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
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篇名: 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
TITLE:
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、18.62 μg/(cm2·h),渗透系数分别为1.029、0.561 cm/h,滞后时间分别为0.124 2、0.367 2 h。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。
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 effects of DS-ME and blank micro-emulsion on normal skin of single administration, normal skin of multiple administration and damaged skin of single administration were investigated by rabbit skin irritation test. The transdermal parameters of DS-ME and commercially available DS gel through isolated skin of mice were compared by Franz diffusion cell. RESULTS: The prepared DS-ME was O/W microemulsion with particle size of (30.140±9.020) nm. Compared with blank ME, DS-ME had no significant difference in rabbit skin irritation score. Steady permeation rates of DS-ME and commercially available DS gel were 34.16 and 18.62 μg/(cm2·h), respectively; the permeation coefficient of them were 1.029 and 0.561 cm/h; the delay time were 0.124 2 and 0.367 2 h. CONCLUSIONS: The particle size of DS-ME is small and not irritant to skin, and can improve  transdermal absorption rate of DS.
期刊: 2017年第28卷第4期
作者: 魏玉,苏成福
AUTHORS: WEI Yu,SU Chengfu
关键字: 双氯芬酸钠;微乳;皮肤刺激性;透皮吸收
KEYWORDS: Diclofenac sodium; Microemulsion; Skin irritation; Transdermal absorption
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