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

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.