[关键词]
[摘要]
目的 制备紫苏醇软膏,考察其性质并进行体外透皮研究。方法 采用乳化法制备紫苏醇软膏并研究其形态、稳定性及体外释放特征,用Franz扩散池考察其透皮吸收行为、HPLC法测定紫苏醇的量。结果 优选的紫苏醇软膏处方为紫苏醇-硬脂酸-单硬脂酸甘油酯-白凡士林-羊毛脂-液体石蜡-三乙醇胺-甘油-尼泊金乙酯,外观为淡黄色半固体,软膏中紫苏醇的有效量为(2.89±0.17)%,12 h体外释放达到61.25%,经皮渗透速率为9.42 μg/(cm2?h), 3 500 r/min离心30 min未分层,在0、40 ℃条件下放置30 d稳定。结论 所制备的紫苏醇软膏可以显著增加药物在皮肤中的经皮渗透量,为研发紫苏醇及其新型局部给药制剂提供依据。
[Key word]
[Abstract]
Objective To prepare perillyl alcohol ointment (PAO) and to investigate its properties and transdermal absorption behavior. Methods The emulsion method was used to prepare PAO. The morphology, stability, and in vitro release were examined, respectively. The transdermal absorption of PAO was evaluated using Franz diffusion cells and the perillyl alcohol content was determined by HPLC. Results The optimal prescription of PAO was perillyl alcohol, stearic acid, glyceryl monostearate, white vaseline, lanolin, liquid paraffin, triethanolamine, glycerine, and ethylparaben. The product was a pale yellow semi-solid oil-in-water emulsion with a uniform appearance. The content of perillyl alcohol in ointment was (2.89 ± 0.17)%, the release accumulation in vitro achieved 61.25% in 12 h, and the percutaneous penetration rate was 9.42 μg/(cm2?h). The ointment was not stratified after the centrifugation at 3 500 r/min for 30 min, and the product was fairly stable under the condition of storing at 0 and 40 ℃ for 30 d. Conclusion The prepared PAO with increased skin retention amount could be developed into a novel preparation of perillyl alcohol for focal administration.
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[基金项目]
河南省重点科技攻关计划项目(092102310028);河南省基础与前沿技术研究计划项目(112102310022)