Biomembrane permeation of nicotine: Mechanistic studies with porcine mucosae and skin
Biomembrane permeation of nicotine: Mechanistic studies with porcine mucosae and skin
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DOI：
10.1021/js960095w
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发表时间：
1997-02-01
影响因子：
3.8
通讯作者：
Chien, YW
中科院分区：
文献类型：
--
作者：
Nair, MK;Chetty, DJ;Chien, YW
在本研究中，使用从家猪新鲜切除的皮肤和吸收性粘膜的各个区域，研究了尼古丁的渗透和分配随pH值的变化。作为一种可电离化合物（pK（a）值为3.04和7.84），不同pH值溶液中的尼古丁提供了一种用于确定分子电荷状态对渗透影响的模型。尼古丁在猪粘膜和皮肤中的渗透符合零级动力学。渗透速率取决于供体溶液的pH值，并随着pH值的增加呈指数增加。鼻粘膜对所有尼古丁物质的渗透性相似，除此之外，非电离物质（NN）的尼古丁在各种皮肤和粘膜标本中的渗透性显著高于电离物质（NNH+、NH+NH+）（p < 0.001）。还观察到非电离尼古丁分子通过吸收性粘膜（鼻、颊、舌下和牙龈）的渗透性高于通过皮肤（腹部、背部、大腿和耳廓）的渗透性。分配研究，结果进一步证实，尼古丁的生物膜渗透遵循pH分配理论。
In the present study, the permeation and partitioning of nicotine as a function of pH was investigated with various regions of skin and absorptive mucosae that were freshly excised from domestic pigs. As an ionizable compound (pK(a) values of 3.04 and 7.84), nicotine in solutions of different pH values provides a model for determining the influence of the charge status of a molecule on permeation. The permeation of nicotine across porcine mucosae and skin followed zero-order kinetics. The rate of permeation was dependent on donor solution pH and increased exponentially as the pH increased. With an exception of the nasal mucosa, which showed similar permneabilities for all species of nicotine, the permeability of nicotine across various skin and mucosal specimens was significantly higher (p < 0.001) for the un-ionized species (NN) than for the ionized species (NNH+, NH+NH+). It was also seen that un-ionized nicotine molecules were more permeable through absorptive mucosae (nasal, buccal, sublingual, and gingival) than through skin (abdominal, dorsal, thigh, and ear pinna). Partition studies were performed and the results further confirmed that biomembrane permeation of nicotine follows the pH-partition theory.