热熔挤出技术制备穿心莲提取物固体分散体

Preparation of Andrographis paniculata Extract Solid Dispersion by Hot-melt Extrusion Technology

目的:采用热熔挤出技术(HME)制备穿心莲提取物的固体分散体,并对其进行体外评价。方法:以穿心莲内酯和脱水穿心莲内酯含量为指标,采用单因素试验,分别对亲水性载体种类、穿心莲提取物与载体用量比例进行筛选,确定最优穿心莲提取物热熔挤出固体分散体的制备方法,并对形成的固体分散体进行体外溶出度试验和差式扫描量热分析、电镜扫描、X-射线衍射等物相鉴别。结果:穿心莲提取物热熔挤出固体分散体的最优制备工艺为:以Soluplus为载体,穿心莲提取物∶Soluplus=1∶2(m/m)混合,热熔挤出区段升温程序为130→135→140→130℃,螺杆转速为27 r/min,加料速度为15 g/min。物相鉴别试验显示穿心莲提取物在热熔挤出分散体中以无定形态分散。结论:HME能使穿心莲提取物以无定形状态分散,提高穿心莲提取物的溶解度。

OBJECTIVE： To prepare Andrographis paniculata extract solid dispersion by using hot-melt extrusion （HME） technology, and to evaluate it in vitro. METHODS： The type of hydrophilic carrier and the proprotion of A. panieulata extract to carri- er were screened by single factor test using andrographolide and dehydroandrographolide as index. The preparation technology of A. paniculata extract solid dispersion was optimized. The dissolution rate in vitro was studied, and DSC, SEM, X-ray diffraction were used to analyze the solid dispersion. RESULTS： The optimal technology ofA. paniculata extract solid dispersion by HME were as follows： chosing polyethylene caprolactam-polyvinyl acetate-soluplus as the carrier; the ratio of A. paniculata extract to soluplus was 1：2（m/m）; the temperate-rasing program of HME should be 130→135→140→130℃ ; the rotation rate of screw arbor was 27 r/min, feeding speed was 15 g/min. The results of physicochemical characterization experiment indicated that A. paniculata extract were in amorphous state in solid dispersion by HME. CONCLUSIONS： HME can disperse A. paniculata extract in amorphous state, and improve its solubility.