正交试验设计优选通脉软膏的辅料组成及其渗透性能与皮肤安全性研究

Optimization of Tongmai ointment excipients by orthogonal test design and its permeability and skin safety research

制备通脉软膏并评价其体外经皮渗透特性及皮肤安全性.以物理性状为指标,参考姜黄素含量筛选通脉软膏辅料比例,选择君药姜黄的主要有效成分姜黄素进行经皮评价,选用Thermo Hypersil GOLD C18色谱柱(250 mm×4.6 mm,5μm),以乙腈-4%冰乙酸溶液(48∶52)为流动相,检测波长为425 nm,采用改良的Franz扩散池分别开展通脉软膏及药粉传统外敷用法的体外经皮吸收试验,并对软膏的致敏性进行评估.结果显示,通脉软膏的最佳配方为凡士林∶羊毛脂∶液体石蜡=40∶10∶15,姜黄素的含量为0.2389 mg·g-1,24 h累计透皮量为0.0411 mg·g-1,累计透皮率为17.27%,所制得的通脉软膏无致敏性.制备的通脉软膏性状较好,其体外透皮性能明显优于传统外敷形式,且皮肤安全性较好.

This study was to prepare Tongmai ointment and evaluate its percutaneous permeability in vitro and skin safety. Taking physical properties as index and referring to the content of curcumin, the formula of Tongmai ointment was screened. The main active component of curcumin was selected by percutaneous evaluation. Thermo Hypersil GOLD C18 column(250 mm×4.6 mm, 5 μm) was used;acetonitrile-4% acetic acid(48∶52) was used as mobile phase,and the detection wavelength was 425 nm. The traditional topical application of Tongmai ointment and powder was carried out by Franz diffusion cell in vitro percutaneous absorption test. The sensitization of the ointment was evaluated. The optimum formula of Tongmai ointment is vaseline:lanolin:liquid paraffin(40∶10∶15), the content of curcumin is 0.2389 mg per gram. The cumulative transdermal volume is 0.0411 mg/g in 24 hours, and the cumulative transdermal rate is 17.27%. Tongmai ointment has no sensitization. The character of Tongmai ointment is good and its transdermal performance in vitro is significantly better than traditional external application and is safe in skin use.