用于盐酸毛果芸香碱缓释眼部给药的原位凝胶化木葡聚糖制剂。

In situ gelling xyloglucan formulations for sustained release ocular delivery of pilocarpine hydrochloride.

作者信息

Miyazaki S, Suzuki S, Kawasaki N, Endo K, Takahashi A, Attwood D

机构信息

Faculty of Pharmaceutical Sciences, Health Science University of Hokkaido, Ishikari-Tohbetsu, 061-0293, Hokkaido, Japan.

出版信息

Int J Pharm. 2001 Oct 23;229(1-2):29-36. doi: 10.1016/s0378-5173(01)00825-0.

DOI:10.1016/s0378-5173(01)00825-0

PMID:11604255

Abstract

Thermoreversible gels formed in situ by aqueous solutions of an enzyme-degraded xyloglucan polysaccharide were evaluated as sustained release vehicles for the ocular delivery of pilocarpine hydrochloride. In vitro release of pilocarpine from gels formed by warming xyloglucan sols (1.0, 1.5 and 2.0% w/w) to 34 degrees C followed root-time kinetics over a period of 6 h. The miotic responses in rabbit following administration of xyloglucan sols were compared with those from in situ gelling Pluronic F127 sols and from an aqueous buffer solution containing the same drug concentration. Sustained release of pilocarpine was observed with all gels, the duration of miotic response increasing with increase of xyloglucan concentration. The degree of enhancement of miotic response following sustained release of pilocarpine from the 1.5% w/w xyloglucan gel was similar to that from a 25% w/w Pluronic F127 gel.

摘要

通过酶降解木葡聚糖多糖水溶液原位形成的热可逆凝胶被评估为用于盐酸毛果芸香碱眼部给药的缓释载体。将木葡聚糖溶胶（1.0%、1.5%和2.0% w/w）加热至34℃形成的凝胶中，毛果芸香碱在6小时内的体外释放遵循根时间动力学。将木葡聚糖溶胶给药后家兔的缩瞳反应与原位凝胶化的泊洛沙姆F127溶胶以及含有相同药物浓度的水性缓冲溶液的缩瞳反应进行比较。所有凝胶均观察到毛果芸香碱的持续释放，缩瞳反应的持续时间随木葡聚糖浓度的增加而增加。从1.5% w/w木葡聚糖凝胶中持续释放毛果芸香碱后缩瞳反应增强的程度与从25% w/w泊洛沙姆F127凝胶中增强的程度相似。