Adis, a Wolters Kluwer Business, Auckland, New Zealand.
CNS Drugs. 2011 Jun 1;25(6):511-22. doi: 10.2165/11207470-000000000-00000.
Fentanyl pectin nasal spray (PecFent®) uses a novel pectin-based delivery system that turns from an aqueous solution into a gel when applied to mucosal surfaces. Fentanyl is absorbed in a controlled manner from the pectin gel formed in the nasal cavity, and has a rapid onset of pain relief and duration of action that matches the time course of a typical episode of breakthrough pain in cancer (BTPc). Relative to administration as oral transmucosal fentanyl, fentanyl administered as fentanyl pectin nasal spray is more rapidly absorbed, reaches higher maximum plasma concentrations and has greater bioavailability. In the treatment of BTPc in two randomized, double-blind, crossover trials in opioid-tolerant adults, fentanyl pectin nasal spray (100-800 μg titrated doses) was significantly more effective than placebo in reducing pain intensity and provided a significantly faster onset of pain relief than oral immediate-release morphine. During long-term treatment of BTPc episodes, fentanyl pectin nasal spray consistently provided effective pain relief in an open-label, 16-week trial. Most patients were satisfied or very satisfied with the ease of use and convenience of the nasal spray. Fentanyl pectin nasal spray 100-800 μg was generally well tolerated and was not associated with nasal tolerability problems.
芬太尼果胶鼻腔喷雾剂（PecFent®）采用了一种新型的果胶基给药系统，当应用于黏膜表面时，它会从水溶液转变为凝胶。芬太尼从鼻腔中形成的果胶凝胶中以受控的方式被吸收，其起效迅速，缓解疼痛的作用持续时间与癌症爆发性疼痛（BTPc）的典型发作过程相匹配。与口服经黏膜给予的芬太尼相比，给予芬太尼果胶鼻腔喷雾剂时，芬太尼吸收更快，达到更高的最大血浆浓度，生物利用度更高。在两项针对阿片类药物耐受成人的随机、双盲、交叉试验中，芬太尼果胶鼻腔喷雾剂（100-800μg 滴定剂量）在减轻疼痛强度方面明显优于安慰剂，并比口服即释吗啡更快地缓解疼痛。在长期治疗 BTPc 发作期间，芬太尼果胶鼻腔喷雾剂在一项开放标签、16 周的试验中持续提供有效的疼痛缓解。大多数患者对鼻腔喷雾剂的易用性和便利性感到满意或非常满意。芬太尼果胶鼻腔喷雾剂 100-800μg 一般耐受性良好，且不会引起鼻腔耐受性问题。
