从棒状制剂中应用的酮替芬的皮肤渗透。

Skin permeation of ketotifen applied from stick-type formulation.

作者信息

Kimura Chiharu, Nakanishi Toshihiro, Tojo Kakuji

机构信息

College of Computer Science and Systems Engineering, Kyushu Institute of Technology, Fukuoka, Japan.

出版信息

Eur J Pharm Biopharm. 2007 Sep;67(2):420-4. doi: 10.1016/j.ejpb.2007.02.022. Epub 2007 Mar 6.

DOI:10.1016/j.ejpb.2007.02.022

PMID:17433642

Abstract

A stick-typed long lasting device for both transdermal and topical drug delivery has been developed. Ketotifen fumarate (KT) was used as a model drug. The effect of a variety of permeation enhancers was investigated using hairless mouse skin in vitro. Polyoxyethylene oleyl ether (POE), among the enhancers used, most enhanced the skin permeation of KT. The permeation enhancement was mainly due to the increase in the drug solubility in the stratum corneum and the resulting increase in the partition coefficient. The rate of skin permeation of KT was approximately proportional to the loading dose of the drug.

摘要

已研发出一种用于经皮和局部给药的棒状长效装置。富马酸酮替芬（KT）用作模型药物。在体外使用无毛小鼠皮肤研究了多种渗透促进剂的作用。在所使用的促进剂中，聚氧乙烯油醚（POE）对KT的皮肤渗透增强作用最为显著。渗透增强主要归因于药物在角质层中溶解度的增加以及由此导致的分配系数的增加。KT的皮肤渗透速率与药物的负载剂量大致成正比。