环孢素脂质体滴眼液在兔眼组织的吸收

目的　研究环孢素脂质体滴眼液在兔眼组织的吸收。方法　 4 2只家兔 ,随机分成 0 .2 5、0 .5、1.0、2 .0、4 .0、6 .0、8.0h 7个时间组 ,每一时间组 6只家兔 (12只眼 ) ,右眼应用环孢素橄榄油滴眼液 ,左眼应用环孢素脂质体滴眼液。用药后分别在 7个时间点抽取房水 ,于 0 .5、1.0、2 .0h摘取眼球 ,分离角膜、虹膜、巩膜 ,采用高效液相色谱 质谱法测定各种组织中环孢素的含量 ,并计算药动学参数和脂质体制剂的相对生物利用度。结果　脂质体制剂吸收进入眼组织的环孢素浓度高于橄榄油制剂 ,且有显著性差异 (P <0 .0 5 )。房水的药代动力学结果表明 ,脂质体和橄榄油滴眼液的Tmax无显著性差异 ,但Cmax之间有显著性差异 (P <0 .0 1) ;脂质体滴眼液组的相对生物利用度明显高于橄榄油滴眼液组。结论　脂质体可以显著改善环孢素在眼部的吸收 ,提高药物在眼部各组织的分布及环孢素的生物利用度

Experimental study on the ocular absorption of liposomal cyclosporin in rabbits

Objective To study the ocular absorption and distribution of liposomal cyclosporin in rabbits.Methods Forty-two rabbits were instilled topically to eye with cyclosporin olive oil solution and liposomal cyclosporin.Following instillation,the aqueous humor were drew out with injector from anesthetic rabbits at 0.25,0.5,1,2,4,6,8h;the cornea,aqueous humor,iris and sclera were obtained from sacrificed rabbits at 0.5,1,2h.The concentration of cyclosporin were measured in various tissues by HPLC-MS method.Results The concentration of cyclosporin in various tissues with liposome was higher than that with cyclosporin olive oil solution,and most of them had significant differences.Conclusion Liposomal cycloporin enhances the absorption and increases the level of cycloporin in ocular tissues.