粉防己碱固体分散体的制备及体外评价
Preparation and in vitro evaluation of tetrandrine solid dispersion
杨岚 1常金花 1刘沛 1马帅 1刘喜纲 1王汝兴1
作者信息
- 1. 承德医学院中药研究所/河北省中药研究与开发重点实验室,河北承德 067000
- 折叠
摘要
目的:制备粉防己碱(tetrandrine,TET)固体分散体(solid dispersion,SD),以增加TET的溶解度及体外溶出度.方法:以PVPVA64为载体,通过溶剂法制备TET-SD,分别以差示扫描量热法(DSC)、X-射线衍射法(XRD)、傅立叶变换红外光谱法(FTIR)、扫描电镜(SEM)以及热重分析(TG)对TET原料药及TET-SD进行表征,并研究其理化性质及体外溶出度.结果:DSC、XRD、FTIR、SEM和TG的结果显示,所制备的TET-SD处于无定型状态,TET与PVPVA64之间存在分子间相互作用.TET-SD在120 min内的体外累积溶出度为92.95％,与TET和二者的物理混合物相比,体外溶出度在120 min内显著提高.结论:TET-SD的制备方法简单、可靠,提高了 TET的体外溶出度.
Abstract
OBJECTIVE To prepare tetrandrine(TET)solid dispersion(SD)to boost the solubility and in vitro dissolution of TET.METHODS After preparation by solvent method with PVPVA64,TET-SD was characterized by differential scanning calorimetry(DSC),X-ray diffraction(XRD),Fourier transform infrared spectroscopy(FTIR),scanning electron microscopy(SEM),glass transition temperature(TG)and dissolution in vitro.And physicochemical properties and dissolution in vitro were examined.RESULTS The results of DSC,XRD,FTIR,SEM and TG indicated that prepared TET-SD was amorphous and intermolecular interaction existed between TET and PVPVA64.In vitro cumulative dissolution of TET-SD within 120 min was 92.95％.As compared with physical mixture of TET-SD and TET,dissolution rate spiked markedly within 120 min and water contact angle shrank.CONCLUSION The preparation method of TET-SD is both simple and reliable.And dissolution rate in vitro of TET improves.
关键词
粉防己碱/固体分散体/制备工艺/质量评价Key words
tetrandrine/solid dispersion/preparation technology/quality assessment引用本文复制引用
基金项目
河北省高等学校科学技术研究重点项目(ZD2021004)
河北省自然科学基金中医药联合基金培育项目(H2022406073)
承德医学院高层次人才科研启动基金(201705)
出版年
2024
NETL
NSTL
万方数据