干姜、丁香、荜澄茄对马钱子总碱贴剂的经皮促渗作用研究

Percutaneous Enhancement Effect of Volatile Oil of Rhizoma Zingiberis,Flos Caryophyllata and Fructus Litseae on Total Alkaloids of Semen Strychni Transdermal Patch

目的考察干姜、丁香、荜澄茄挥发油及其混合挥发油对马钱子总碱贴剂的经皮促渗作用。方法利用改良Franz扩散池法,以氮酮为阳性对照,不含促渗剂的马钱子总碱为阴性对照,考察含不同质量分数的(3%,5%,7%,10%)干姜、丁香、荜澄茄挥发油对模型药马钱子总碱经小鼠皮肤的促渗效果,然后将筛选出来的最好质量分数的挥发油,折半后按1∶1混合再对马钱子总碱的经皮渗透作用进行考察,采用HPLC测定马钱子总碱的含量。结果同系列中以10%干姜油、7%丁香油、5%荜澄茄油及5%干姜+5%氮酮的混合挥发油对贴剂中马钱子总碱的促渗效果最好,其8 h平均累积渗透量(Q8)分别为2.311、2.016、2.656与2.532(mg·cm-2);6h时增渗倍数分别为1.692、2.687、3.420与1.991。与阴性对照组的Q8比较,10%干姜油、5%荜澄茄油的差异有非常显著性意义(P<0.01)。结论 10%干姜挥发油、7%丁香挥发油、5%荜澄茄挥发油以及5%干姜+5%氮酮的混合挥发油能明显提高马钱子总碱在贴剂中的渗透量,促渗效果好。

Objective To investigate in vitro percutaneous penetration effect of different concentration of single and mixed volatile oil from Rhizoma Zingiberis （RZ）, Flos Caryophyllata （FC）, Fructus Litseae （FL） on total Alkaloids of Semen Strychni （TASS） Transdermal Patch through mouse skin. Methods A modified Franz diffusion cell method was used, penetration enhancing effect of 3%, 5%, 7% and 10% volatile oil from RZ, FC and FL on TASS Transdermal Patch through mouse skin in vitro were investi- gated with Azone as positive control and TASS Transdermal Patch without penetration enhancers as negative control. The content of TASS was determined by HPLC. After the best enhancing concentrations of the three kinds of volatile oils were chosen, the mixed oils were investigated by halving and pairing them as 1： 1. Results 10% volatile oil from RZ, 7% volatile oil from FC, 5 % volatile oil from FL and 5 % Azone ＋ 5 % volatile oil of RZ had the best enhancing effect among the homologous series, the av- erage cumulative permeation volume in 8h （Q8） of TASS Transdermal Patch with them were 2. 311 , 2. 016, 2. 656 and 2. 532 （ mg. cm-2 ） respectively ; and enhancing rates（ER） in 6h were 1. 692, 2. 687, 3. 420 and 1. 991 respectively. Compared with the negative control group, 10% volatile oil from RZ and 5% volatile oil from FL had statistical significance by T Test （P 〈 0.01 ） . Conclusion 10% volatile oil from RZ, 7% volatile oil from FC, 5% volatile oil from FL, and 5% Azone ＋ 5% volatile oil of RZ could enhance permeation volume of TASS from Patch through mouse skin obviously.