文章基本信息

标题：Modification of Ocular Permeability of Peptide Drugs by Absorption Promoters
本地全文：下载
作者：Hitoshi SASAKI ; Kenzo YAMAMURA ; Takahiro MUKAI 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2000
卷号：23
期号：12
页码：1524-1527
DOI：10.1248/bpb.23.1524
出版社：The Pharmaceutical Society of Japan
摘要：The purpose of this study was to investigate the effect of absorption promoters on the ocular membrane permeability of thyrotropin-releasing hormone (TRH) and luteinzing hormone-releasing hormone (LHRH) as model peptides. The permeabilities of TRH and LHRH were measured using a two-chamber glass diffusion cell mounted with isolated ocular membranes of albino rabbits. Saponin, EDTA, benzalkonium chloride and paraben were used as absorption promoters. These promoters enhanced the permeability of hydrophilic molecules through the cornea and conjunctiva. The promoting effects of the absorption promoters on the conjunctival drug penetrations were not as strong as those on the corneal penetrations. The different responses of the corneal and conjunctival drug penetrations to these promoters may be useful in controlling the extent and pathway of the ocular and systemic absorptions of instilled drugs. The promotional effects of absorption promoters on the corneal drug pentration apparently increased with an increase in pentrant molecular weights, although those on the conjunctival drug penetrations did not depend on the molecular weights.
关键词：TRH;LHRH;ocular penetration;drug delivery;cornea