Terpenes in propylene glycol as skin-penetration enhancers: Permeation and partition of haloperidol, fourier transform infrared spectroscopy, and differential scanning calorimetry
Terpenes in propylene glycol as skin-penetration enhancers: Permeation and partition of haloperidol, fourier transform infrared spectroscopy, and differential scanning calorimetry
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DOI：
10.1002/jps.10160
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发表时间：
2002-07-01
影响因子：
3.8
通讯作者：
Chan, SY
中科院分区：
文献类型：
--
作者：
Vaddi, HK;Ho, PC;Chan, SY
在丙二醇（PG）中以5%w/v使用相应的醇萜烯香芹酚、芳樟醇和α-萜品醇以增加氟哌啶醇（HP）通过人皮肤的体外渗透。可能的增强机制，然后阐明与HP-角质层（SC）的结合研究，傅立叶变换红外光谱，差示扫描量热法。在HP渗透的最大增加实现芳樟醇，其次是香芹酚和松油醇。HP渗透芳樟醇预计达到治疗血浆浓度和治疗每日渗透量。香芹酚增加滞后时间，这是由于缓慢的增强子内SC的再分配。香芹酚增加了分区的药物粉碎SC。纯PG提取脂质SC，但低于实现的萜烯在PG。萜烯提取脂质在类似的程度。在SC中存在的剩余脂质中的双层凝聚力的增加可以归因于脂质双层内的萜烯的排列。芳樟醇的较高渗透归因于其在脂质双层内的分子取向。萜烯类化合物表现出不同的SC脱水率，但不改变角蛋白二级结构的百分比。(C)2002 Wiley-Liss，Inc.和美国制药协会。
The respective alcoholic terpenes carvacrol, linalool, and a-terpineol were used at 5% w/v in propylene glycol (PG) to increase the in vitro permeation of haloperidol (HP) through human skin. The possible enhancement mechanism was then elucidated with HP-stratum corneum (SC) binding studies, Fourier transform infrared spectroscopy, and differential scanning calorimetry. The greatest increase in the permeation of HP was achieved with linalool followed by carvacrol and terpineol. HP permeation with linalool was predicted to reach a therapeutic plasma concentration and therapeutic daily-permeated amounts. Carvacrol increased lag time, which was attributed to slow redistribution of the enhancer within SC. Carvacrol increased the partition of the drug to the pulverized SC. Pure PG extracted lipids from SC but less than that achieved by the terpenes in PG. Terpenes extracted lipids to a similar extent. An increase in bilayer cohesion in the remaining lipids present in the SC could be attributed to the alignment of terpenes within the lipid bilayer. The higher permeation with linalool was attributed to its molecular orientation within the lipid bilayer. Terpenes showed different rates of SC dehydration but did not change the percentages of secondary structures of keratin. (C) 2002 Wiley-Liss, Inc. and the American Pharmaceutical Association.