AAPS PharmSciTech. 2013 Dec;14(4):1279-83. doi: 10.1208/s12249-013-0020-8.
The aim of this study was the optimization of a lidocaine-based film formulation for the prevention of pain from needle prick during the injection of local anesthetic in dentistry. Film performances were evaluated in vitro by studying lidocaine permeation across pig esophageal epithelium as model for nonkeratinized buccal mucosa. The results obtained showed that the molecular weight of the film-forming polymer had no effect on lidocaine transport. The introduction of the adhesive Plastoid® into the film determined a significant increase of drug permeation rate, which was further improved by the addition of Azone®. On the contrary, the effect of sodium taurocholate was negligible.
本研究的目的是优化一种基于利多卡因的薄膜配方，以预防牙科局部麻醉注射时针刺疼痛。通过研究利多卡因在猪食管上皮组织中的渗透情况，评估薄膜在体外的性能，猪食管上皮组织可作为非角化颊黏膜的模型。结果表明，成膜聚合物的分子量对利多卡因的传递没有影响。将粘性 Plastoid®引入薄膜中会显著增加药物渗透速率，而添加 Azone®则会进一步提高渗透速率。相反，牛磺胆酸钠的作用可以忽略不计。
