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YH1885의 체내동태(제1보) : 흰쥐에서 14C-YH1885의 단회투여시 흡수, 조직분포 및 배설
안병락(Byung Nak Ahn),Naoki Fujio,Naotoshi Kusumoto,Yoshifumi Abe,Masaaki Odomi,이종욱(Jong Wook Lee) 대한약학회 1997 약학회지 Vol.41 No.3
The absorption, distribution and excretion of 14C labeled YH1885 {5,6-Dimethyl-2(4-fluorophenylamino)-4-(1-methyl-1,2,3,4-tetrahydroisoquinolin-2-yl)pyrimidine hydrochloride), a new proton pumpinhibitor, were investigated in rats after a single administration of 14C-YH1885. 1. After intravenous administration of 5mg/kg, the blood level of radioactivity declined in a biphasic fashion with the mean terminal elimination half-life of 12.4hr. 2. After oral administration of 20mg/kg, the maximum blood level of radioactirity was reached at 4.0hr in female rats. The blood level of radioactivity-time profiles in male and female rats were similar, and the absorptionof 14C-YH1885 was not affected by food. 3. Appproximately 89% and 1% of radioactivity of the total dose were excreted in feces and urine, respectively. 4. Biliary excretion of radioactivity was 47.9% of the dose. Enterohepatic circulation of radioactivity was 49.6%. 5. Radioactivity was excreted maily into feces via bile. 6. The concentration of radioactivity in most tissues reached the peak level at 4.0hr after dosing, and then declined. Autoradiograms of male rats showed that the radioactivity levlels in the fat, harder's gland, liver and G-Itract were higher than those in the other tissues and the elimination of radioactivity from fat and liver was slow. 7. Autoradiograms of a pregnant rat showed that radioactivity was transferred to mammary gland, placenta and fetus. The radioactivity level in the mammary gland was higher than that in the blood.
상피세포 성장인자의 경피흡수 : 정상피부 , 각질제거피부 및 화상피부에 있어서
심창구,조애리,이정욱,안병락,정주영,고여욱 한국약제학회 1996 Journal of Pharmaceutical Investigation Vol.26 No.1
In vivo and in vitro skin permeation of recombinant ^(125)I-EGF through normal. stripped and the first degree burn skin were studied. The in vitro skin permeation rate through the first degree burn skin (296 cpm/㎠/hr) and the stripped skin (1131 cpm/㎠/hr) were 3.5 times and 13 times higher, respectively, as compared with the one through normal skin. In vivo absorption study with the first degree burn skin, the peak concentration of EGF in the skin was achieved at 1-3 hr and decreased afterward up to 8 hr with an elimination constant of 1.31 × 10³g/㎖/hr. To investigate the higher elimination rate of EGF in burn skin, binding and metabolism studies were conducted. No significant metabolism of EGF in burn skin (100℃, 5second burning) was observed. With the presence of unlabelled-EGF, ^(125)I-EGF permeation through the burn skin showed higher permeation rate than the one without unlabelled-EGF. The result may indicate that EGF-receptor binding play a role in determining the skin permeation rate.