延胡索乙素纳米混悬剂制备及体外评价  

Preparation and in Vitro Evaluation of Tetrahydropalmatine Nanosuspension

作　　者：胡宇峰 马思媛 王梦琳 魏晓彤 石双慧 姜明瑞 王慧楠 张婧秋 刘芊芊 张新宁 王英姿[1] HU Yufeng;MA Siyuan;WANG Menglin;WEI Xiaotong;SHI Shuanghui;JIANG Mingrui;WANG Huinan;ZHANG Jingqiu;LIU Qianqian;ZHANG Xinning;WANG Yingzi(Beijing University of Chinese Medicine,Beijing 102488,China)

机构地区：[1]北京中医药大学,北京102488

出　　处：《辽宁中医药大学学报》2024年第8期18-24,共7页Journal of Liaoning University of Traditional Chinese Medicine

基　　金：国家重点研发计划项目(2018YFE0197900);国家中医药管理局高水平建设学科项目(zyyzdxk-2023272)。

摘　　要：目的制备延胡索乙素纳米混悬剂(THP-NS)及其冻干粉,并对其进行体外评价。方法通过沉淀-均质法制备延胡索乙素纳米混悬剂,在单因素实验基础上,以粒径与多分散系数(PDI)的归一值作为考察指标,考察延胡索乙素用量、透明质酸钠用量、泊洛沙姆407用量对纳米混悬剂制备的影响,通过Box-Behnken设计响应面法优化THP-NS的处方工艺,并制备冻干粉末。采用透射电镜法(TEM)、差示扫描量热法(DSC)、X射线衍射(XRD)、傅里叶变换红外光谱法(FT-IR)对THP-NS进行表征,透析袋法评价其体外溶出度。结果延胡索乙素纳米混悬剂最佳处方为延胡索乙素用量51.0 mg,透明质酸钠用量3.1 mg,泊洛沙姆407用量18.4 mg。平均粒径为(195.57±1.80)nm,PDI为0.23±0.019,与Box-Behnken响应面法预测值接近。Zeta电位值为-31.0 mV,延胡索乙素纳米混悬剂外貌为球形,THP-NS中延胡索乙素以结晶状态存在,THP-NS在24 h累积溶出度达到97.43%。结论将延胡索乙素制备成纳米混悬剂药物处方设计合理、工艺可行,显著提高了其体外溶出率。Objective To prepare tetrahydropalmatine nanosuspension and lyophilized powder,and perform in vitro evaluation.Methods A precipitation homogenization method was used to prepare tetrahydropalmatine nanosuspension.Based on single factor experiments,overall values of average particles size and polydispersity index(PDI)were employed as evaluation indexes,the dosage of tetrahydropalmatine,sodium hyaluronate,and Poloxam 407 as the influencing facters.Box-Behnken response surface design method was employed to investigate the optimal prescriptions of tetrahydropalmatine nanosuspension,and the freeze-dried powder was prepared.THP-NS was characterized by transmission electron microscope(TEM),transmission electron microscopy(DSC),X-ray powder diffraction(XRD)and fourier transform infrared spectroscopy(FT-IR).Dissolution of tetrahydropalmatine nanosuspension were determined by dialysis bag method.Results Optimal formulation of tetrahydropalmatine nanosuspension:tetrahydropalmatine dosage 51.0 mg,sodium hyaluronate dosage 3.1 mg,and poloxamer 407 dosage 18.4 mg.Average particle size was(195.57±1.80)nm,PDI was(0.229±0.019),which were close to that of predicted values.Zeta potential was-31.0 mV.Tetrahydropalmatine existed in an crystalline state in THP-NS.Appearances of tetrahydropalmatine nanosuspension were spherical,and cumulative dissolution was reached 97.43%in 24 h.Conclusion The design of the drug prescription to prepare the nanosuspension with tetrahydropalmatine is reasonable and the technology is feasible,the dissolution rate was significantly improved.

关 键 词：延胡索乙素 纳米混悬剂 Box-Behnken响应面设计 累计溶出度 

分 类 号：R283[医药卫生—中药学]