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      • SCOPUSKCI등재

        Use of the Stratum Corneum Reservoir for The Prediction of Skin Penetration

        Ae Ri Cho Lee,Kakuji Tojo 한국약제학회 1993 Journal of Pharmaceutical Investigation Vol.23 No.3

        A simple and quick method based on the transient diffusion theory for predicting the steady state rate of penetration of a drug after transdermal drug administration was proposed. The amount of drug entering the stratum corneum was determined by 20 strippings with an adhesive tape. From the profile of the amount of drug as a function of the number of strippings, the quantity of drug on the surface of stratum corneum was extrapolated. Based on the amounts of drug entering the stratum corneum during two time intervals (t₁ and t₂) within 1 hour after the application, the diffusion and partition coefficient were determined. Once the diffusion coefficient of the drug in the stratum corneum and the partition coefficient (stratum corneum/vehicle) were determined from the present approach, the steady-state flux of penetration across the stratum corneum was calculated. The steady-state rates of penetration of ascorbic acid and estradiol across hairless mouse skin were evaluated from this approach and compared with those obtained from in vitro penetration experiment using excised hairless mouse skin. The data confirmed that the proposed method can predict the steady-state rate of penetration of these drugs across the stratum corneum

      • SCOPUSKCI등재

        Use of the Stratum Corneum Reservoir for the Prediction of Skin Penetration

        Cholee, Ae-Ri,Tojo, Kakuji The Korean Society of Pharmaceutical Sciences and 1993 Journal of Pharmaceutical Investigation Vol.23 No.3

        A simple and quick method based on the transient diffusion theory for predicting the steady state rate of penetration of a drug after transdermal drug administration was proposed. The amount of drug entering the stratum corneum was determined by 20 strippings with an adhesive tape. From the profile of the amount of drug as a function of the number of strippings, the quantity of drug on the surface of stratum corneum was extrapolated. Based on the amounts of drug entering the stratum corneum during two time intervals $(t_1\;and\;t_2)$ within 1 hour after the application, the diffusion and partition coefficient were determined. Once the diffusion coefficient of the drug in the stratum corneum and the partition coefficient (stratum corneum/vehicle) were determined from the present approach, the steady-state flux of penetration across the stratum corneum was calculated. The steady-state rates of penetration of ascorbic acid and estradiol across hairless mouse skin were evaluated from this approach and compared with those obtained from ill vitro penetration experiment using excised hairless mouse skin. The data confirmed that the proposed method can predict the steady-state rate of penetration of these drugs across the stratum corneum.

      • Characterization of Skin Permeation of Vitamin C : Theoretical Analysis of Penetration Profiles and Differential Scanning Calorimetry Study

        Cho LEE, Ae-Ri,TOJO, Kakuji 德成女子大學校 藥學硏究所 1999 藥學論文誌 Vol.10 No.1

        A mechanism for the relatively high permeability of vitamin C in relation to the change in the protein domain of the stratum corneum has been proposed. Firstly, the skin permeation characteristics of vitamin C (l-[1-^14C]-ascorbic acid) using whole skin and stripped skin of the hairless mouse were investigated. By employing a double layer model, physiochemical properties such as diffusivity and solubility of vitamin C in each skin layer, stratum corneum and viable skin were determined. Then, the high skin permeation rate of vitamin C was characterized. A differential scanning calorimetry, (DSC), study was employed to investigate the effect of vitamin C on the stratum corneum, a major diffusion barrier for the skin transport of the compound. Vitamin C was found to permeate rapidly through the skin, in spite of its low lipophilicity. The diffusivity determined from the lag-time was approximately 1000 times higher in the stripped skin, compared with whole skin. There is a dramatic increase (10-fold) in the permeation rate in stripped skin indicating the major barrier presented by the stratum corneum to the skin permeation of vitamin C. The DSC profile showed four very distinctive transitions near 100, 128, 135 and 145℃ which are associated with protein transitions. Comparing normal skin, the peaks are sharpened and there are additional phase transitions above 90℃. An increase in sharpness reflects an increase in the hydration state of the sample, as hydrogen bonds between H_2O molecules and other hydrogen donating chemicals of skin components become major chemical bonds in hydrated samples. The higher permeation rate of vitamin C observed may be due to its enhancing effect on the hydration capacity of skin and solubilizing action on the protein domain of the stratum corneum.

      • Evaluation for Intrinsic Skin Permeation of Unstable Compounds

        Lee Ch'o, Ae-Ri,Tojo, Kakuji 德成女子大學校 藥學硏究所 1997 藥學論文誌 Vol.8 No.1

        An evaluation method is proposed for the intrinsic skin permeation rate of unstable compounds. Vitamin C and vitamin E were used as the model compounds. The degradation of vitamin C and E in the solutions followed first-order kinetics with degradation constants of 0.26h^-1 and 0.014h^-1, respectively. The apparent skin permeation profiles of vitamin C and E in vitro, approximated by a nonlinear profile of the polynomial regression method, was corrected for intrinsic permeation rate considering first-order degradation in the receptor solution. The intrinsic profiles evaluated agreed well with the ones determined from radio-labelled compounds, indicatingthe feasibility of the present analysis.

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