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目的:研制丁卡因脂质体凝胶剂,为临床新制剂的开发提供参考。方法:以逆相蒸发—超声法等制备丁卡因脂质体凝胶剂;并采用改良Franz扩散池体外经皮渗透实验技术,对丁卡因脂质体凝胶剂及其普通凝胶剂的经皮渗透作用进行了比较。结果:丁卡因脂质体平均粒径为105.5 nm,平均包封率为 63.8％;体外透皮实验中,12 h累积透皮吸收百分率(Q％)为34.6％,明显高于普通凝胶制剂(17.7％);皮内药物滞留百分率(Q_滞％)分别为24.6％,明显高于普通凝胶制剂(0.65％)。结论:丁卡因脂质体凝胶剂有望成为适于临床给药的一种新剂型。
Objective: To develop tetracaine liposome gel and provide a reference for the development of new clinical preparations. Methods: The tetracaine liposome gel was prepared by reverse phase evaporation - ultrasonic method. The percutaneous permeability test of modified Franz diffusion cell was used to evaluate the effects of tetracaine liposome gel and its common gel Transdermal permeation was compared. RESULTS: The average tethering rate of tetracaine liposomes was 105.5 nm with an average entrapment efficiency of 63.8%. In vitro transdermal experiments, the cumulative transdermal absorption percentage (Q%) at 12 h was 34.6%, which was significantly higher than that of ordinary gel (17.7%). The percentage of drug retention (Q_% hysteresis) in intradermal skin was 24.6%, which was significantly higher than that of common gel preparation (0.65%). Conclusion: Tetracaine liposome gel is expected to become a new dosage form suitable for clinical administration.