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

作　　者：杨岚[1] 常金花[1] 刘沛[1] 马帅[1] 刘喜纲[1] 王汝兴[1] YANG Lan;CHANG Jinhua;LIU Pei;MA Shuai;LIU Xigang;WANG Ruxing(Institute of Chinese Mate-ria Medica,Chengde Medical University,Hebei Province Key Laboratory of Research&Development for Chinese Materia Medica,Hebei Chengde 067000,China)

机构地区：[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

出　　处：《中国医院药学杂志》2024年第20期2340-2345,共6页Chinese Journal of Hospital Pharmacy

基　　金：河北省高等学校科学技术研究重点项目(编号:ZD2021004);河北省自然科学基金中医药联合基金培育项目(编号:H2022406073);承德医学院高层次人才科研启动基金(编号:201705)。

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。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 

分 类 号：R943[医药卫生—药剂学]