Lim Stephen C B, Paech Michael J, Sunderland Bruce, Liu Yandi
Pharmacy Department, Armadale Health Service, Armadale, Australia.
Drug Des Devel Ther. 2013 Apr 12;7:317-24. doi: 10.2147/DDDT.S42619. Print 2013.
The objective of this study was to prepare a novel fentanyl wafer formulation by a freeze-drying method, and to evaluate its in vitro and in vivo release characteristics, including its bioavailability via the sublingual route.
The wafer formulation was prepared by freeze-drying an aqueous dispersion of fentanyl containing sodium carboxymethylcellulose and amylogum as matrix formers. Uniformity of weight, friability, and dissolution testing of the fentanyl wafer was achieved using standard methods, and the residual moisture content was measured. The fentanyl wafer was also examined using scanning electron microscopy and x-ray diffraction. The absolute bioavailability of the fentanyl wafer was evaluated in 11 opioid-naïve adult female patients using a randomized crossover design.
In vitro release showed that almost 90% of the fentanyl dissolved in one minute. In vivo, the first detectable plasma fentanyl concentration was observed after 3.5 minutes and the peak plasma concentration between 61.5 and 67 minutes. The median absolute bioavailability was 53.0%.
These results indicate that this wafer has potential as an alternative sublingual fentanyl formulation.
本研究的目的是通过冷冻干燥法制备一种新型芬太尼晶片制剂，并评价其体外和体内释放特性，包括其舌下途径的生物利用度。
通过冷冻干燥含有羧甲基纤维素钠和支链淀粉作为基质形成剂的芬太尼水分散体制备晶片制剂。使用标准方法实现芬太尼晶片的重量均匀性、脆碎度和溶出度测试，并测量残留水分含量。还使用扫描电子显微镜和X射线衍射对芬太尼晶片进行了检查。采用随机交叉设计在11名未使用过阿片类药物的成年女性患者中评估芬太尼晶片的绝对生物利用度。
体外释放显示，几乎90%的芬太尼在1分钟内溶解。在体内，3.5分钟后观察到首次可检测到的血浆芬太尼浓度，血浆浓度峰值出现在61.5至67分钟之间。中位绝对生物利用度为53.0%。
这些结果表明，这种晶片有潜力作为舌下芬太尼的替代制剂。
