基于多组分评价的雷公藤提取物固体分散体的制备及体外表征  

Preparation and characterization of solid dispersion in vitro from extract of Tripterygium wilfordii based on multi-component evaluation

作　　者：霍涛涛 张美敬[1,2] 陶春 杨海跃 孙欣荣[1,4] 刘志宏[1] 宋洪涛[1] 

机构地区：[1]福州总医院药学科,福建福州350025 [2]福建医科大学药学院,福建福州350108 [3]厦门大学医学院,福建厦门361102 [4]福建中医药大学药学院,福建福州350122

出　　处：《中草药》2018年第1期128-134,共7页Chinese Traditional and Herbal Drugs

基　　金：福州总医院院立课题(2016L02);福建省科技计划重大项目(2012I1001)

摘　　要：目的制备雷公藤提取物(ETW)固体分散体(ETW-SD),提高其体外溶出度。方法通过溶剂-熔融法,以聚乙二醇6000(PEG 6000)、泊洛沙姆188(F68)为载体制备ETW-SD。以雷公藤甲素、雷公藤内酯酮、雷公藤次碱、雷公藤红素以及雷公藤内酯甲为评价指标,通过体外溶出度、电子扫描电镜(SEM)、差示热量扫描(DSC)和X-射线衍射(XRD)对ETW-SD进行表征。结果 ETW-SD的最优处方为ETW-PEG 6000-F68(1∶2∶1)。与原料药相比,在60 min内雷公藤内酯酮、雷公藤甲素的溶出度分别提高了3.32倍,雷公藤次碱提高了2倍,而雷公藤红素和雷公藤内酯甲的溶出度均达到83%以上。Objective To improve the dissolution in vitro, thereby to prepare the solid dispersion（SD） from the extract of Tripterygium wilfordii（ETW）. Methods Polyethylene glycol 6000（PEG 6000） and poloxamer 188（F68） were used as carrier to prepare ETW-SD by solvent-melting method. The triptolide, triptonide, wilforine, tripterine and wilforlide were used as the evaluation indexes to characterize the optimal prescription of ETW-SD by dissolution in vitro, scanning electron microscopy（SEM）, differential scanning calorimetry（DSC）, and X-ray diffraction（XRD）. Results The optimal formulation for ETW-SD composed of ETW-PEG 6000-F68（1∶2∶1）. Compared with the raw materials, the dissolution of triptonide, triptolide and wilforine increased by a factor of 3.32, and wilforine by 2 times, while the dissolution of tripterine and wilforlide reached more than 83% within 60 min.

关 键 词：雷公藤 雷公藤甲素 雷公藤内酯酮 雷公藤次碱 雷公藤红素 雷公藤内酯甲 体外溶出度 XRD SEM 固体分散体 

分 类 号：R283.6[医药卫生—中药学]