酮咯酸氨丁三醇凝胶剂体外经皮渗透研究

Study on the permeation of ketorolac tromethamine from gels through rat skin in vitro

目的:考察凝胶剂作为酮咯酸氨丁三醇透皮给药载体的可行性。方法:制备卡波姆940药物凝胶,采用Franz扩散池用离体大鼠皮肤进行体外经皮渗透实验,以HPLC法测定渗透介质中药物含量并求算累积渗透量及稳态透皮速率。结果:以1.0%卡波姆940为凝胶基质,以硼砂溶液调节凝胶的pH为6.0时所制备的凝胶为最佳凝胶基质。3%的月桂氮芯卓酮及5%的丙二醇均可以显著提高凝胶中药物的经皮渗透,且两者联用存在协同作用。结论:本实验的凝胶基质可为生产提供参考依据。

OBJECTIVE To evaluate the permeation of ketorolac tromethamine from gels through rat skin. METHODS The carbopol gels containing the drug were formulated. The permeation test in vitro was carried out by using Franz diffusion cell. The concentration of ketorolac tromethamine in receptor medium was measured by HPLC. Then the cumulative penetration （Q） and the penetration rate （J58） were calculated. RESULTS It was shown that 1% of carbopol 940 （the pH of gels was adjusted to 6. 0） was the optimum matrix. 3% azone and 5 % propylene glycol significantly enhanced the permeation of the drug from gels through rat skin respectively, and combination with azone and propylene glycol could lead to synergistic effect. CONCLUSION The optimized gel base material can act as bases for the production of ketorolac gel.