香附挥发油体外促硝西泮透皮作用研究

Enhancing Percutaneous Permeability of Nitrazepam through Rat Skin by Essential Oil from Cyperus rotundus L.

目的考察香附挥发油对硝西泮体外经SD大鼠皮肤渗透的影响,为筛选中药透皮促进剂和开发硝西泮透皮制剂提供依据。方法用改良的Franz扩散池进行体外透皮实验,高效液相色谱法测定硝西泮的含量。结果当供给液中香附挥发油浓度>1%时,香附挥发油对地西泮有良好的促透效果,随浓度的增大促透效果越好。0.5 mg.mL-1硝西泮加入3%月桂氮酮或3%、5%香附挥发油后24 h平均累积渗透量分别为143.7,172.6,229.3μg.(cm2)-1;24h平均透皮速率常数分别为6.381,7.511,10.32μg.(cm2)-1.h-1;增渗倍数分别为1.970,2.319,3.186。结论香附挥发油对硝西泮有较强的促透皮作用。

Objective To study the effects of the essential oil from Cyperus rotundus L. on percutaneous permeability of nitrazepam through rat skin in vitro, and provide the basis for screening penetration enhancers from traditional Chinese medicine and developing the transdermal formulation of nitrazepam. Methods Transdermal test was performed by the modified Franz diffusion cell in vitro and the cumulative permeation content of nitrazepam was determined by HPLC. Results A good percutaneous permeability was obtained when the essential oil from Cyperus rotundus L. was more than 1% , and the effect of which was in a dose-dependent manner. The 24-hour average cumulative permeation amounts of 0.5 mg· mL^- 1 nitrazepam with 3% Azone, and 3% , 5% Cyperus rotundus volatile oil were 143.7,172.6 and 229.3 μg·（cm^2）^-1 , respectively; the average penetration constants were 6. 381, 7. 511, and 10.32μg·（cm^2）^-1 , respectively; the enhanced permeability factors were 1.970, 2. 319, 3. 186, respectively. Conclusion The essential oil from Cyperus rotundus L. shows strong penetration enhancing effect for nitrazepam.