Hui-Rong X I, Hui-Ping M A, Ke-Ming Chen, Xiao-Shuan Liu
Pharmacy Department, Gansu Provincial Hospital of Traditional Chinese Medicine Lanzhou 730000, China.
the 940 Hospital of Joint Logistic Support Force of Chinese People's Liberation Army Lanzhou 730050, China.
Zhongguo Zhong Yao Za Zhi. 2020 Oct;45(20):4902-4908. doi: 10.19540/j.cnki.cjcmm.20200328.301.
The optimal process conditions for preparing icariin nanosuspension(ICA-NS) and lyophilized powder were determined to initially investigate their stability and characterize the prepared nanosuspension. The anti-solvent precipitation-high shear method was used in the experiment, and the particle size(size), polydispersity index(PDI), and sedimentation ratio(H_0/H) were used as indicators to determine the optimal process conditions of ICA-NS by single-factor test method. Lyophilized powder of nanosuspension was prepared by freeze-drying method, and its crystalline morphology was observed by transmission electron microscope. The equilibrium solubility of icariin, nanosuspension and lyophilized powder was determined by shake flask method and their stability was initially investigated. The crystal structure of nano-lyophilized powder was characterized by differential scanning calorimetry(DSC) and X-ray powder diffraction(XRD). Finally, the dissolution in vitro of nano-lyophilized powder was determined by the small cup method to prepare the ideal icariin nanoparticles. Soy lecithin(SPC) was used as the main stabilizer and povidone was used as the steric stabilizer. The prepared ICA-NS was nearly round in shape, uniform in size, and stable at room temperature. The average particle size was(62.51±7.11) nm. The drug loading was 16% and the solubility was 50 times higher than that of the original drug. Drugs in suspension and lyophilized powder were dispersed in nanoparticles in an amorphous state. The in vitro dissolution experiments showed that the cumulative release rate of nano-lyophilized powder reached 100% at 10 min, indicating that the dissolution rate of lyophilized powder was significantly increased after preparing into nano-lyophilized powder. Preparation of ICA-NS lyophilized powder by antisolvent precipitation-high shear method is simple, easy to operate, and can significantly improve its water solubility. However, the process conditions have some influence on its stability, which needs further study.
为初步研究淫羊藿苷纳米混悬液（ICA - NS）及其冻干粉末的稳定性并对所制备的纳米混悬液进行表征，确定了制备淫羊藿苷纳米混悬液和冻干粉末的最佳工艺条件。实验采用抗溶剂沉淀 - 高剪切法，以粒径（size）、多分散指数（PDI）和沉降比（H_0/H）为指标，通过单因素试验法确定ICA - NS的最佳工艺条件。采用冷冻干燥法制备纳米混悬液的冻干粉末，用透射电子显微镜观察其晶体形态。采用摇瓶法测定淫羊藿苷、纳米混悬液和冻干粉末的平衡溶解度，并初步考察其稳定性。用差示扫描量热法（DSC）和X射线粉末衍射（XRD）对纳米冻干粉末的晶体结构进行表征。最后，采用小杯法测定纳米冻干粉末的体外溶出度，以制备理想的淫羊藿苷纳米粒。以大豆卵磷脂（SPC）为主要稳定剂，聚维酮为空间稳定剂。所制备的ICA - NS形状近似圆形，粒径均匀，在室温下稳定。平均粒径为（62.51±7.11）nm。载药量为16%，溶解度比原药高50倍。混悬液和冻干粉末中的药物以无定形状态分散在纳米粒中。体外溶出实验表明，纳米冻干粉末在10 min时累积释放率达到100%，表明制备成纳米冻干粉末后冻干粉末的溶出速率显著提高。采用抗溶剂沉淀 - 高剪切法制备ICA - NS冻干粉末方法简单、易于操作，可显著提高其水溶性。然而，工艺条件对其稳定性有一定影响，有待进一步研究。
