Department of Surgical and Oncologic Disciplines, University of Palermo, Italy.
Int J Pharm. 2013 Aug 16;452(1-2):128-34. doi: 10.1016/j.ijpharm.2013.04.070. Epub 2013 May 2.
Naltrexone is widely used in the treatment of opiate addiction but its current peroral administration is characterized by low bioavailability with various side effects. The development of a long-acting transbuccal delivery device (IntelliDrug) for NLX may be useful to improve patient compliance and the therapy effectiveness. The aims of the study are (a) to test basic safety and effectiveness of controlled transbuccal drug delivery on human subjects; (b) to compare NLX bioavailability following transbuccal delivery vs per os conventional delivery; and (c) to test the hypothesis that transbuccal delivery is more efficient than the conventional route. In this randomized cross-over pilot study, 12 healthy subjects received in a different order 2 types of NLX administration, per os or transbuccal delivery, based on which group they were randomized to. For per os administration 50mg NLX tablets were used, while for transbuccal administration, a NLX-loaded prototype of the IntelliDrug device was fixed on patients' dental arch. Serial blood samples were drawn and analysed for the NLX concentration. The IntelliDrug prototype functioned properly and it did not exert any adverse side-effect. The transbuccal route resulted in administration efficiency 4-17 times higher than conventional per os route. Transbuccal delivery of NLX appears to be a more efficient drug administration route compared to peroral one. It allows to reach a given therapeutic blood level using a small drug dose.
纳曲酮被广泛用于治疗阿片类药物成瘾，但目前的口服给药方式存在生物利用度低和多种副作用的特点。开发一种长效经颊给药装置（IntelliDrug）用于纳曲酮可能有助于提高患者的依从性和治疗效果。该研究的目的是：（a）测试在人体受试者中经颊控释给药的基本安全性和有效性；（b）比较经颊给药与口服常规给药后纳曲酮的生物利用度；（c）验证经颊给药比常规途径更有效的假设。在这项随机交叉先导研究中，12 名健康受试者以不同的顺序接受了 2 种纳曲酮给药方式，即口服或经颊给药，这取决于他们被随机分配到的组别。口服给药使用 50mg 纳曲酮片剂，而经颊给药则将纳曲酮负载的 IntelliDrug 装置原型固定在患者的牙弓上。采集并分析了一系列血样以检测纳曲酮的浓度。IntelliDrug 原型运行良好，没有产生任何不良反应。与口服常规途径相比，经颊途径的给药效率高出 4-17 倍。与口服途径相比，经颊给予纳曲酮似乎是一种更有效的药物给药途径。它可以使用小剂量药物达到给定的治疗血药水平。
