设计一种含氢磷脂的聚乙烯醇作为盐酸（±）-普萘洛尔直肠给药的控释载体。

Design of a polyvinyl alcohol hydrogen containing phospholipid as controlled-release vehicle for rectal administration of (+/-)-propranolol HCl.

作者信息

Morimoto K, Fukanoki S, Hatakeyama Y, Nagayasu A, Morisaka K, Hyon S H, Ikada Y

机构信息

Department of Pharmaceutical Sciences, Osaka University of Pharmaceutical Sciences, Japan.

出版信息

J Pharm Pharmacol. 1990 Oct;42(10):720-2. doi: 10.1111/j.2042-7158.1990.tb06567.x.

DOI:10.1111/j.2042-7158.1990.tb06567.x

PMID:1982145

Abstract

Polyvinyl alcohol hydrogels which contained phospholipid, egg yolk lecithin or hydrogenated soya lecithin were designed as a transrectal delivery system for propranolol hydrochloride. The hydrogel preparations containing phospholipid were prepared by a low-temperature crystallization method. The release profile of propranolol from hydrogel preparations containing phospholipid complied with Fickian diffusion (Higuchi model). The release of propranolol from the hydrogel preparation decreased with higher contents of phospholipid (approximately 2% w/w). In rats plasma concentrations of propranolol after rectal administration of hydrogel preparations containing phospholipid (1 and 2% w/w) were prolonged compared with those of rats receiving preparations without phospholipid.

摘要

含有磷脂、蛋黄卵磷脂或氢化大豆卵磷脂的聚乙烯醇水凝胶被设计为盐酸普萘洛尔的经直肠给药系统。含磷脂的水凝胶制剂采用低温结晶法制备。盐酸普萘洛尔从含磷脂水凝胶制剂中的释放曲线符合菲克扩散（Higuchi模型）。随着磷脂含量（约2%w/w）的增加，盐酸普萘洛尔从水凝胶制剂中的释放量减少。与接受不含磷脂制剂的大鼠相比，直肠给予含磷脂（1%和2%w/w）水凝胶制剂的大鼠血浆中普萘洛尔的浓度持续时间延长。