| 引用本文: | 余慧,彭俊清,陈浩,王红莲,余露山.热熔造粒技术提高恩格列净溶出速度的研究[J].中国现代应用药学,2016,33(7):904-907. |
| YU Hui,PENG Junqing,CHEN Hao,WANG Honglian,YU Lushan.Study of Hot Melt Granulation to Improve Dissolution Rate of Empagliflozin[J].Chin J Mod Appl Pharm(中国现代应用药学),2016,33(7):904-907. |
|
| 摘要: |
| 目的 采用热熔造粒技术提高恩格列净的体外溶出速度。方法 选用微晶纤维素为辅料，热熔造粒法制备恩格列净与微晶纤维素的组合物，组合物1，2，3中恩格列净与微晶纤维素的质量比分别为1∶2，1∶3和1∶4。采用显微镜观察组合物外观，采用差示扫描量热法、X-射线粉末衍射法对所得组合物进行检测, 并对比组合物和不同粒径药物的体外溶出速度。结果 组合物中恩格列净的存在形式是晶体与无定形的混合状态, 体外溶出度实验表明其溶出速度能得到提升，组合物2、3的溶出速度与微粉化的原料药溶出速度类似。结论 采用热熔造粒技术能有效提高药物的溶出速度。 |
| 关键词: 恩格列净 溶出速度 微粉化 |
| DOI： |
| 分类号:R944.2 |
| 基金项目: |
|
| Study of Hot Melt Granulation to Improve Dissolution Rate of Empagliflozin |
|
YU Hui1,2, PENG Junqing2, CHEN Hao2, WANG Honglian2, YU Lushan1
|
|
1.College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China;2.Zhejiang Huahai Pharmaceutical Co., Ltd., Linhai 317024, China
|
| Abstract: |
| OBJECTIVE To improve the dissolution rate of empagliflozin by hot-melt granulation technology. METHODS The compositions of empagliflozin were prepared by hot-melt granulation, with microcrystalline cellulose (MCC) as filler, the ratio empagliflozin to MCC in composition 1, 2 and 3 was 1∶2，1∶3 and 1∶4, respectively . Appearances were observed by microscope, the physical states of compositions were investigated by differential scanning calorimetry (DSC) and X-ray powder diffraction analysis (XRPD). The dissolution rate of empagliflozin with different particle sizes and different compositions were also compared. RESULTS The DSC and XRPD spectrum of the compositions showed that empagliflozin existed in amorphous form and crystal form. The dissolution rate of compositions have been improved by hot-melt granulation. The dissolution rate of composition 2 and 3 were similar to that of micronized empagliflozin. CONCLUSION Dissolution rate of empagliflozin has been improved by hot-melt granulation. |
| Key words: empagliflozin dissolution rate micronization |
