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目的:考察醇质体作为尼美舒利经皮给药载体的体外渗透性及刺激性。方法:采用注入法制备尼美舒利醇质体,采用Franz扩散池和鼠皮进行体外渗透实验,HPLC测定药物浓度并计算药物稳态透皮速率、12 h累积释放量及皮内滞留量;采用小鼠皮肤红斑平均积分考察尼美舒利醇质体刺激性。结果:测得尼美舒利醇质体的稳态经皮渗透速率和12 h累积释放量分别是(16.28±1.68)μg.(cm2.h)-1,(195.38±19.89)μg/cm2,与脂质体相比提高了1.9倍(P<0.05);而醇质体的皮内滞留量为(318.67±38.57)μg/cm2,仅是脂质体的1.07倍(P>0.05)。皮肤刺激性实验显示,NIM醇质体的红斑指数与生理盐水的差异并不明显(P>0.05)。结论:尼美舒利醇质体的经皮渗透性和皮肤刺激性都优于脂质体,是一种有效的经皮给药制剂。
OBJECTIVE: To investigate the in vitro permeability and irritation of ethosomes as transdermal delivery of nimesulide. Methods: Nimesulide plasmids were prepared by injection method. Franz diffusion cells and rat skin were used for in vitro permeation test. The drug concentration was determined by HPLC and the steady-state transdermal rate of drug, cumulative release of 12 h and intradermal retention were calculated. Mice skin erythema average score using nimesulide alcohol plastid irritation. RESULTS: The steady-state transdermal permeation rate and cumulative 12-h release of nimesulide were (16.28 ± 1.68) μg.cm 2 · h -1, 195.38 ± 19.89 μg / cm 2, (P <0.05). The intradermal retention of ethosomes was (318.67 ± 38.57) μg / cm2, which was only 1.07 times that of liposomes (P> 0.05). Skin irritation experiments showed that there was no significant difference between the erythrocyte index of NIM and the normal saline (P> 0.05). Conclusion: Nimesulide ethosomes are superior to liposomes in percutaneous permeability and skin irritation, which is an effective preparation for transdermal delivery.