摘要
目的制备眼用阿奇霉素脂质体原位凝胶,并对其体外释放行为和刺激性进行考察。方法薄膜分散法制备阿奇霉素脂质体,将其分散于泊洛沙姆407(P407)中制备阿奇霉素脂质体凝胶,根据胶凝温度筛选P407浓度,双室法对该制剂的体外释药行为进行考察,荧光示踪法测定制剂眼部滞留时间,同体自身对照观察制剂的眼部刺激性。结果处方中P407最佳浓度为20%,脂质体凝胶中药物的释放明显慢于其他制剂,眼部滞留时间(28.1±5.5)min,明显长于其他三种剂型(P<0.05),且对兔眼无刺激。结论 P407原位脂质体凝胶缓释特性突出、刺激性低,适合作为阿奇霉素眼用给药载体。
AIM To prepare the ocular liposomal gel for azithromycin, study its release in vitro and ocular irritation. METHODS Azithromycin liposome was prepared by film dispersion method, and dispersed it in poloxamer 407 （P407） to prepare azithromycin liposomal gel, the best concentration of P407 was selected according to the temperature of gel. The two- compartment in vitro method was used to evaluate azithromycin release from azithromycin liposomal gel, ocular residence time was determined by fluorescence- labeled technique, ocular safety was evaluated by ocular irritation test in rabbit. RESULTS The best concentration of P407 in prescription was 20%, azithromycin release from the liposomal gel was slower than other preparations, the ocular residence time was （28.1 ± 5.5） min, which was much longer than other preparations （P 〈 0.05） , and it had no irritation after ocular administration. CONCLUSION With a more sustained release and less irritation, P407 liposomal insitu gel is a suitable vehicle for ocular administration of azithromycin.
出处
《中国新药与临床杂志》
CAS
CSCD
北大核心
2014年第12期907-910,共4页
Chinese Journal of New Drugs and Clinical Remedies
