Clinical Pharmacology, McNeil AB, Karl XII gatan 5, S-22220 Lund, Sweden.
Nicotine Tob Res. 2011 Dec;13(12):1176-82. doi: 10.1093/ntr/ntr139. Epub 2011 Aug 17.
As the efficacy of nicotine replacement therapy might be improved by faster systemic nicotine uptake, a new nicotine mouth spray has been developed. The current study was performed to evaluate the single-dose pharmacokinetics of nicotine at 3 doses of the mouth spray and to compare the speed of nicotine uptake from the spray versus nicotine lozenge and gum.
In a randomized crossover study, 45 healthy adult smokers received single doses of nicotine mouth spray 1, 2, and 4 mg, nicotine lozenge 4 mg, and nicotine gum 4 mg on separate occasions. Blood samples were collected for 12 hr to determine pharmacokinetic variables.
Mean plasma nicotine concentrations during the first 10 min, measured using area under the curve (AUC(10 min)), were 3 times as high with spray 4 mg as with lozenge or gum. The AUC(10 min) with 2 and 1 mg doses of spray, respectively, was twice and 1.5 times as high as the AUC(10 min) with lozenge or gum. The maximum baseline-corrected plasma nicotine concentration (cC(max)) with 4 mg spray exceeded that for lozenge and gum by 34% and 20%; the median time to reach C(max) was 10-12.5 min for the 3 doses of spray, 45 min for lozenge, and 30 min for gum. The mean baseline-corrected area under the plasma nicotine concentration-versus-time curve (cAUC(∞)) with 4 mg spray was 15% higher than that with gum but did not differ significantly from that with lozenge.
Nicotine delivered via the mouth spray is absorbed considerably faster than nicotine given via gum or lozenge.
由于尼古丁替代疗法的疗效可能因更快的全身尼古丁吸收而提高，因此开发了一种新的尼古丁口腔喷雾。本研究旨在评估 3 种剂量的尼古丁口腔喷雾的单剂量药代动力学，并比较喷雾与尼古丁含片和尼古丁胶的尼古丁吸收速度。
在一项随机交叉研究中，45 名健康成年吸烟者在不同时间分别接受了 1、2 和 4mg 的尼古丁口腔喷雾、4mg 的尼古丁含片和 4mg 的尼古丁胶的单次剂量。采集了 12 小时的血样以确定药代动力学变量。
使用曲线下面积（AUC（10 分钟））测量的前 10 分钟内，喷雾 4mg 时的平均血浆尼古丁浓度是含片或口香糖的 3 倍。分别使用 2mg 和 1mg 剂量的喷雾的 AUC（10 分钟）是含片或口香糖的 2 倍和 1.5 倍。喷雾 4mg 时的最大基线校正血浆尼古丁浓度（cC（max））比含片和口香糖分别高出 34%和 20%；喷雾 3 个剂量的 C（max）中位达峰时间为 10-12.5 分钟，含片为 45 分钟，口香糖为 30 分钟。喷雾 4mg 时的基线校正后的血浆尼古丁浓度-时间曲线下面积（cAUC（∞））平均比口香糖高 15%，但与含片无显著差异。
与口香糖或含片相比，口腔喷雾给予的尼古丁吸收速度明显更快。
