布洛芬纳米微粉的制备、表征及体外透皮性研究.pdfVIP

·制剂与工艺· 布洛芬纳米微粉的制备、表征及体外透皮性研究Δ ＊ # 邓怡平 ，赵修华 ，祖元刚，王 璐（东北林业大学森林植物生态学教育部重点实验室，哈尔滨 150040） 中图分类号 R943；R927 文献标志码 A 文章编号 1001-0408（2017）01-0099-04 DOI 10.6039/j.issn. 1001-0408.2017.01.26 摘 要 目的：制备布洛芬纳米微粉并对其进行表征，考察其体外透皮作用。方法：采用乳化法，以氯仿-乙醇（7∶3，V/ V）为有机 相、超纯水为水相、聚山梨酯80为表面活性剂制备布洛芬纳米微粉。利用激光粒度分析方法、扫描电镜、傅里叶变换红外光谱、X 射线衍射、差示扫描对制备的布洛芬纳米微粉进行表征。比较布洛芬纳米微粉与原料药的饱和溶解度、体外溶出度和体外透皮 率。结果：确定的处方及制备工艺为聚山梨酯805mg/mL 、水相-有机相体积比40∶1、布洛芬质量浓度250mg/mL 、匀浆速度5000 r/min 、匀浆时间2min 。所制布洛芬纳米微粉为多孔疏松珊瑚状，其化学结构未改变，由原来的晶体态变为无定形态，粒径为 179.6nm ，载药量为8.99％；其饱和溶解度、溶出度和透皮率分别是原料药的148、1.23、4.08倍。结论：所制布洛芬纳米微粉具有良 好的水溶性和体外透皮性。 关键词 布洛芬；乳化法；纳米微粉；表征；透皮 Preparation ，Characterization and Transdermal Ability Study in vitro of Ibuprofen Nano-powder DENG Yiping ，ZHAO Xiuhua ，ZU Yuangang ，WANG Lu （Key Laboratory of Forest Plant Ecology ，Ministry of Education ，Northeast Forestry University ，Harbin 150040，China ） ABSTRACT OBJECTIVE ：To prepare and characterize Ibuprofen （IBU ）nano-powder ，and to investigate its transdermal ability in vitro. METHODS ：Using chloroform-ethanol （7∶3，V/ V）as organic phase ，deionized water as aqueous phase and polysorbate 80 as surfactant ，the emulsification method was used to prepare IBU nano-powder. Laser granulometric analysis ，Fourier transform in- frared spectroscopy （FT-IR ），X-ray diffraction （XRD ），differential scanning calorimetry （DSC ）were used to characterize IBU na- no-powder. IBU nano-powder was compared with bulk drug in respects of saturation solubility ，dissolution rate and transdermal rate in vitro. RESULTS ：The optimum condition was as follows that the concentration of polysorbate 80 was 5 mg/mL ；the volume ra- tio of water phase-organic phase was 40∶1；the concentration of IBU was 250mg/mL ；homogenate speed was 5000r/min ；homog- enate time was 2 min. Prepared IBU nano-powder was polyporous crumbly coralliform ，and its chemical structure kept stable ；the n