双氯芬酸钠柔性脂质体的研究

目的 研究双氯芬酸钠柔性脂质体，为临床新制剂的开发提供参考。方法 以逆相蒸发－超声法制备双氯芬酸钠柔性脂质体，并对其性态、包封率、透过率、体外透皮以及抗炎药效学进行了试验。结果 双氯芬酸钠柔性脂质体平均粒径为81.5nm，平均包封率为73．12％；在0.3MPa外压作用下，柔性脂质体的透过速率平均达到水的90％；体外透皮实验中，24h累积透皮吸收百分率Q％为58．62％，优于普通脂质体和凝胶剂；对角叉菜胶所致的炎症有显著的抑制作用，比其凝胶剂作用持久。结论 双氯芬酸内柔性脂质体有望成为适于临床给药的一种新剂型。

Study on diclofenac sodium flexible liposomes

OBJECTIVE To study diclofenac sodium flexible liposomes in order to develop a new therapeutic preparation.METHODS Diclofenac sodium transfersomes was prepared by reverse phase evaporation and then sonication.The appearance,embedding ratio,ratio of permeation,skin penetration in vitro and the pharmacodynamic tests were investigated respectively.RESULTS The mean diameter of the flexible liposomes was 81.5 nm, mean embedding ratio was 73.12%.Under the pressure of 0.3 MPa, its ratio of permeation was 90% compared with water. The test in vitro showed that the accumulated penetration (Q%) of the flexible liposomes after 24h was 58.62%,more than conventional liposomes and gels. The flexible liposomes had significant anti inflammatory effect on the inflammatory swelling induced by carrageenin,with longer action time than gels.CONCLUSION Flexible liposomes may become a promising carrier of diclofenac sodium for clinical use.