甘草次酸固体分散体3种制备工艺比较  

Comparison of Three Preparation Technologies of Glycyrrhetinic Acid Solid Dispersion

作　　者：潘虹[1] 李飞 柴硕 刘婷婷[1] 刘畅[1] 隋小宇[1] PAN Hong;LI Fei;CHAI Shuo;LIU Tingting;LIU Chang;SUI Xiaoyu(School of Pharmacy,Qiqihar Medical University,Qiqihar,Heilongjiang,China 161006)

机构地区：[1]齐齐哈尔医学院药学院,黑龙江齐齐哈尔161006

出　　处：《中国药业》2022年第18期57-61,共5页China Pharmaceuticals

基　　金：黑龙江省省属本科学校基本科研业务费科研项目[2019-KYYWF-1243]。

摘　　要：目的比较3种不同方法制备的甘草次酸(GA)固体分散体溶出度及物化性质。方法分别采用熔融法、溶剂-熔融法、溶剂法制备GA-聚乙二醇4000固体分散体(GA-PEG4000-SD)。采用桨法测定体外溶出度,傅里叶变换红外光谱法测定化学结构,差示扫描量热分析(DSC)法和X-射线衍射(XRD)法物相鉴别固体分散体。结果与GA原料药比较,3种方法制备的GA-PEG4000-SD的溶出度均明显升高,溶剂法制备的固体分散体的溶出度最高,药载比对于固体分散体的溶出度也有明显影响。物相分析表明药物以片状不规则晶体分散于载体中,FTIR分析表明药物与载体材料间可能有氢键形成。结论与熔融法和溶剂-熔融法比较,溶剂法制备的固体分散体药物的结晶程度更低,体外溶出效果更好。Objective To compare the dissolution rate and physicochemical properties of glycyrrhetinic acid(GA)solid dispersions prepared by three different methods.Methods Glycyrrhetinic acid-polyethylene glycol 4000 solid dispersion(GA-PEG4000-SD)was prepared by melting method,solvent-melting method and solvent method respectively.The in vitro dissolution rate was determined by paddle method,the chemical structure was determined by Fourier transform infrared spectroscopy(FTIR),and the solid dispersion was identified by differential scanning calorimetry(DSC)and X-ray diffraction(XRD).Results Compared with that of GA active pharmaceutical ingredients(API),the dissolution rate of GA-PEG4000-SD prepared by the three methods was significantly higher,and the dissolution rate of solid dispersion prepared by solvent method was the highest.The drug loading ratio also had a significant effect on the dissolution rate of solid dispersion.The phase analysis result showed that the drug was dispersed in the carrier as irregular flake crystals,and the FTIR analysis showed that there might be a hydrogen bond between the drug and the carrier material.Conclusion Compared with that prepared by the melting method and the solvent-melting method,the solid dispersion prepared by the solvent method has a lower degree of crystallinity and a better dissolution effect in vitro.

关 键 词：甘草次酸 固体分散体 制备工艺 溶出度 物相分析 

分 类 号：R943[医药卫生—药剂学]