环孢菌素A外用实验研究

Experimental studies of skin penetrating capacity and external application of cyclosporin A

目的 从定性、定时二方面探讨环孢菌素A透皮能力。方法 通过对豚鼠的活体、体外透皮实验及抑制实验测定CYA透皮能力。结果 ①环孢菌素A在活体透皮实验中 ,在促渗剂相同的条件下 ,随CYA浓度增加透皮量增加。②环孢菌素A在活体透皮实验中 ,在相同的CYA浓度条件下加入促渗剂氮酮透皮量多于加入丙二醇透皮量。③环孢菌素A在离体透皮实验中 ,在促渗剂相同的条件下随CYA浓度增加透过量增加。④环孢菌素A在离体透皮实验中 ,在相同浓度CYA不同促渗剂条件下 ,加入氮酮透过量优于加入丙二醇。结论 ①在活体、离体透皮实验及抑制实验中都证明环孢菌素A可透过皮肤。②在适当条件下 ,CYA不仅可以透过皮肤而且透过率很大。

Objective To make quantitative and qualitative experimental studies of the skin-penetrating capacity and external application of cyclosporin A(CYA) .Methods Skin penetrating capacity testing and suppression testing were performed in guinea pig.Results ① When using 2% Azone as the same penetration-aiding agent, bolld CYA level was significantly higher ( P <0.01) in the high (5%) dose group than in the middle (3.7%) one, and also higher( P <0.01) in the middle than in the low (2.5%) . ② At the same CAY dose of 3.7%, the bolld CYA level was higher ( P <0.01) with 2% Azone than with 2.5% propylene glycol as penetration-aiding agent . ③ The dose effect relationship of the in vitro CYA test was also evident , as the penetration of CYA became significantly intensive with the increase of CYA dose and action duration under the presence of the same penetration aiding agent . ④ As CYA penetration aiding agent of in vitro test , 2% Azone was more effective than 2.5% propylene glycol .Conclusion ① Cyclosporin A can penetrate skin , as shown by the in vivo and in vitro penetration test and dermatitis -inhibiting test . ②The skin penetration rate of CYA can be substantially improved by using appropriate conditions. ③The cyclosporin A effect in inhibiting contact dermatitis of guinea pigs is dependent on the drug dose .