丹皮酚微乳的制备及经皮吸收研究应用.docVIP

丹皮酚微乳制备及经皮吸收研究 韩盈，刘继勇，李凤前，彭程，孙华君，胡晋红作者介绍：韩盈（1983-），女，汉族，硕士硕士。E-mail:。 作者介绍：韩盈（1983-），女，汉族，硕士硕士。E-mail:。 通讯作者：Tel:，Fax:，E-mail: 。 （第二军医大学 长海医院 药学部，上海 33） 摘要：选择适宜百分比油相、表面活性剂、助表面活性剂、水相制备丹皮酚微乳制剂以增加药品溶解度和经皮渗透量，优化处方，并对其理化性质进行研究。经过绘制伪三元相图研究形成O/W微乳区域和能力；以单位面积累积渗透量为指标，优化处方；并考察了制剂外观、形态、粒径分布等理化性质。处方选择肉豆蔻酸异丙酯（IPM）为油相，lecithin为表面活性剂，聚氧乙烯辛基苯基醚（OP）为助表面活性剂；微乳中Lecithin和OP百分比为3∶7时，O/W微乳区最大，确定了5个处方。经过处方筛选确定了最好处方，制备出澄清透明、平均粒径为（58.2±5.0）nm丹皮酚微乳制剂。 关键词：丹皮酚；微乳；伪三元相图；经皮给药；体外评价 Preparation and in vitro transdermal permeation of paeonol microemulsion Han-Ying，LIU Ji-Yong，Li Feng-Qian，Peng-Cheng，SUN Hua-jun，HU Jin-Hong* (Department of Pharmacy，Changhai Hospital，Second Military Medical University，Shanghai 33，China) Abstract: To prepare the microemulsion of paeonol in order to increase solubility and its in vitro transdermal delivery by using appropriate proportion of oil，surfactant(S)，cosurfactant(CoS) and water．The formulation of proportion was optimized．The physicochemical properties of the microemulsion was studied. Pseudo—tertiary phase diagrams were prepared to obtain the area and ability of O/W microemulsion formation. Using in vitro cumulative amount permeated as index, optimize the formulation of microemulsion. The physicochemical properties including appearance, particle size distribution and shape were examined. IPM was selected as oil, lecithin and OP were used as surfactant and cosurfactant, repectively. In microemulsion, when the ratio of lecithin and OP was 3:7, the area of O/W microemulsion was largest, meanwhile obtain 5 formulations. Through the screening of formulations, the optimized formulation was obtained. Prepare the clear paeonol microemulsion, the a particle size distribution was（58.2±5.0）nm. Key words: paeonol; microemulsion; Pseudo—tertiary phase diagrams; transdermal delivery system; in vitro evaluation 微乳（microemulsion，ME）作为一个新型经皮给药载体，是由水相、油相、表面活性剂和助表面活性剂在合适百分比自发形成一个透明或半透明各向同性且热力学稳定体系，其粒径通常为10～100nm。微乳作为经皮给药载体，含有增加亲脂性或亲水性药品溶解度、提升药品透皮速率、维持恒定有效血药浓度等优点。 丹皮酚(Paeonol