Miyajima Atsushi, Kigure Akira, Anata Taichi, Hirota Takashi
Department of Biopharmaceutics, Faculty of Pharmaceutical Sciences, Tokyo University of Science, Japan.
Department of Biopharmaceutics, Faculty of Pharmaceutical Sciences, Tokyo University of Science, Japan.
Drug Metab Pharmacokinet. 2015 Dec;30(6):385-90. doi: 10.1016/j.dmpk.2015.07.004. Epub 2015 Aug 5.
Ivermectin (IVM) is used as an oral medication for scabies, a skin infection caused by a mite, sarcoptes scabiei, which parasitizes in the stratum corneum. After oral administration IVM is absorbed from the intestine, and finally distributed to the stratum corneum to eliminate the mites. However its transport mechanism remains unclear. A pharmacokinetic study was performed using hairless Wistar Yagi (HWY) rats, which have no or atrophied sebaceous glands, and Wistar rats as a reference. After oral administration of IVM to both groups, the area under the concentration-time curve of IVM in the dermis and epidermis (dermis-epidermis) of HWY rats were about 60% lower than that of Wistar rats, even though the plasma concentration profiles were comparable in both groups. In addition at 12 h after the administration, IVM concentration in the outer stratum corneum, the shallower layer of the dermis-epidermis, was higher compared to that in the deeper layer. In the dermis-epidermis of the skin from various locations, the concentrations of IVM and squalene, the latter of which is secreted to the skin surface via the sebaceous gland, were positively well correlated. Those results suggest that IVM is transported to the stratum corneum via the sebaceous glands.
伊维菌素（IVM）作为一种口服药物用于治疗疥疮，疥疮是一种由疥螨（疥螨属）引起的皮肤感染，疥螨寄生于角质层。口服后，IVM从肠道吸收，最终分布到角质层以消灭螨虫。然而，其转运机制仍不清楚。使用无毛Wistar Yagi（HWY）大鼠（其皮脂腺无或萎缩）和Wistar大鼠作为对照进行了一项药代动力学研究。对两组大鼠口服IVM后，HWY大鼠真皮和表皮（真皮 - 表皮）中IVM的浓度 - 时间曲线下面积比Wistar大鼠低约60%，尽管两组的血浆浓度曲线相当。此外，给药后12小时，真皮 - 表皮较浅的外层角质层中的IVM浓度高于较深的层。在来自不同部位皮肤的真皮 - 表皮中，IVM和角鲨烯（后者通过皮脂腺分泌到皮肤表面）的浓度呈正相关。这些结果表明，IVM通过皮脂腺转运到角质层。
