原料药粒径对头孢地尼颗粒体外溶出行为的影响

The in vitro influence of particle sizeof cefdinir granules on the dissolution behavior

目的考察原料药粒径对头孢地尼颗粒体外溶出度的影响。方法参照2010版中国药典第二法,以p H=6.8磷酸盐缓冲液为溶出介质,转速为50 r·min-1,采用紫外分光光度法为分析方法,考察不同粒径的原料制备的头孢地尼颗粒与参比制剂溶出的一致性。结果粒径为D90:142.90μm、D50:30.25μm、D10:3.47μm(100目筛)和D90:51.21μm、D50:10.71μm、D10:2.25μm(200目筛)的头孢地尼原料制成的颗粒溶出行为与原研不相似;在不同溶出介质中,D90:35.62μm、D50:6.98μm、D10:1.66μm的头孢地尼原料制成的颗粒,与参比制剂的溶出行为均相似。结论建立的分析方法简单可靠,原料微粉化能够有效提高难溶性药物的溶出度。

Objective To study the in vitro effects of the drug material particle size on the dissolution behavior of cefdinir granules. Methods According to the second method of the CP 2010,phosphate buffer solution （pH6.8）was selectedasstripping medium,along withthe stirring speed of 50 r·min -1 and UV spectrophotometry methods,to study the consistency of dissolution behavior between refer-ence preparation and cefdinir granules which were prepared fromraw material of different particle sizes.Results The dissolution behav-ior of cefdinir granules is notsimilar to original one,when the particle size is either D90：142.90 μm,D50：30.25 μm,D10：3.47 μm（100 mesh）,D90：51.21 μm,D50：10.71 μm,or D10：2.25 μm（200 mesh）.And when particle size of cefdinir is D90：35.62 μm,D50：6.98μm and D10：1.66 μm,the dissolution behavior of cefdinir granulesis similar to the reference preparationin different kinds of dissolution medium.Conclusions The established method is simple and reliable,and the micronization of raw material can effectively improve the dissolution rate ofinsoluble drug.