3味中药挥发油对磷酸川芎嗪贴剂促渗作用的比较

目的考察草果挥发油、白豆蔻挥发油、砂仁挥发油单独和组合使用对磷酸川芎嗪（ligustrazine phosphate,LP）黏胶分散型透皮贴剂在离体裸鼠皮肤的促渗作用。方法采用E 100、丁二酸等制备LP黏胶分散型透皮贴剂;采用改良的Franz扩散池进行裸鼠体外透皮吸收实验;采用HPLC法进行接受液中药物含量测定。结果加入挥发油及氮酮促渗剂的LP贴剂的12 h累积渗透量（Q12）都有所增加,质量浓度为3%草果挥发油、5%白豆蔻挥发油、7%砂仁挥发油、1.5%草果挥发油＋2.5%白豆蔻挥发油、2.5%白豆蔻挥发油＋3.5%砂仁挥发油及3%氮酮组的Q12分别是（0.972±0.121）、（0.953±0.243）、（0.876±0.138）、（0.932±0.192）、（0.667±0.171）、（0.862±0.139）mg cm-2;增渗倍数（ER）分别是1.638、1.596、1.489、1.596、1.149、1.489;与阴性对照组比较,3%草果挥发油、5%白豆蔻挥发油、1.5%草果挥发油＋2.5%白豆蔻挥发油有明显的促渗作用（P〈0.01）。结论各种质量浓度单一及组合的挥发油对贴剂中LP都具有一定促渗作用,以3%草果挥发油的促渗作用最好。

Percutaneous enhancement effect of volatile oil from 3 herbs on ligustrazine phosphate transdermal patches

Objective To investigate the enhancement effect of single and combined volatile oil from Frustus Tsaoko（FT）,Frustus Amomi Rotundus（FAR） and Frustus Amomi（FA） on the percutaneous permeation of ligustrazine phosphate（LP） adhesive-dispersion-type transdermal patches through nude mouse skin in vitro.Methods LP adhesive-dispersiontype transdermal patches were prepared with Eudragit 100,succinic acid,etc.A test of penetration through nude mouse skin was conducted by an improved method of Franz diffusion cells.The HPLC method was used to detect the content.Results The average cumulative permeation volume at 12 h（Q12） was increased after adding the above volatile oil and azone as enhancers in LP patches.The Q12 of 3% volatile oil of FT,5% volatile oil of FAR,7% volatile oil of FA,1.5% volatile oil of FT ＋ 2.5% volatile oil of FAR,2.5% volatile oil of FAR ＋ 3.5% volatile oil of FA and 3% Azone was（0.972±0.121）,（0.953±0.243）,（0.876±0.138）,（0.932±0.192）,（0.667±0.171） and（0.862±0.139） mg cm-2,respectively,and the enhancing rates were 1.638,1.596,1.489,1.596,1.149,and 1.489,respectively.The difference between the negative group and 3% volatile oil of FT,5% volatile oil of FAR,1.5% volatile oil of FT ＋ 2.5% volatile oil of FAR,and 7% volatile oil of FA group had significant promoting effect（P 0.01）.Conclusion All kinds of single and combined volatile oil mentioned above have penetration enhancing effect on LP in the patches to some degree,and among them 3% volatile oil of FT has the best promoting effect.