固体分散技术用于提高格列美脲片溶出度研究

Solid Dispersion Technology for Improving Dissolution Rate of Glimepiride Tablets

目的利用固体分散技术提高格列美脲(GM)片的体外溶出度。方法以二氯甲烷为溶剂、聚维酮K30(PVP K30)为载体,用溶剂法制备GM固体分散体(SD);采用显微扫描电镜(SEM),X-射线衍射分析(XRD),差示扫描量热分析(DSC),红外光谱分析(FTIR)技术对GM固体分散体进行物相鉴定;制备GM普通片和SD片,测定溶出曲线,并用f2因子法与以格列美脲片(亚莫利,赛诺菲安万特<北京>制药有限公司)为参比制剂的溶出曲线进行相似性比较。结果 GM∶PVP K30=1∶4制备的固体分散体中GM以非晶形态分散于PVP K30中,体外溶出度为89.28%,88.73%,90.76%,相似因子f2为82.60,79.40,81.00。结论固体分散技术可显著提高GM片的体外溶出度,GM SD的溶出行为与参比制剂非常相似。

Objective To improve the dissolution rate in vitro of Glimepiride（GM）Tablets by using the solid dispersion（SD）technology. Methods The GM solid dispersion was prepared by the solvent method with polyvinyl pyrrolidone K30（PVP K30）as the carrier and methylene chloride as the solvent. The SEM,XRD,DSC and FTIR analytical techniques were adopted to perform the quantitative phase identification of GM in SD;the common tablets and SD tablets of GM were compared,the dissolution curve of GM was measured,its dissolution curve was performed the similarity comparison with the reference preparation Amaryl made by the Sanofi-Aventis（Beijing） pharmaceutical Co. Ltd. ,by using the f2 factor method. Results GM with the non-crystallite form was dispersed in PVP K30 within SD prepared under the GM and PVP K30 weight ratio of 1 ：4,its dissolution in vitro and similarity factor f2 were 89. 28%,88. 73%, 90. 76% and 82. 60,79. 40,81. 00 respectively. Conclusion The SD technology can remarkably improve the dissolution rate in vitro of GM tablets and its dissolution behavior is similar to the reference preparation.