首页|载体材料对汉防己甲素固体分散体性质的影响

载体材料对汉防己甲素固体分散体性质的影响

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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.
Effect of carrier materials on properties of tetrandrine solid dispersions
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.

tetrandrinesolid dispersiondissolutionsurface free energyspreading coefficient

冯唐德、欧丽泉、赵国巍、敖腾、张俊芳、蔡萍

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江西中医药大学现代中药制剂教育部重点实验室,南昌 330004

汉防己甲素 固体分散体 溶出 表面自由能 铺展系数

江西省中医药局科技项目江西省卫生健康委科技项目江西中医药大学中药制剂技术与装备创新团队项目

2023A0374202211402CXTD22006

2024

中国新药杂志
中国医药科技出版社 中国医药集团总公司 中国药学会

中国新药杂志

CSTPCD北大核心
影响因子:1.039
ISSN:1003-3734
年,卷(期):2024.33(7)
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