双氯芬酸钠微乳的家兔皮肤刺激性及体外透皮吸收性能评价Δ.PDFVIP

双氯芬酸钠微乳的家兔皮肤刺激性及体外透皮吸收性能评价Δ ＊ 魏 玉 ，苏成福（河南中医学院药学院，郑州 450008） 中图分类号 R943 文献标志码 A 文章编号 1001-0408（2017）04-0490-04 DOI 10.6039/j.issn. 1001-0408.2017.04.16 摘 要 目的：对双氯芬酸钠微乳（DS-ME ）的性质、皮肤刺激性及体外透皮吸收进行考察，探讨其局部外用给药的可行性。方法： 采用紫外分光光度法测定DS-ME 中DS 的含量；采用激光粒度仪测定DS-ME 的粒径分布；家兔皮肤刺激性实验考察DS-ME 和空 白ME 对单次给药正常皮肤、多次给药正常皮肤和单次给药破损皮肤的影响；Franz 扩散池法比较DS-ME 与市售DS 凝胶经小鼠离 体皮肤的透皮参数。结果：所制DS-ME 为O/W 型微乳，粒径为（30.140±9.020）nm ；与空白ME 比较，DS-ME 对家兔皮肤的刺激评 分无明显差异；DS-ME 与市售DS 凝胶的稳态渗透速率分别为34.16、18.62µg/（cm2·h ），渗透系数分别为1.029、0.561cm/h ，滞后时 间分别为0.1242、0.3672h 。结论：DS-ME 的粒径小，无皮肤刺激性，可提高DS 的透皮吸收速率。 关键词 双氯芬酸钠；微乳；皮肤刺激性；透皮吸收 Evaluation of Rabbit Skin Irritation and in vitro Transdermal Absorption of Diclofenac Sodium Microemul- sion WEI Yu ，SU Chengfu（College of Pharmacy ，Henan University of TCM ，Zhengzhou 450008，China ） ABSTRACT OBJECTIVE ：To investigate the property ，skin irritation and in vitro transdermal absorption of Diclofenac sodium microemulsion （DS-ME ），and to explore the feasibility of local external use of it. METHODS ：The content of DS in DS-ME was determined by ultraviolet spectrophotometry. The distribution of particle size was determined by laser particle size analyzer. The ef- 网 fects of DS-ME and blank micro-emulsion on normal skin of single administration ，normal skin of multiple administration and dam- aged skin of single administration were investigated by rabbit skin irritation test. The transdermal parameters of DS-ME and commer- 房 cially available DS gel through isolated skin of mice were compared by Franz diffusion