甘草酸为稳定剂的葛根素纳米乳冻干粉的制备及体外评价  

Preparation and in vitro evaluation of puerarin nanoemulsion lyophilized powder with glycyrrhizic acid as stabilizer

作　　者：张琳琳 李小芳[1] 宋佳文 谢龙 廖艳梅 仲粒 ZHANG Lin-lin;LI Xiao-fang;SONG Jia-wen;XIE Long;LIAO Yan-mei;ZHONG Li(College of Pharmacy,Chengdu University of Traditional Chinese Medicine,Key Laboratory of Standardization of Chinese Herbal Medicine,Ministry of Education,Key Laboratory of Systematic Research,Development and Utilization of Chinese Medicine Resources in Sichuan Province,State Key Laboratory Breeding Base of Co-founded by Sichuan Province and Ministry of Science and Technology,Chengdu 611137,China)

机构地区：[1]成都中医药大学药学院中药材标准化教育部重点实验室四川省中药资源系统研究与开发利用重点实验室省部共建国家重点实验室培育基地,四川成都611137

出　　处：《中草药》2020年第11期2929-2936,共8页Chinese Traditional and Herbal Drugs

基　　金：四川省科技厅科研项目(2019YFS0113);国家中医药管理局项目(2018ZY03002)。

摘　　要：目的以天然表面活性剂甘草酸为稳定剂制备葛根素纳米乳冻干粉(puerarinnanoemulsionlyophilizedpowder,Pue-NE-LP),并对其进行体外评价。方法采用高速剪切联合高压均质法制备葛根素纳米乳(Pue-NE),进一步结合冷冻干燥法制备Pue-NE-LP。以平均粒径和多分散指数(PDI)作为评价指标,通过单因素试验筛选出最优处方及工艺参数。并对制备的Pue-NE-LP进行理化性质表征和体外溶出度测定。结果以5%辛癸酸甘油酯为油相,2.0 mg/mL甘草酸为稳定剂,7%葡萄糖为冻干保护剂制得的Pue-NE-LP平均粒径为(215.1±0.7)nm,PDI为0.133±0.024。扫描电镜显示Pue-NE-LP呈不规则的小片状,大小较均匀;X射线衍射显示Pue-NE-LP呈无定型状态存在。体外释放结果表明Pue-NE-LP的溶出度明显高于物理混合物。结论以天然表面活性剂甘草酸为稳定剂制备的Pue-NE-LP,不仅制备方法简单,而且能显著改善Pue的溶解性和生物利用度,为Pue-NE制剂的多元开发提供参考。Objective Puerarin nanoemulsion lyophilized powder(Pue-NE-LP) was prepared using natural surfactant glycyrrhizic acid as stabilizer and evaluated in vitro. Methods Pue-NE was prepared by high-speed shear and high-pressure homogenization method, and further combined with freeze-drying method to prepare Pue-NE-LP. Taking the average particle size and polydispersity index(PDI) as the evaluation indexes, the optimal prescription and process parameters of this experiment were screened out through a single factor test. The prepared Pue-NE-LP was characterized by physicochemical properties and dissolution in vitro. Results The average particle size and PDI of Pue-NE-LP prepared with 5% glyceryl caprylate as oil phase, 2.0 mg/mL glycyrrhizic acid as stabilizer, and 7% glucose as lyophilization protectant was(215.1 ± 0.7) nm and(0.133 ± 0.024), respectively. Scanning electron microscopy showed that Pue-NE-LP was irregularly small and uniform in size;X-ray diffraction showed that Pue-NE-LP existed in an amorphous state. In vitro release results showed that the dissolution rate of Pue-NE-LP was significantly higher than the physical mixture. Conclusion Pue-NE-LP prepared with natural surfactant glycyrrhizic acid as a stabilizer is not only simple to prepare, but also can significantly improve the solubility and bioavailability of puerarin. It provides a reference for the multiple development of Pue-NE formulations.

关 键 词：葛根素 甘草酸 天然表面活性剂 稳定剂 纳米乳 冻干粉 体外溶出 高速剪切联合高压均质法 冷冻干燥法 冻干保护剂 

分 类 号：R283.6[医药卫生—中药学]