Uchida T, Yasutake T, Goto S
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
Chem Pharm Bull (Tokyo). 1992 Feb;40(2):463-6. doi: 10.1248/cpb.40.463.
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.
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。