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研究了环孢素柔性脂质体经小鼠皮肤给药的药动学行为 ,并与用新山地明小鼠灌胃给药进行了比较。将环孢素柔性脂质体非封闭性应用于小鼠皮肤 ,研究血药浓度的经时变化以及在肾脏和皮肤的分布状况。与灌胃给予同剂量新山地明的体内行为相比 ,柔性脂质体经皮给药后的相对生物利用度为 (82 .5 1± 5 .45 ) % ,肾脏组织AUC比值为 (15 0 .6± 15 .6 2 ) % ,皮肤中药物含量显著高于口服组 (P <0 .0 1)。结果表明环孢素柔性脂质体能有效经皮转运药物 ,在脂肪含量高的肾脏、皮肤组织分布较多。
The pharmacokinetics of ciclosporin-loaded liposomes on the skin of mice was studied and compared with the intragastric administration of cinobufacient mice. Cyclosporine-based flexible liposomes were applied to the skin of mice to study the changes of plasma concentration over time and their distribution in the kidney and skin. The relative bioavailability after transdermal delivery of flexible liposomes was (82.51 ± 5.45)% and that of kidney tissue was (15 0 .6 ± 15 .62%), the skin of the drug content was significantly higher than the oral group (P <0.01). The results show that cyclosporine flexible liposomes can effectively transdermal drug delivery, in the high fat content of the kidney, skin tissue distribution more.