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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。
Objective: To study the effects of various transdermal accelerators on tetracaine transdermal penetration and to find a tetracaine gel with shorter onset time. Methods: Tetracaine gel formulations with different prescriptions were prepared. Franz diffusion cells were used to determine the drug concentration in vitro. The in vitro skin penetration test was carried out. The in-vivo efficacy was determined by acupuncture. Results: Azinonin could increase the transdermal rate of tetracaine but prolonged the lag time, and had poor anesthesia in vivo. The lag time was shortened with ethanol alone and the onset time of anesthesia was shortened. Conclusion: The ethanol-containing tetracaine gel has the best local anesthetic effect and can be developed and utilized.