盐酸青藤碱醇质体凝胶与脂质体凝胶体外经皮渗透动力学比较研究

摘要

目的:比较盐酸青藤碱醇质体凝胶(SHEG)与其脂质体凝胶(SHLG)的体外经皮渗透行为,以期为筛选出较优的盐酸青藤碱(SH)经皮吸收制剂奠定基础.方法:制备SHEG与SHLG;以离体鼠皮为屏障,采用Franz扩散池法对其体外经皮渗透行为进行比较研究.结果:两种制剂的经皮渗透动力学均符合Higuchi方程,即SHLG:Q=27.22t1/2-16.04(r=0.996 5);SHEG:Q=33.46t1/2-19.59(r=0.995 0),稳态透皮速率J分别为27.22 μg·cm-2·h-1和33.46 μg·cm-2·h-1,在经皮渗透24 h后,皮肤内的蓄积量分别为21.05 μg·cm-2和18.95 μg·cm-2,凝胶中的残留量为53.44 μg·cm-2和48.09 μg·cm-2.两种SH制剂比较,以上参数差异均有统计学意义(P<0.05).结论:与SHLG相比,SHEG在促进药物经皮吸收方面具有更好的效果.%Objective: To compare the in vitro transdermal penetration of sinomenine hydrochloride ( SH ) ethosomal gels ( SHEG ) and liposomal gels ( SHLG ) to screen the optimal external preparation for SH. Method: SHEG and SHLG were prepared. Skipped mouse skin as the barrier, the in vitro transdermal penetration of the two preparations was studied and compared using Franz diffusion cells. Result: The in vitro transdermal penetration of the two preparations was fitted Higuchi equation, Q = 27.22t1/2 - 16. 04( r = 0. 996 5) for SHLG and Q=33.46t1/2-19.59(r = 0. 995 0) for SHEG. The stability penetration rate ( J ) was 27.22 μg · cm-2 · h -1 and 33. 46μg · cm-2 · h-1 , respectively. After 24h transdermal penetration, the SH cumulative amount in skin and residual a-mount in the gels was 21. 05μg · cm-1 and 18. 95 μg · cm-1 , 53. 44 μg · cm-1 and 48. 09 μg · cm-1 , respectively. The above indices all showed significant difference between the two preparations( P <0. 05 ). Conclusion: Compared with SHLG, SHEG exhibits better transdermal enhancement in vitro.