摘要
目的:研究载体材料对汉防己甲素(TET)-固体分散体(SD)性质的影响。方法:分别以聚乙烯吡咯烷酮K30(PVPK30)、羟丙基甲基纤维素55(HPMC55)和Soluplus^(■)为载体材料,按TET-载体材料1∶4的质量比,采用喷雾干燥法制备了TET-SD,并对TET-SD的理化性质及溶出行为进行研究。结果:理化性质研究结果表明,3种TET-SD均为无定形态,药物和载体材料之间存在分子间相互作用,水接触角减小,粉体均为表面光滑的球形,粉体粒径显著减小。统计分析结果表明,TET-PVPK30-SD和TET-HPMC55-SD中TET的溶出行为与相应的物理混合物(PM)相比没有显著差异,TET-Soluplus^(■)-SD中TET的溶出行为与TET-Soluplus^(■)-PM相比显著改善。结论:3种无定形状态TET-SD对TET溶出行为的改善存在显著差异,可能是由于TET-PVPK30-SD的表面自由能极性成分含量和铺展系数与相应的TET-PVPK30-PM相近,使TET-PVPK30-SD中TET的溶出行为与TET-PVPK30-PM中TET的溶出行为相比没有显著差异;TET-HPMC55-SD的铺展系数较小,使TET在TET-HPMC55-SD中分散不均匀,可能存在相分离,影响了TET的溶出。
Objective:This work aimed to study the effect of carrier materials on the properties of tetrandrine-solid dispersion(TET-SD).Methods:TET-SD was prepared by spray drying method using polyvinylpyrrolidone(PVPK30),hydroxypropyl methylcellulose 55(HPMC55) and Soluplus^(■) as carrier materials at a mass ratio of 1∶4.The physicochemical properties and dissolution of TET-SD were studied.Results:The results of physicochemical properties showed that all the three TET-SDs were amorphous.Since there was intermolecular interaction between the drug and the carrier materials,the water contact angle was reduced,the powder indicated a smooth spherical surface,and the particle size of the powder significantly reduced.The statistical analysis showed that the dissolution behaviors of TET in TET-PVPK30-SD and TET-HPMC55-SD were not significantly different from that of the corresponding physical mixture(PM),and the dissolution of TET in TET-Soluplus^(■)-SD was significantly improved compared with that in TET-Soluplus^(■)-PM.Conclusion:The three amorphous TET-SDs have significant differences in the improvement of TET dissolution,which may be due to the following reasons:the content of surface free energy polar component and spreading coefficient of TET-PVPK30-SD are similar to that of TET-PVPK30-PM,making no significant difference between the dissolution behavior of TET in TET-PVPK30-SD and that in TET-PVPK30-PM.The spread coefficient of TET-HPMC55-SD is small,making the TET in the TET-HPMC55-SD disperse inhomogeneously and phase separation exist,which affects the dissolution of TET.
作者
冯唐德
欧丽泉
赵国巍
敖腾
张俊芳
蔡萍
FENG Tang-de;OU Li-quan;ZHAO Guo-wei;AO Teng;Zhang Jun-fang;CAI Ping(Key Laboratory of Modern Chinese Medicine Preparation,Ministry of Education,Jiangxi University of Traditional Chinese Medicine,Nanchang 330004,China)
出处
《中国新药杂志》
CAS
CSCD
北大核心
2024年第7期714-721,共8页
Chinese Journal of New Drugs
基金
江西省中医药管理局科技计划项目(2023A0374)
江西省卫生健康委科技计划资助项目(202211402)
江西中医药大学中药制剂技术与装备创新团队资助项目(CXTD22006)。
关键词
汉防己甲素
固体分散体
溶出
表面自由能
铺展系数
tetrandrine
solid dispersion
dissolution
surface free energy
spreading coefficient
作者简介
冯唐德,男,硕士研究生,主要从事药物新剂型与新技术研究。联系电话:(0791)87118658,E-mail:1213164283@qq.com;通讯作者:赵国巍,女,博士,副教授,主要从事药物新剂型与新技术研究。联系电话:(0791)87118658,E-mail:weiweihaoyunqi@163.com。
