载体材料对汉防己甲素固体分散体性质的影响
Effect of carrier materials on properties of tetrandrine solid dispersions
冯唐德 1欧丽泉 1赵国巍 1敖腾 1张俊芳 1蔡萍1
作者信息
- 1. 江西中医药大学现代中药制剂教育部重点实验室,南昌 330004
- 折叠
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-Solu-plus®-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.
Abstract
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.
关键词
汉防己甲素/固体分散体/溶出/表面自由能/铺展系数Key words
tetrandrine/solid dispersion/dissolution/surface free energy/spreading coefficient引用本文复制引用
基金项目
江西省中医药局科技项目(2023A0374)
江西省卫生健康委科技项目(202211402)
江西中医药大学中药制剂技术与装备创新团队项目(CXTD22006)
出版年
2024
NETL
NSTL
维普
万方数据