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该文拟采用经皮微透析技术测定花椒挥发油对不同脂溶性中药成分皮肤药动学行为的影响,评价其在体经皮促透特征。选择川芎嗪和葛根素作为亲脂性和亲水性模型药物,采用浓差法考察微透析探针体外回收率与传递率,采用反向渗析法测定药物探针在体回收率;以常用化学促透剂氮酮为阳性对照,测定不同浓度花椒挥发油对川芎嗪和葛根素的皮肤药动学行力影响。结果显示,2种模型药物探针回收率与传递率相等,药物在渗析膜间无相互作用,川芎嗪和葛根素的在体相对回收率分别为59.17%,19.85%。在体经皮试验表明花椒挥发油对川芎嗪具良好促透效果,且呈浓度依赖性关系,5%花椒挥发油的在体促透倍数(ER)为98.64,比氮酮最佳浓度的促透效果更好(3%氮酮,ER=89.11);同时,花椒挥发油也可显著增加葛根素的在体经皮吸收,也表现出浓度依赖性关系。因此,该研究进一步证实花椒挥发油作为经皮促透剂的良好促透性能,为其在中药外用制剂中的应用提供了数据支持。
This article intends to use percutaneous microdialysis technique to determine the volatile oil of Z. prunella on the pharmacokinetics of different fat-soluble components of the skin pharmacokinetic behavior, evaluation of the percutaneous dermal penetration characteristics. Ligustrazine and puerarin were selected as the lipophilic and hydrophilic model drugs. The concentration recovery method was used to investigate the recovery rate and transmissibility of microdialysis probes in vitro. The reverse recovery method was used to determine the recovery rate of drug probes in vivo. Azo Azone as a positive control, determination of different concentrations of volatile oil of ligustrazine and puerarin skin pharmacokinetic force. The results showed that the recovery rate and transmissibility of drug probe in the two models were equal, and there was no interaction between drugs in the dialysis membrane. The relative recoveries of ligustrazine and puerarin in vivo were 59.17% and 19.85% respectively. In the body skin test showed that volatile oil of Zanthoxylum bungeanum has good penetration enhancement effect, and in a concentration-dependent manner, 5% Zanthoxylum volatile oil in vivo body translucency (ER) was 98.64, the optimum concentration of Azone Anesthetic effect (3% Azone, ER = 89.11). At the same time, the volatile oil of Zanthoxylum bungeanum also significantly increased the percutaneous absorption of puerarin and showed a concentration-dependent relationship. Therefore, this study further confirmed that the volatile oil of Zanthoxylum Bungeanum as transdermal permeable agent had good permeability and provided the data support for its application in the preparation of traditional Chinese medicine.