Ueda Osamu, Hasegawa Masaaki, Kitamura Shigeyuki
Functional Food Development Group, Functional Food Research & Development Center, Shiseido Co., Ltd., Kanagawa, Japan.
Drug Metab Pharmacokinet. 2009;24(2):180-4. doi: 10.2133/dmpk.24.180.
In this study, the absorption, distribution and excretion of ceramide were examined in rats. After a single oral administration of (3)H-ceramide, mean plasma concentration of radioactivity reached maximum at approximately 10.67 hr and decreased with a T(1/2) of 67.12 hr. The mean cumulative excretion of radioactivity in urine and feces accounted for approximately 4.79% and 87.44%, respectively, of the dose. At 96 hr after dosing, 1.67% and 3.67%, respectively, of the dose were still present in the skin and carcass. The radioactivity in the skin at 12 hr was lower than that in plasma and the ratio of skin to plasma concentration was 0.7. However, at 120 hr after dosing, the ratio of skin to plasma concentration increased to 4. A detailed analysis of the distribution of radioactivity in a section of skin showed that radioactivity was located in the dermis and epidermis. At 168 hr, the radioactivity in the epidermis was 8.0% of the radioactivity in skin. The results of the present study clearly demonstrate that some ceramide orally administered is distributed gradually in the dermis after gastrointestinal absorption, followed by transfer from the dermis to the epidermis.
在本研究中,对大鼠体内神经酰胺的吸收、分布和排泄情况进行了检测。单次口服(3)H-神经酰胺后,放射性物质的平均血浆浓度在约10.67小时达到最大值,并以67.12小时的半衰期下降。尿液和粪便中放射性物质的平均累积排泄量分别约占给药剂量的4.79%和87.44%。给药后96小时,皮肤和 carcass 中仍分别存在1.67%和3.67%的给药剂量。给药后12小时,皮肤中的放射性低于血浆中的放射性,皮肤与血浆浓度之比为0.7。然而,给药后120小时,皮肤与血浆浓度之比增至4。对皮肤切片中放射性物质分布的详细分析表明,放射性物质位于真皮和表皮中。在168小时时,表皮中的放射性为皮肤中放射性的8.0%。本研究结果清楚地表明,口服的一些神经酰胺在胃肠道吸收后逐渐分布于真皮,随后从真皮转移至表皮。