摘要
目的:采用纳米晶体技术改善抗缺氧新结构化合物7-羟乙基白杨素(7-HEC)的溶解性,制备7-HEC纳米晶体,并进行理化性质表征和释放行为评价。方法:使用反溶剂沉淀结合超声分散法将7-HEC制备成纳米晶体,以平均粒径和PDI作为评价指标,进行单因素试验设计优化处方工艺,经差示扫描量热法(DSC)、X射线衍射法(XRD)对纳米晶体的晶型结构进行表征,并考察其体外释放行为。结果:筛选出7-HEC纳米晶体最佳制备工艺:HPMC和SDS以2∶1的比例作为稳定剂,药载比为2∶1,制得的7-HEC纳米晶体为乳状混悬液,粒径为(281.77±1.32)nm,PDI值为0.17±0.02。纳米化后的7-HEC晶型部分发生了变化,在84 h内,纳米晶体累积释放率达到84.65%,而原料药释放率仅为20.22%。结论:7-HEC纳米晶体粒径小且分布均匀,提高了释放率,这为7-HEC制剂进一步开发提供了依据,具有较好的应用前景。
Objective:Nanocrystal technology was used to improve the solubility of 7-hydroxyethyl chrysin(7-HEC),a new structure compound against hypoxia,and 7-HEC nanocrystals(7-HEC-NC)were prepared,and physicochemical property characterization and release behavior evaluation were performed.Methods:Anti-solvent method was used to prepare the nanocrystals.The formulation and preparation process of the 7-HEC-NC were optimized by the single-factor experimental design with the average particle diameter and PDI as the evaluation index;The particle size and the polydispersity coefficient of the 7-HEC nanocrystals were measured;The crystal structure of NC was characterized by differential scanning calorimetry(DSC)and X-ray powder diffractometry(XRD).In vitro dissolution was also determind.Results:The optimal formulation was as follows:HPMC and SDS were used as stabilizers in a 2∶1 ratio with a 2∶1 drug loading ratio to produce a 7-HEC-NC as an emulsion suspension.The particle size was(281.77±1.32)nm,PDI was 0.17±0.02.Nanosized 7-HEC has a partially altered crystalline shape.The cumulative release rate of the 7-HEC-NC reached 84.65%in 84 h,while the release rate of the API was only 20.22%.Conclusion:The preparation of a small and uniformly distributed particle size of 7-HEC-NC could significantly improve the release rate performance of 7-HEC,which provides a basis for the further development of 7-HEC.
作者
田贻婷
何蕾
石志群
张朋朋
邹蓓蕾
景临林
马慧萍
TIAN Yi-ting;HE Lei;SHI Zhi-qun;ZHANG Peng-peng;ZOU Bei-lei;JING Lin-lin;MA Hui-ping(College of Pharmacy,Gansu University of Chinese Medicine,Lanzhou 730000,China;Key Laboratory of the Plateau Medicine,Pharmacy Department,The 940th Hospital of Joint Logistics Support force of Chinese People’s Liberation Army,Lanzhou 730050,China)
出处
《中华中医药杂志》
CAS
CSCD
北大核心
2023年第6期2883-2888,共6页
China Journal of Traditional Chinese Medicine and Pharmacy
基金
军队卫勤保障能力创新与生成专项计划(No.21WQ045)。
关键词
7-羟乙基白杨素
纳米晶体
单因素试验
反溶剂沉淀法
表征
7-hydroxyethyl chrysin(7-HEC)
Nanocrystals
Single factor test
Anti-solvent precipitation method
Characterization
