布渣叶总黄酮固体分散体的制备及体外溶出度测定

Preparation and dissolution of solid dispersion of total flavonoids from Microtis Folium

目的:采用固体分散体技术考察不同载体材料对布渣叶总黄酮提取物溶出度的影响。方法:选择不同种类的聚乙二醇、泊洛沙姆、聚乙烯吡咯烷酮为载体材料,与布渣叶总黄酮提取物按质量比1∶4混合均匀,分别用熔融法和溶剂法制备固体分散体,以固体分散体中总黄酮、牡荆苷、异牡荆苷、水仙苷的90 min累积溶出度作为评价指标,比较不同载体制备的固体分散体的释药速率,并采用X射线衍射和红外光谱分析对其物相特征进行研究。结果:与布渣叶总黄酮提取物和物理混合物相比,以PEG和泊洛沙姆所制备的布渣叶提取物固体分散体中总黄酮、牡荆苷、异牡荆苷和水仙苷的体外溶出度与溶出速率均明显增加。其中以泊洛沙姆407为载体材料所制备的固体分散体中总黄酮体外溶出度最佳,90 min累积溶出度达到84%;以PEG6000为载体材料所制备的固体分散体中牡荆苷、异牡荆苷、水仙苷体外溶出度最佳,90 min累积溶出度均达96%以上。结论:采用固体分散体技术,选择PEG6000或泊洛沙姆407为载体制备布渣叶总黄酮提取物固体分散体,对提取物中脂溶性成分的溶出有明显改善作用。

OBJECTIVE To investigate the effects of different carrier materials on dissolution of total flavonoids extract from microtis folium by using solid dispersion technology.METHODS Different types of polyethylene glycol,poloxamers and polyvinyl pyrrolidone were adopted as carrier materials.Microtis folium extract and carrier materials were mixed at the ratio of 1∶4to prepare solid dispersions by using fusion method and solvent method.Cumulative dissolutions of total flavonoids,vitexin,isovitexin and narcissin in solid dispersions in90 min were selected as the evaluation index to compare the release rates of solid dispersions prepared by different carrier materials.Furthermore,the phase characteristics of the solid dispersions were investigated by x-ray diffractometry and fourier infrared absorption spectrometry.RESULTS Compared with its physical mixture,the in vitro dissolution and dissolution rate evidently increased for total flavonoids,vitexin,isovitexin and narcissin of the solid dispersions prepared with PEG and poloxamer.And the solid dispersions prepared with poloxamer 407 as carrier material had the optimal dissolution of total flavonoids in vitro,the cumulative dissolution of which was up to 84%in 90 min.Solid dispersion prepared with PEG6000 as carrier material had the optimal dissolution of vitexin,isovitexin and narcissin,and the cumulative dissolution was up to 96%in 90 min.CONCLUSION Solid dispersion of microtis folium extracts prepared with PEG6000 or poloxamer 407 can significantly improve dissolution of liposoluble constituents in the extracts.