正交设计法优化托西酸舒他西林明胶微球的制备工艺及释放度考察

Optimization of the process of sultamicillin tosilate gelatin microspheres by orthogonal design and its release in vitro

目的去除托西酸舒他西林的苦味,改善颗粒剂的口感,制备托西酸舒他西林明胶微球。方法以明胶为载体,液体石蜡为油相,司盘-80为乳化剂,用乳化分散法制备托西酸舒他西林明胶微球,采用正交设计优化明胶微球制备工艺。高效液相色谱法测定微球中药物含量,计算微球的载药量、包封率及体外释药量。结果明胶微球形态良好,无苦味,粒径范围为1.9-12.6μm,平均粒径为6.31μm,平均载药量为20.11%,平均包封率为75.29%,体外5min释药达90%以上。结论此法制备的托西酸舒他西林明胶微球粒径分布集中,去除托西酸舒他西林苦味符合设计要求,具有良好的应用前景。

Purpose To remove the bitter taste of sultamicillin tosilate, to improve the flavor of granules and to study the preparation of sultamicillin tosilate gelatin microspheres. Methods The degradable gelatin was used as a carrier, liquid paraffin as the oil phase and span-80 as the emulsifier . The emulsifying-scattering technique was used for the preparation of gelatin micropheres. The orthogonal design method was applied to optimize the preparation technology.HPLC method was used for the determination of sultamicillin tosilate in gelatin microspheres.Results The gelatin microspheres had a good shape and no bitter taste.Its diameter was in the range of 1 .9 - 12.6μm,and the average particle diameter was 6.31μm.The average drug loading and rate of entrapment of sultamicillin tosilate in the microspheres were 20.11 % and 75 .29 % . More than ninety percent sultamicillin tosilate was released in vitro from the microspheres. Conclusion The size distribution of sultamicillin tosilate gelatin micropheres is focalizing.The removing the bitter taste of sultamicillin tosilate meets the requirements of design and it has favorable application perspective.