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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。
Objective To improve the dissolution rate of enzaprine in vitro by hot melt granulation technology. Methods The microcrystalline cellulose was used as excipient and the hot-melt granulation method was used to prepare the composition of engelline and microcrystalline cellulose. The mass ratio of engelles net to microcrystalline cellulose in the compositions 1, 2 and 3 were 1: 2, 1: 3 and 1: 4. The appearance of the composition was observed with a microscope, the composition was detected by differential scanning calorimetry, X-ray powder diffraction, and the in vitro dissolution rate of the composition and drugs of different particle sizes was compared. Results The present form of engelhline in the composition was in a mixture of crystalline and amorphous phases. In-vitro dissolution tests showed that the dissolution rate was improved. Compositions 2 and 3 were eluted at a similar rate to micronized APIs. Conclusion Hot melt granulation technology can effectively improve the dissolution rate of the drug.