他莫昔芬磁性微球的制备及体外评价  

The preparation and in vitro evaluation of Tamoxifen loaded magnetic microspheres

作　　者：刘让如[1] 陈德梅[1] 黄艳[1] 王勇[1] 张俊清[1] 

机构地区：[1]海南医学院药学院海南省热带药用植物研究开发重点实验室,海南海口571101

出　　处：《华西药学杂志》2012年第3期250-252,共3页West China Journal of Pharmaceutical Sciences

基　　金：海南省自然科学基金(No.309028)

摘　　要：目的制备他莫昔芬磁性微球,并考察其性质和体外释放行为。方法采用乳化化学交联二步法制备他莫昔芬磁性微球,并利用扫描电子显微镜、激光散射技术、多晶X-射线衍射仪、热重分析仪、紫外光谱、红外光谱等手段表征他莫昔芬磁性微球的外貌、粒径、结构、药物包封、Fe含量、磁响应性等,并用动态恒温振荡结合HPLC法考察其体外释药行为。结果所得磁性微球为灰色粉末状固体,呈球形,粒径呈近正态分布,Fe含量为1.9%,体外释放曲线用Higuchi方程拟合为:Q=38.386t1/2+20.162(r=0.9769),具有明显的缓释特性。微球经约10 min磁分离后,透光率可达96%以上,磁响应性能好。结论乳化化学交联二步法制备他莫昔芬磁性微球工艺简易可行,有明显的缓释特性和较强的磁响应性,为他莫昔芬靶向制剂的研究奠定了基础。OBJECTIVE To prepare and characterize Tamoxifen loaded magnetic microspheres and investigate its release in vitro.METHODS The microspheres were prepared by emulsion cross-linking and two-step techniques and characterized by scanning electron microscopy,laser scattering technique,X-ray diffraction,thermogravimetic analyzer,UV and FT-IR.The release of drug from microspheres in vitro was performed by dynamic thermostatic oscillation and HPLC.RESULTS The results showed microspheres followed normal distribution.The release curve fitted Higuchi equation：Q=38.386t1/2＋20.162（r=0.9769）,which would ensure desirable sustained-release character.The content of Fe in microspheres was 1.9%.After about 10 min of magnetic separation,the transmittance of microspheres solution attached to 96%,which manifested that microspheres were of strong magnetic responsiveness.CONCLUSION The process of the microspheres was simple and feasible.The microspheres exerted desirable release characteristics and strong magnetic responsiveness,which laid a foundation for targeting preparations of Tamoxifen.

关 键 词：他莫昔芬 磁性微球 表征 体外释放 

分 类 号：R94[医药卫生—药剂学]