基于反溶剂冻干技术穗花杉双黄酮的制备和分析表征  

Preparation and analytical characterization of micronized amentoflavone by antisolvent freeze-drying method

作　　者：任秋霞[1,2] 周喆[2] 王升启[2] 

机构地区：[1]天津中医药大学,天津300193 [2]军事医学科学院放射与辐射医学研究所,北京100850

出　　处：《国际药学研究杂志》2013年第2期237-241,共5页Journal of International Pharmaceutical Research

基　　金：国家自然科学基金资助项目(81172981)

摘　　要：目的采用反溶剂冻干法制备穗花杉双黄酮微粉,以解决该药水溶性差的问题,提高药物口服生物利用度。方法通过考察反溶剂冻干法反应溶剂与水的比例、药物溶液浓度、反应温度、搅拌速度和搅拌时间对颗粒粒径的影响,得到适宜的微粉化条件。在此基础上分别利用激光粒度分析、扫描电镜、傅立叶转换红外光谱、粉末X线衍射和体外溶出实验对原料药和微粉进行分析表征。结果最佳处方制备的微粉颗粒粒径在0.08μm左右,冻干后样品为无定形。结论本方法制备的穗花杉双黄酮微粉溶解度和溶出速率显著提高,为改善药物的口服生物利用度提供了基础。Objective The micronized amentoflavone was prepared by the anti-solvent freeze-drying method in order to im- prove water solubility of the drug. Methods The effects of the proportion of the reaction solvent with water, drug concentration, preci- pition temperature, stirring rate, and stirring time on particle sizes were investigated, and the optimum conditions were obtained. The microsized amentoflavone and the raw amentoflavone were well characterized by laser particle size analyzer, scanning electron microsco- py, Fourier transform infrared spectrometry, powder X-ray diffraction and the in vitro dissolution experiment. Results The particle size of the optimal formulation was around 0. 08 um, and the microsized amentoflavone was amorphous after freeze-drying. Conclusion The solubility and dissolution rate of the amentoflavone was significantly increased after micronization, which provides a basis for impro- ving the oral hioavailabilitv.

关 键 词：穗花杉双黄酮 反溶剂冻干 微粉化 

分 类 号：R283[医药卫生—中药学]