青防肿痛外敷散剂与凝胶剂的体外渗透行为比较

目的:比较青防肿痛外敷散剂与凝胶剂体外渗透行为的差异性。方法:采用透皮扩散仪,以青藤碱为指标,含角质层的Wistar大鼠腹部皮肤为渗透媒介,采用HPLC考察青防肿痛外敷散剂与凝胶剂在不同时间点的青藤碱经皮渗透量,流动相甲醇-水-乙二胺(50∶50∶0.1),检测波长262 nm,比较2种剂型的体外渗透行为。结果:青防肿痛外敷散剂与凝胶剂12 h单位面积累计透过量分别为0.405 24,0.191 14 mg·cm-2,累计透过率分别为74.52%,35.15%。2种剂型中青藤碱的渗透行为均符合Higuchi方程,透皮速率分别为0.180 5,0.073 4 mg·cm-2·h-1。结论:青防肿痛外敷散剂与凝胶剂均具有缓释释药效果。在释药前期,凝胶剂较外敷散剂释药迅速;在整体经皮渗透过程中,外敷散剂较凝胶剂显著提高了青藤碱的经皮渗透量及透过速率。

Comparison of in vitro Penetration Behavior Between Qingfang Zhongtong External Application Powder and Gel

Objective: To compare in vitro permeation behavior differences between Qingfang Zhongtong external application powder and gel. Method: Taking transdermal diffusion instrument,with sinomenine as index component,abdominal skin of wistar rats containing cuticular as permeability medium,percutaneous penetration content of sinomenine in Qingfang Zhongtong external application powder and gel at seteing times were determined by HPLC,mobile phase was methanol-water-ethylene diamine (50:50:0.1),detection wavelength was 262 nm,in vitro permeation behavior of these two formulations was compared. Result: Cumulative penetration content of Qingfang Zhongtong external application powder and gel were 0.405 24,0.191 14 mg·cm^-2 in 12 hours,respectively.Cumulative penetration percentage of them were 74.52% and 35.15%,respectively.Penetration behavior of sinomenine in these two formulations conformed to Higuchi equation,transdermal rate were 0.180 5,0.073 4 mg·cm^-2·h^-1,respectively. Conclusion: Both Qingfang Zhongtong external application powder and gel have sustained release effect.The gel releases drugs much more quickly at an early period,but during whole process of percutaneous penetration,external application powder can significantly improve both cumulative penetration content and transdermal rate of sinomenine.