丁卡因凝胶剂的研制与药效测定

 目的：研究各种透皮促进剂对丁卡因经皮渗透的影响，找出一种起效时间较短的丁卡因凝胶剂。方法：配制不同处方的丁卡因凝胶剂，采用Franz扩散小池，HPLC检测药物浓度进行离体皮肤渗透实验，然后采用针刺法进行在体药效测定。结果：月桂氮酮使丁卡因透皮速率提高，但滞后时间延长，在体麻醉效果不佳；单用乙醇不延长滞后时间，在体麻醉起效时间缩短。结论：含乙醇的丁卡因凝胶剂局麻效果最好，可以开发利用。

Preparation of percutaneous tetracaine gels and in vivo effects assessment

OBJECTIVE: To study the effect of penetration enhancers on the transdermal delivery of tetracaine and find a percutaneous tetracaine formulation with short onset time. METHODS: In vitro permeability of tetracaine from various gels was studied by using Franz diffusion cells. Then a double blinded trial was undertaken to assess the practical effects of these gels through pinprick method. RESULTS: Laurcapram could increase permeation flux of tetracaine obviously, especially when propylene glycol and ethanol were presented, but these gels showed poor anaesthetic effects with prolonged lag time. Ethanol alone did not prolong lag time and increase rapidity of action. CONCLUSION: Tetracaine gel containing ethanol would be a new formulation with ideal local anaesthetic effect.