Nimni M E, Ertl D, Oakes R A
University of Southern California School of Medicine, Department of Biochemistry, Orthopaedic Hospital, Los Angeles 90007.
J Pharm Pharmacol. 1990 Oct;42(10):729-31. doi: 10.1111/j.2042-7158.1990.tb06570.x.
Effective penetration of griseofulvin across the dermal barrier has been achieved using an anhydrous solvent system of benzyl alcohol (10%), acetone (40%), and isopropanol (50%). There were quantitative differences in the relative accumulation of griseofulvin in skin compared with internal organs, when the topical and oral routes of administration were compared. The topical route enhanced localized concentrations of griseofulvin at the site of application, and these persisted for several days. After daily topical application a steady state was reached at day 3, when the diffusion across the skin barrier and epidermal loss seemed to equal the total amount applied to the skin surface. The application of griseofulvin topically, required a much smaller amount of drug to achieve similar integumentary levels compared with the amount required orally.
使用由10%苯甲醇、40%丙酮和50%异丙醇组成的无水溶剂系统，已实现灰黄霉素对皮肤屏障的有效渗透。当比较局部给药和口服给药途径时，与内部器官相比，灰黄霉素在皮肤中的相对蓄积存在量的差异。局部给药途径提高了灰黄霉素在用药部位的局部浓度，且这些浓度可持续数天。每日局部给药后，在第3天达到稳态，此时经皮肤屏障的扩散和表皮损失似乎等于施用于皮肤表面的总量。与口服所需的量相比，局部应用灰黄霉素需要少得多的药物量就能达到相似的体表水平。
