利多卡因微乳凝胶剂的制备及初步药效学研究

目的制备利多卡因微乳凝胶剂,并对其药效学及皮肤刺激性进行初步研究。方法以油酸乙酯为油相,聚山梨酯-80为表面活性剂,无水乙醇为助表面活性剂,用水滴定的方法制备利多卡因微乳。以卡波姆940为凝胶骨架,采用直接溶胀法制备利多卡因微乳凝胶。采用Zetasizer Nano-ZS90马尔文激光粒度仪测定微乳的粒径。采用日立H-7650透射电子显微镜观察微乳的形态。采用热板法观察该药对小鼠的镇痛作用。采用连续给药的方法,考察该药对家兔正常皮肤与破损皮肤的刺激性。结果利多卡因微乳凝胶外观为白色透明凝胶态,微乳呈圆球形,微乳粒径<100 nm。利多卡因微乳凝胶剂能延长热板致痛的潜伏期,对家兔皮肤无刺激性。结论利多卡因微乳凝胶剂具有较好的局麻镇痛作用和安全性。

Preparation and Preliminary Pharmacodynamics of Llidocaine Gel-microemulsion

OBJECTIVE To prepare llidocaine gel-microemulsion, and study the pharmacodynamic effects of llidocaine gel-microemulsion. METHODS To use ethylis oleate as oil phase, Polysorbate 80 as surfactant, ethanol as cosurfactant, we prepared lidocaine microemulsion by water titration method. With Carbopol 940 as a substrate, we prepared microemulsion-based gel of lidocaine by direct swelling method. To measure particle size of lidocaine microemulsion with Zetasizer Nano-ZS90. With transmission electron microscope, to observe the lidocaine microemulsion morphologic. With hot plate, the antinociception effects of the drug in mice was observed. To study the Skin irritation by the method of continuous administration of the drug. RESULTS The appearance of llidocaine gel-microemulsion was transparent white gel, the shape of microemulsion was sphere, Particle size of microemulsion was less than 100 nm. Llidocaine gel-microemulsion had the significant effect of the analgesic, it caused no irritability to rabbit skin. CONCLUSION Llidocaine gel-microemulsion has good analgesic effects and safety.