Single-Dose Pharmacokinetics of Nicotine When Given With a Novel Mouth Spray for Nicotine Replacement Therapy
Single-Dose Pharmacokinetics of Nicotine When Given With a Novel Mouth Spray for Nicotine Replacement Therapy
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DOI：
10.1093/ntr/ntr139
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发表时间：
2011-12-01
影响因子：
4.7
通讯作者：
Perfekt, Roland
中科院分区：
文献类型：
--
作者：
Kraiczi, Holger;Hansson, Anna;Perfekt, Roland
由于尼古丁替代治疗的疗效可能会通过更快的全身尼古丁吸收来改善，因此开发了一种新的尼古丁口腔喷雾剂。本研究旨在评价3种剂量的尼古丁口腔喷雾剂单次给药的药代动力学，并比较尼古丁从喷雾剂与尼古丁含片和口香糖中摄取尼古丁的速度。在一项随机交叉研究中，45名健康成年吸烟者在不同场合接受尼古丁口腔喷雾剂1、2和4 mg、尼古丁含片4 mg和尼古丁口香糖4 mg单次给药。用曲线下面积（AUC（10 min））测定的前10 min内的平均血浆尼古丁浓度，4 mg喷雾剂是锭剂或口香糖的3倍。2 mg和1 mg喷雾剂的AUC（10 min）分别是锭剂或口香糖AUC（10 min）的2倍和1.5倍。4 mg喷雾剂的最大基线校正血浆尼古丁浓度（cC（max））分别比含片和咀嚼胶高34%和20%; 3种喷雾剂达到C-max的中位时间为10-12.5 min，含片为45 min，咀嚼胶为30 min。4 mg喷雾剂的平均基线校正血浆尼古丁浓度-时间曲线下面积（cAUC（无穷大））比口香糖高15%，但与含片无显著差异。通过口腔喷雾剂递送的尼古丁比通过口香糖或含片递送的尼古丁吸收快得多。
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(infinity)) 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.