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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 |
| 阅读数： | 313 次 |
| 本月下载数： | 2 次 |
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