate concentrations of 0.1-10 ㎍/㎖. The AUQ in the liver, kidney, spleen. intestine and lung was higher in treatment with ACVMP-AF than that in treatment with ACV. In treatment with ACVMP-AF, the weighted-average overall drug targeting efficiency(Te) for the liver was higher than in treatment with ACV(57.00 vs 13.31%), and the weighted-average tissue exposure(Re) was 5.03 for the liver. These results indicated that ACVMP-AF conjugate was rapidly taken up by hepatocytes and could be an efficient and selective hepatic targeting system.

      • SCOPUSKCI등재

        아시알로페투인을 약물수송체로 이용한 아시클로버의 간표적화

        용철순,손성호,전철수,오두만 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 ε-NH₂ groups of lysine 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 min¹ which was greater than that of ACV. The elimination rate constant from terminal phase was 0.021 min¹. 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.

      • Hepatic Targeting of Acyclovir Using Asialofetuin as a Drug Carrier

        Yong, Chul Soon,Son, Sung Ho,Jun, Chul Soo,Oh, Doo-Man 영남대학교 약품개발연구소 1995 영남대학교 약품개발연구소 연구업적집 Vol.5 No.-

        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 ε-NH₂ groups of lysine 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.

      • 아시아클로버-아시알로페투인 접합체의 간 포획 및 안정성

        손성호,허근,이영대,오두만,용철순 영남대학교 약품개발연구소 1997 영남대학교 약품개발연구소 연구업적집 Vol.7 No.-

        For the puropse of improving the chemotherapeutic index of acyclovir(ACV), it was conjugated with asialofetrin(AF), which has been reported to enter into hepatocytes. When [H³] acyclovir in itself or its conjugate were administered to rats, the latter was taken up more selectively by the liver than any other tissues. The stability of ACVMP-AF conjugate in phosphate buffer (pH 5.0) and rat liver homogenate showed a pseudo-first order profile. ACVMP-AF, however, was relatively stable in pH7.4 phosphate buffer and rat plasma. The conjugate was added to the isolated rat hepatocyte and cellular uptake was monitored by scintillation counting for up to 6 hours at 37℃. Hepatocytes incubated with the conjugate exhibited radioactivites significantly enhanced over control levels dose-dependently. i.e., a 3-40 fold increase in radioactivities was observed over controls at the conjugate concentrations of 0.1-10μg/ml. The AUQ in the liver, kidney, spleen, intestine and lung was higher in treatment with ACVMP-AF than that in treatment with ACV. In treatment with ACVMP-AF, the weighted-average overall drug targeting efficiency(Te) for the liver was higher than in treatment with ACV(57.00 vs 13.31%), and the weighted-average tissue exposure(Re) was 5.03 for the liver. These results indicated that ACVMP-AF conjugate was rapidly taken up by hepatocytes and could be an efficient and selective hepatic targeting system.

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