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目的考察氮酮对不同亲脂性中药有效成分的经皮促透作用特征,探讨其对中药外用制剂中复杂成分的经皮促透效果。方法选择不同亲脂性中药有效成分,包括强亲脂性和强亲水性药物,即蛇床子素、川芎嗪、阿魏酸、葛根素、京尼平苷,采用体外透皮试验测定不同浓度氮酮对各药物的经皮促透吸收情况,并建立药物油水分配系数值(log Ko/w)与其对应促透倍数间的相关性。结果氮酮对不同亲脂性药物均表现出显著经皮促透作用,并呈现先随氮酮浓度增加而增强,达到一定浓度后其促透倍数开始下降的作用趋势;氮酮作用下药物log Ko/w值与促透倍数对数值呈抛物线关系,对log Ko/w值约为-0.5的药物具有最佳的经皮促透作用。结论氮酮对不同亲脂性中药有效成分均具有良好促透作用,且其促透倍数对数值与药物log Ko/w值呈抛物线关系。
Aim To investigate the transdermal permeation effect of Azone on the active ingredients of different lipophilic traditional Chinese medicines and to explore their percutaneous penetration enhancement effect on the complex components in traditional Chinese medicine preparations. Methods The active ingredients of different lipophilic traditional Chinese medicines were selected, including strong lipophilic and strong hydrophilic drugs, ie osthole, ligustrazine, ferulic acid, puerarin and geniposide. The in vitro transdermal test was used to determine the effects of different concentrations of azone The transdermal pervious permeability of each drug was established and the correlation between log Ko / w value and the corresponding transflective ratio was established. Results Azone showed a significant transdermal permeation effect on different lipophilic drugs and showed an increasing trend with increasing concentration of azone. After reaching a certain concentration, the number of transketolants began to decrease. Logarithm of konjac The value of / w has a parabolic relationship with the logarithm of transketolability and has the best transdermal permeability to the drug with a log Ko / w value of about -0.5. Conclusion Azone has a good osmotic effect on the active ingredients of different lipophilic herbs, and its logarithm value of osmotic multiple has a parabolic relationship with log Ko / w value.