Mittal Ashu, Sara Udai Vir Singh, Ali Asgar, Aqil Mohammed
ITS-Paramedical College (Pharmacy), Muradnagar, Ghaziabad, India.
Biol Pharm Bull. 2008 Sep;31(9):1766-72. doi: 10.1248/bpb.31.1766.
The purpose of this research was to evaluate the effect of penetration enhancers on permeation kinetics of nitrendipine (NTP) through two different skin models. The permeation profile and related kinetics parameters such as activity parameter, diffusion parameter, lag time, relative activity parameter and relative diffusion parameter of NTP was determined in presence of some novel and widely accepted permeation enhancers. Among all the more pronounced enhancing effect was obtained with oleic acid (OA) as it presented the highest permeability coefficient. The enhancement was found to be increased in the following order: Dimethyl sulphoxide (DMSO)<Isopropyl myristate (IPM)<Sodium lauryl sulphate (SLS)<Tween 20 (T20)<Myristic acid (MA)<Lauric acid (LA)<Capric acid (CA)<Tween 80 (T80)<Span 80 (S80)<Thyme oil (TO)<Palmarosa oil (PA)<Petitlgrain oil (PT)<Basil oil (BO)<Oleic acid (OA). The increase in drug permeation was attributed mainly to the decrease in diffusion path length. Essential oils and surfactant (span 80) have shown relative activity parameter (Kr value) well above unity and relative diffusion parameter (Dr value) almost equal or less than unity, which would be attributed to gradual increase in membrane permeability leading to higher permeation. Oleic acid is effective for augmenting skin permeation of NTP, with potential application in transdermal delivery of the drug.
本研究的目的是评估渗透促进剂对尼群地平（NTP）透过两种不同皮肤模型的渗透动力学的影响。在一些新型且广泛认可的渗透促进剂存在的情况下，测定了NTP的渗透曲线以及相关动力学参数，如活性参数、扩散参数、滞后时间、相对活性参数和相对扩散参数。在所有促进剂中，油酸（OA）表现出最显著的促进效果，因为它具有最高的渗透系数。促进效果按以下顺序增强：二甲基亚砜（DMSO）＜肉豆蔻酸异丙酯（IPM）＜月桂醇硫酸酯钠（SLS）＜吐温20（T20）＜肉豆蔻酸（MA）＜月桂酸（LA）＜癸酸（CA）＜吐温80（T80）＜司盘80（S80）＜百里香油（TO）＜玫瑰草油（PA）＜苦橙叶油（PT）＜罗勒油（BO）＜油酸（OA）。药物渗透的增加主要归因于扩散路径长度的缩短。香精油和表面活性剂（司盘80）的相对活性参数（Kr值）远高于1，相对扩散参数（Dr值）几乎等于或小于1，这归因于膜通透性的逐渐增加导致更高的渗透率。油酸对增强NTP的皮肤渗透有效，在该药物的透皮给药中具有潜在应用价值。
