Keller-Stanislawski B, Caspary S
Department of Clinical Pharmacology, Johann Wolfgang Goethe-University, Frankfurt/Main, Fed. Rep. of Germany.
Arzneimittelforschung. 1992 Sep;42(9):1160-2.
Tobacco use has resulted in major health related problems world-wide. Transdermal nicotine replacement therapy is one of the most promising strategies in smoking cessation. In the present trial the pharmacokinetic properties of two matrix patches (A and B) were characterized and compared after daily application on day 4. Predose nicotine concentrations on day 4 with patch B were higher than with patch A (12.7 +/- 9.5 ng/ml vs. 8.3 +/- 5.3 ng/ml). With patch A there was a steeper increase up to the peak level, followed by a decline gradually up to 24 h. 24 h after application predose levels were reached again, demonstrating absence of significant accumulation of nicotine. The calculated elimination half-lives of nicotine (3.4 +/- 1.8 h after patch A and 3.3 +/- 2.0 h after patch B) were longer than after i.v. application (published values range from 40 to 120 min). Under steady state cotinine concentrations remained constant.
在全球范围内,吸烟已导致了与健康相关的重大问题。经皮尼古丁替代疗法是戒烟最具前景的策略之一。在本试验中,对两种基质贴片(A和B)在第4天每日使用后的药代动力学特性进行了表征和比较。第4天贴片B的给药前尼古丁浓度高于贴片A(12.7±9.5 ng/ml对8.3±5.3 ng/ml)。贴片A在达到峰值水平之前有更陡峭的上升,随后逐渐下降直至24小时。给药24小时后再次达到给药前水平,表明不存在尼古丁的显著蓄积。计算得出的尼古丁消除半衰期(贴片A后为3.4±1.8小时,贴片B后为3.3±2.0小时)比静脉注射后更长(已发表的值范围为40至120分钟)。在稳态下,可替宁浓度保持恒定。