KINETIC EVALUATION OF TRANSDERMAL NICOTINE DELIVERY SYSTEMS
KINETIC EVALUATION OF TRANSDERMAL NICOTINE DELIVERY SYSTEMS
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DOI：
10.3109/03639049309038769
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发表时间：
1993-01-01
影响因子：
3.4
通讯作者：
CHIEN, YW
中科院分区：
文献类型：
--
作者：
HO, H;CHIEN, YW
为了评价系统设计的效果和产品的互换性，在相同的条件下考察了4种新近上市的尼古丁缓释透皮给药系统(TDS)中尼古丁的皮肤渗透和释放动力学。本研究首先以无毛大鼠皮肤为动物模型，评价了各种TDS的渗透机制，并通过人体皮肤渗透实验对其进行了验证。4个TDS中有3个在稳态时以零级渗透动力学传递尼古丁，渗透速率范围为0.072-0.197 mg/cm~2/小时，而第4个TDS呈现三相零级渗透速率曲线。3个TDS以非线性方式释放尼古丁，可用线性Q-T1/2关系来描述，而1个TDS在稳态下产生恒定释放。这些TDS对尼古丁的不同皮肤渗透性可以用它们不同的系统设计和结构组成来解释。
The skin permeation and release kinetics of nicotine from four nicotine-releasing transdermal delivery systems (TDS) marketed recently was investigated under identical conditions to evaluate the effect of system design and the interchangeability of these products. In the study, hairless rat skin was first used as an animal model to evaluate the permeation mechanisms of various TDS's, which were then verified by studying the permeation through human cadaver skin. Three of the four TDS's were found to deliver nicotine at zero(th)-order permeation kinetics at steady state with permeation rate ranging from 0.072 - 0.197 mg/cm2/hr, while the fourth one produced a triphasic zero(th)-order permeation rate profile. Three TDS's released nicotine at non-linear manner, which could be described by a linear Q vs. t1/2 relationship, while one TDS yielded a constant release at steady state. The different skin permeation profiles of nicotine delivered by these TDS's could be explained by the difference in their system designs and structural compositions.