Nasal nicotine spray: a rapid nicotine delivery system
Nasal nicotine spray: a rapid nicotine delivery system
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尼古丁鼻喷雾剂：快速尼古丁输送系统
作者：
G. Sutherland;M. Russell;J. Stapleton;C. Feyerabend;O. Ferno
在10名受试者中比较了两种鼻用尼古丁喷雾剂给药后的血浆尼古丁浓度。在前2.5分钟内吸收特别快，在此期间，两种产品的血液尼古丁浓度平均升高8.6 ng/ml，随后在给予2 mg尼古丁碱后5分钟进一步小幅升高至平均峰值10.5 ng/ml（平均值27.8 µg/kg）。尽管受试者之间的Cmax差异为4倍，但两种产品中个体受试者的水平相当一致。两种产品在血液尼古丁浓度或心血管反应方面无显著差异，两种产品AUC之间的相关性为0.68（P=0.01）。8名受试者报告了头晕目眩或轻微头晕的主观感觉，这在尼古丁咀嚼胶或皮肤贴剂吸收较慢后并不典型。通过重复给药，即使是鼻吸收效率最低的受试者，吸烟范围内的血液尼古丁水平也很快就会升高。在临床条件下随意使用的第二项研究中，两种产品作为辅助戒烟的治疗用途似乎完全可以接受。在4周内没有升级到过度使用的趋势，9名受试者的血液尼古丁浓度平均仅为他们先前吸烟水平的44%。只有一名受试者的水平相当于以前吸烟，并讨论了为什么这不是更常见的可能原因。
Plasma nicotine concentrations following administration by two types of nasal nicotine spray were compared in ten subjects. Absorption was particularly rapid during the first 2.5 min, the average rise in blood nicotine concentrations during this time being 8.6 ng/ml for the two products, followed by a small further rise to an average peak increase of 10.5 ng/ml 5 min after the dose of 2 mg nicotine base (mean 27.8 µg/kg). Despite a four-fold Cmax variation between subjects, the levels of individual subjects were fairly consistent across the two products. There were no significant differences between the two products in blood nicotine concentrations or cardiovascular responses, and the correlation between the AUCs from the two products was 0.68 (P=0.01). Eight subjects reported subjective feelings of light-headedness or slight dizziness, which are not typical after slower absorption from nicotine gum or skin patches. Blood nicotine levels within the smoking range were soon built up with repeated doses, even in the subject with the least efficient nasal absorption. In a second study of ad libitum use under clinical conditions both products appeared sufficiently acceptable for therapeutic use as an aid to smoking cessation. There was no tendency to escalate to excessive use over 4 weeks, and blood nicotine concentrations in nine subjects averaged only 44% of their prior smoking levels. Only one subject had levels equivalent to prior smoking and possible reasons why this was not more common are discussed.