吲哚美辛醇质体的研制与质量评价

Preparation and Quality Evaluation of Indomethacin Ethosomes

采用改进的pH梯度法制备吲哚美辛(1)醇质体,所得制品平均粒径为197.84 nm,包封率为(88.25±1.04)%。用Franz扩散池测试其对大鼠离体皮肤的渗透特性,并与1脂质体和搽剂对比。结果表明,1醇质体、1脂质体和搽剂的体外渗透速率分别为102.99、27.45和73.06 g·cm-2·h-1,给药4 h后皮内滞留量分别为96.54、78.52和36.62 g/cm2。用乙酸致小鼠扭体和甲醛致小鼠左前足疼痛试验考察制品的镇痛作用,用卡拉胶致小鼠左后足肿胀和二甲苯致小鼠耳肿胀考察其抗炎作用。结果表明,所制备的1醇质体抑制小鼠疼痛与炎症的效果均优于其脂质体和市售搽剂。

The indomethacin （1） ethosomes were prepared by an improved pH gradient method. The average particle size and the entrapment efficiency of the product were 197.84 nm and （88.25±1.04） %. The in vitro permeabilities of the product, 1 liposomes and the commercial liniment through the excised rat skin were investigated by Franz diffusion cell. The results showed that the permeation rates of the ethosomes, liposomes and liniment were 102.99, 27.45 and 73.06μg.cm-2.h-1, respectively. The retention amount in skin after applying these preparations for 4 h were 96.54, 78.52 and 36.62μg/cm2, respectively. The acetate-induced mice writhing and formaldehyde-induced mice left forefoot pain were employed to evaluate the analgesic effect of 1 ethosomes. And the anti-inflammatory effect was investigated by carrageenan-induced left hindfoot swelling and xylene-induced ear swelling experiments. The results showed that the anti-inflammatory and analgesic effects of the ethosomes on these mice were superior to the liposomes and commercial liniment.