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市售聚合物混合物作为含头孢羟氨苄或茶碱的缓释微胶囊成分的效用。

Utility of mixture of commercially available polymers as constituents of sustained-release microcapsules containing cefadroxil or theophylline.

作者信息

Uchida T, Yasutake T, Goto S

机构信息

Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.

出版信息

Chem Pharm Bull (Tokyo). 1992 Feb;40(2):463-6. doi: 10.1248/cpb.40.463.

Abstract

Hydroxy propyl methyl cellulose acetate succinate high grade (AS-HG) and ethyl cellulose (EC) mixture microcapsules containing cefadroxil or theophylline were prepared by a solvent evaporation method in liquid paraffin dissolved sorbitan tri-stearate as a dispersing agent, and their sustained-release properties were evaluated. The microcapsules prepared with AS-HG:EC (in a 2:5 weight ratio) mixture containing 20% of cefadroxil or theophylline exhibited apparent zero-order releasing pattern in pH 6 to 8, at 50 rpm and 37 degrees C (paddle method). These microcapsules were administered orally to beagle dogs and the plasma concentrations of cefadroxil or theophylline were measured periodically. As a result of in vivo investigation, a satisfactory sustained-release plasma pattern and an apparent zero-order process in the gastrointestinal absorption were confirmed by deconvolution analysis of both drugs.

摘要

采用溶剂蒸发法,以溶解于液体石蜡中的司盘三硬脂酸酯为分散剂,制备了含头孢羟氨苄或茶碱的羟丙基甲基纤维素琥珀酸酯高级品(AS-HG)与乙基纤维素(EC)的混合物微胶囊,并对其缓释性能进行了评价。含20%头孢羟氨苄或茶碱的AS-HG:EC(重量比为2:5)混合物制备的微胶囊在pH 6至8、转速50 rpm及37℃(桨法)条件下呈现明显的零级释放模式。将这些微胶囊口服给予比格犬,并定期测定头孢羟氨苄或茶碱的血浆浓度。体内研究结果表明,通过对两种药物的反卷积分析,证实了令人满意的缓释血浆模式以及胃肠道吸收中的明显零级过程。

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