不同基源冰片促透效果的差异研究

Study on the difference of permeation effects of different sourced borneol

目的研究天然冰片、艾片及合成冰片对模型药物经皮渗透效果的差异。方法采用改良的Franz扩散池考察不同基源冰片对天麻素、欧前胡素经皮渗透性的影响;利用HPLC法测定透皮接收液中天麻素、欧前胡素的含量。结果三种基源冰片对天麻素、欧前胡素均具有明显的促透作用,且促透效果存在差异;对于天麻素,其促透效果大小顺序为:艾片>合成冰片>天然冰片;对于欧前胡素,其促透效果大小顺序为:天然冰片>合成冰片>艾片;三种冰片对天麻素的促透效率均显著高于对欧前胡素的促透效率。结论三种基源冰片对同一药物的促透效果存在差异,说明不同构型冰片对药物的促透效果存在立体选择性;三种基源冰片促透不同药物时,扰乱脂质有序排列、抽提脂质的能力存在明显不同;与亲脂性药物相比,冰片对亲水性药物的经皮渗透性效果更好。

Objective To investigate the differences in percutaneous penetration of model drugs by natural borneol, blumea camphor and synthetic borneol.Methods The influence of different sourced borneol on the percutaneous permeability of gastrodin, imperatorin was studied using a modified Franz diffusion device, and the contents of gastrodin and imperatorin in the transdermal receiving solution were determined by HPLC. Results Three kinds of borneol had obvious permeation effects on gastrodin and imperatorin, and there were differences in promoting effect. For gastrodin, the order of permeation effect was: blumea camphor>synthetic borneol>natural borneol;For imperatorin, the order of permeation effect was: natural borneo>synthetic borneol>blumea camphor. These kinds of borneol had higher permeation ratios to gastrodin than to imperatorin. Conclusion Three kinds of borneol had different effects on the penetration of the same drug, indicating that there were stereoselective effects in promoting the penetration of drugs with different configurations of borneol. When different borneol promoted different drugs, the ability to disrupt lipid arrangement and extract lipids was significantly different. Compared with lipophilic drugs, the effect of borneol on the transdermal permeability of hydrophilic drugs was better.