N-甲基-2-吡咯烷酮对雌二醇皮肤渗透的影响。

Effect of N-methyl-2-pyrrolidone on skin permeation of estradiol.

作者信息

Koizumi Atsuko, Fujii Makiko, Kondoh Masuo, Watanabe Yoshiteru

机构信息

Department of Pharmaceutics and Biopharmaceutics, Showa Pharmaceutical University, Tokyo, Japan.

出版信息

Eur J Pharm Biopharm. 2004 May;57(3):473-8. doi: 10.1016/j.ejpb.2003.12.006.

DOI:10.1016/j.ejpb.2003.12.006

PMID:15093595

Abstract

N-Methyl-2-pyrrolidone (NMP) increased the skin permeation of estradiol (E2) in Yucatan micropig epidermis using a modified Franz-type diffusion cell. The addition of NMP significantly increased the fluxes of E2 from water and soybean oil. The flux and skin concentration of E2 were higher from soybean oil than from water and increased with increasing NMP concentrations in soybean oil. Correlation was observed with E2 flux and skin concentration (R(2) = 0.804) NMP enhanced E2 skin permeation because NMP made E2 skin concentration higher. Thus, NMP (10%) was added to the oily gel made by isocetyl isostearate and hydrogenated phospholipid. E2 permeation from the gel without NMP was the same as that from soybean oil suspension. The flux of E2 from the gel with NMP was 0.6 microg/h per cm(2) and might be sufficient for estrogen replacement therapy.

摘要

使用改良的弗兰兹型扩散池，N-甲基-2-吡咯烷酮（NMP）增加了尤卡坦微型猪表皮中雌二醇（E2）的皮肤渗透。添加NMP显著增加了E2从水和大豆油中的通量。E2从大豆油中的通量和皮肤浓度高于从水中的，并且随着大豆油中NMP浓度的增加而增加。观察到E2通量与皮肤浓度之间存在相关性（R(2) = 0.804）。NMP增强了E2的皮肤渗透，因为NMP使E2的皮肤浓度更高。因此，将NMP（10%）添加到由异壬酸异壬酯和氢化磷脂制成的油性凝胶中。不含NMP的凝胶中E2的渗透与大豆油悬浮液中的相同。含NMP的凝胶中E2的通量为每平方厘米0.6微克/小时，这可能足以用于雌激素替代疗法。