水杨酸微乳的制备及其体外透皮吸收研究

发布时间：2019-01-02 20:47

【摘要】：目的:制备水杨酸微乳并考察其对离体小鼠皮肤经皮吸收的影响。方法:以聚山梨酯80为乳化剂、丙二醇为助乳化剂、油酸乙酯为油相,通过伪三元相图确定微乳的处方。采用激光粒度分析仪测定微乳的粒径分布;采用紫外分光光度法测定水杨酸含量;采用Franz扩散池法比较所制备的水杨酸微乳与市售水杨酸软膏的体外透皮速率。结果:水杨酸微乳的处方为5%水杨酸、6.8%油酸乙酯、32.4%混合乳化剂(聚山梨酯80-丙二醇之比为4∶1)。所制得的水杨酸微乳为O/W型微乳,粒径为(70.35±17.78)nm;其与市售水杨酸软膏的稳定渗透速率分别为(573.72±8.94)、(310.52±7.11)μg/(cm2·h),渗透系数分别为(1.588±0.019)、(0.430±0.001 2)cm/h,前者为后者的3.69倍;水杨酸微乳的透皮吸收行为符合零级动力学释放规律。结论:所制水杨酸微乳可促进水杨酸的透皮吸收,为制备胃肠道刺激性小、生物利用度高的水杨酸新剂型提供一定的理论依据。
[Abstract]:Aim: to prepare salicylic acid microemulsion and to investigate the effect of salicylic acid microemulsion on percutaneous absorption of mouse skin in vitro. Methods: using polysorbate 80 as emulsifier, propylene glycol as co-emulsifier and ethyl oleate as oil phase, the formulation of microemulsion was determined by pseudo-ternary phase diagram. The particle size distribution of microemulsion was measured by laser particle size analyzer, the content of salicylic acid was determined by ultraviolet spectrophotometry, and the transdermal rate of salicylic acid microemulsion and salicylic acid ointment was compared with that of salicylic acid ointment by Franz diffusion cell method in vitro. Results: the formulation of salicylic acid microemulsion was 5% salicylic acid, 6.8% ethyl oleate and 32.4% mixed emulsifier (the ratio of polysorbate 80 to propylene glycol was 4:1). The salicylic acid microemulsion is O / W microemulsion with particle size of (70.35 卤17.78) nm;. The stable osmotic rate of salicylic acid ointment and salicylic acid ointment were (573.72 卤8.94), (卤310.52 卤7.11) 渭 g / (cm2 h), osmotic coefficient was (1.588 卤0.019), (0.430 卤0.001 2) cm/h, respectively). The former was 3.69 times of the latter. The transdermal absorption behavior of salicylic acid microemulsion was in accordance with the zero order kinetic release rule. Conclusion: salicylic acid microemulsion can promote the transdermal absorption of salicylic acid and provide a theoretical basis for the preparation of a new dosage form of salicylic acid with low irritability and high bioavailability.
【作者单位】：泰山医学院药学院;
【分类号】：R943

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