黄芩苷纳米结晶的制备工艺  

Preparation Technology of Baicalin Nanocrystallines

作　　者：张秋菊[1] 洪彤彤[1] 魏世杰[1,2] 隋宏[1,3] 王文苹[1,3] 

机构地区：[1]宁夏医科大学药学院,银川750004 [2]宁夏医科大学附属总医院临床药理研究室,银川750004 [3]宁夏回药现代化工程技术研究中心,银川750004

出　　处：《中国实验方剂学杂志》2014年第2期14-18,共5页Chinese Journal of Experimental Traditional Medical Formulae

基　　金：2011年宁夏自然科学基金项目(NZ11103)

摘　　要：目的:优选黄芩苷纳米结晶的制备工艺并考察其稳定性。方法:以粒径及多分散系数(PDI)为指标,采用单因素试验优选黄芩苷纳米混悬液的制备工艺;经离心富集和冷冻干燥制备黄芩苷纳米结晶,观察结晶形态,比较混悬液与冻干粉的初步稳定性;采用摇瓶法测定平衡溶解度。结果:最佳制备工艺为黄芩苷溶于二甲基亚砜中配成50 g·L-1的溶液,注入20倍量0.5%卵磷脂水溶液中,冰水浴下30 000 r·min-1高速剪切8 min;制备的纳米混悬液粒径280.6 nm(PDI=0.047),纳米结晶粒径583.6 nm(PDI=0.12),结晶呈类球形;室温放置30 d后混悬液粒径急剧增大,而冻干粉粒径无明显变化。纳米结晶溶解度较原药提高了1.64倍。结论:沉淀法制备黄芩苷纳米混悬液简便可行且可显著提高纳米结晶中黄芩苷的溶解度,但工艺条件对纳米结晶粒径及稳定性存在一定影响。Objective： To optimize preparation process of baicalin nanocrystallines and investigate its stability. Method： Taking mean particle size and polydispersity index（PDI） as indicators,preparation process of baicalin nanosuspensions was optimized by single factor tests.Baicalin nanocrystallines was then collected by centrifugation and freeze-dried,morphology of obtained nanocrystals were analyzed,initial stability of nanosuspensions and its freeze-dried powder were also observed.Equilibrium solubility of coarse baicalin and nanocrystals was compared by shaking flask method. Result： Nanosuspensions were prepared by injecting 1 mL of baicalin solution in DMSO（50 g·L-1） into 20 mL of 0.5% lecithin solution by a high shear of 30 000 r·min-1 for 8 min under ice-water bath.These obtained nanocrystals showed an average particle size of 280.6 nm （PDI=0.047） and that of 583.6 nm （PDI=0.12） after freeze-drying,these nanocrystals were investigated as sphere-like particles;Particle size of nanosuspensions increased up to 672.0 nm after stored at room temperature for 30 d,but no significant change was found for freeze-dried powder of nanocrystals.Equilibrium solubility of nanocrystals showed as 1.64-fold of coarse baicalin. Conclusion： Precipitation method showed to be a simple and feasible approach to prepare baicalin nanosuspensions with solubility increased,but more attention should be paid to collection and drying process which affect particle size and stability of nanocrystals.

关 键 词：黄芩苷 纳米结晶 沉淀法 稳定性考察 冷冻干燥工艺 

分 类 号：R283.6[医药卫生—中药学]