丹皮酚微的制备及经皮吸收研究.docVIP

丹皮酚微乳的制备及经皮吸收研究摘要：选择适宜比例的油相、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物溶解度和经皮渗透量，优化处方，并对其理化性质进行研究。通过绘制伪三元相图研究形成O/W微乳的区域和能力；以单位面积累积渗透量为指标，优化处方；并考察了制剂的外观、形态、粒径分布等理化性质。处方选用肉豆蔻酸异丙酯（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与OP比例为37时，O/W微乳区最大，确定了5个处方。通过处方筛选确定了最佳处方，制备出澄清透明、平均粒径为（58.2±5.0）nm的丹皮酚微乳制剂。 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 microemulsionAbstract: 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）作为一种新型经皮给药的载体，是由水相、油相、表面活性剂和助表面活性剂在适当的比例自发形成的一种透明或者半透明的各向同性的且热力学稳定的体系，其粒径一般为10～100nm。微乳作为经皮给药载体，具有增加亲脂性或亲水性药物的溶解度、提高药物的透皮速率、维持恒定的有效血药浓度等优点。 丹皮酚(Paeonol,Pae)又称牡丹酚，是毛茛科植物牡丹（Paeonia suffruticosa Andr.）根皮和萝摩科植物徐长卿 Pycnostelma Paniculatum (Bunge)K . Schu全草的主要活性成分，具有镇静、催眠、解热、镇痛、抗炎、抗过敏、抗菌等多种药理活性。上市的剂型主要是丹皮酚注射剂，丹皮酚片以及丹皮酚软膏。临床上用于治疗风湿痛、胃痛和其他疼痛、湿疹、过敏性皮炎等，具有较好疗效。丹皮酚用于经皮给药，克服了治疗湿疹、过敏性皮炎等传统激素类药物副作用大的缺点，而且它作为中药单体具有毒副作用低等优越性。 为了克服丹皮酚水溶性差、熔点低、易挥发、稳定性差等缺陷，本研究尝试将