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对乙酰氨基酚从原位凝胶化木葡聚糖制剂的口服持续给药。

Oral sustained delivery of paracetamol from in situ gelling xyloglucan formulations.

作者信息

Miyazaki Shozo, Endo Kumiko, Kawasaki Naoko, Kubo Wataru, Watanabe Hideki, Attwood David

机构信息

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

出版信息

Drug Dev Ind Pharm. 2003 Feb;29(2):113-9. doi: 10.1081/ddc-120016718.

DOI:10.1081/ddc-120016718
PMID:12648007
Abstract

The purpose of this study was to evaluate the potential of a xyloglucan formulation with in situ gelling properties for the oral sustained delivery of paracetamol. Gelation of dilute aqueous solutions of the polysaccharide xyloglucan occurred in rabbit and rat stomachs as the orally administered chilled solutions attained body temperature. In vitro studies demonstrated diffusion-controlled release of paracetamol from the gels over a period of 6 hr. The bioavailabilities of paracetamol from the xyloglucan gels formed in situ in the stomachs of rabbits after oral administration of the liquid formulations were similar to that of a commercially available suspension containing an identical dose of paracetamol.

摘要

本研究的目的是评估具有原位凝胶化特性的木葡聚糖制剂用于口服对乙酰氨基酚缓释给药的潜力。当口服的冷却溶液达到体温时,多糖木葡聚糖的稀水溶液在兔和大鼠胃中发生凝胶化。体外研究表明,对乙酰氨基酚在6小时内从凝胶中以扩散控制的方式释放。口服液体制剂后,在兔胃中原位形成的木葡聚糖凝胶中对乙酰氨基酚的生物利用度与含有相同剂量对乙酰氨基酚的市售混悬剂相似。

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