姜黄素微球中药物存在形式与释药行为的关系研究  

Relation between drug release and the drug status within curcumin-loaded microsphere

作　　者：陈德[1] 刘意[2] 范凯燕 谢依侨 俞安安 夏自花 杨帆[1] 

机构地区：[1]广东药学院药科学院,广东广州510006 [2]广东药学院医药化工学院,广东广州510006

出　　处：《药学学报》2016年第1期140-146,共7页Acta Pharmaceutica Sinica

基　　金：广东省科技厅重大项目资助项目(2011A080504003)

摘　　要：为了研究姜黄素微球中药物的存在形式及其与微球释药行为的关系,本文以聚乳酸-羟基乙酸共聚物(PLGA)为载体材料,使用SPG(shirasu porous glass)膜乳化装置制备了高、中、低3种载药量的姜黄素微球,并使用高效液相色谱法(HPLC)对3批微球的体外释放情况进行了研究。利用扫描电镜(SEM)对3批微球的形貌进行了观察,同时利用X-射线粉末衍射(XRD)、差示扫描量热仪(DSC)和红外光谱(IR)对微球中姜黄素的存在形式进行研究。制备的3批微球的载药量分别为(5.85±0.21)%、(11.71±0.39)%和(15.41±0.40)%,姜黄素与PLGA之间并未发生化学连接。在载药量最低的微球中,姜黄素以无定形的非晶体状态分散在PLGA中,但载药量较高的两批微球中分别出现(2.12±0.64)%和(5.66±0.07)%药物结晶。结果发现,不同载药量的微球中姜黄素的存在形式不尽相同,同时这种区别也导致了3批微球的体外释放呈现梯度式差异。To study the relation between drug release and the drug status within curcumin-loaded microsphere, SPG（shirasu porous glass） membrane emulsification was used to prepare the curcumin-PLGA（polylactic-co-glycolic acid） microspheres with three levels of drug loading respectively, and the in vitro release was studied with high-performance liquid chromatography（HPLC）. The morphology of microspheres was observed with scanning electron microscopy（SEM）, and the drug status was studied with X-ray diffraction（XRD）, differential scanning calorimetry（DSC） and infrared analysis（IR）. The drug loading of microspheres was（5.85 ± 0.21） %,（11.71 ± 0.39） %,（15.41 ± 0.40） %, respectively. No chemical connection was found between curcumin and PLGA. According to the results of XRD, curcumin dispersed in PLGA as amorphous form within the microspheres of the lowest drug loading, while（2.12 ± 0.64） % and（5.66 ± 0.07） % curcumin crystals was detected in the other two kinds of microspheres, respectively, indicating that the drug status was different within three kinds of microspheres. In the data analysis, we found that PLGA had a limited capacity of dissolving curcumin. When the drug loading exceeded the limit, the excess curcumin would exist in the form of crystals in microspheres independently. Meanwhile, this factor contributes to the difference in drug release behavior of the three groups of microspheres.

关 键 词：姜黄素 聚乳酸-羟基乙酸共聚物 微球 体外释放 晶体 

分 类 号：R943[医药卫生—药剂学]