莫匹罗星软膏的体外透皮吸收

摘要

目的 比较莫匹罗星软膏实验制剂和市售参比制剂的透皮吸收效果,探讨莫匹罗星软膏中药物体外透皮吸收的动力学模式.方法 采用高效液相色谱法,Inerstil ODS-SP色谱柱(4.6 mm×150 mm,5μm);流动相:0.1 mol·L-1磷酸二氢钠缓冲液(1 mol·L-1氢氧化钠溶液调节pH值至6.3)-乙腈(75:25);检测波长:230 nm;流速:1.0 mL·min-1.体外透皮实验采用改良的单室Franz扩散池,以巴马香乳猪皮作为体外透皮实验皮肤,对两组软膏的透皮吸收结果进行对比,分别在不同时间点取样测定透皮接收液中药物的浓度,计算累积透皮量.结果 亲水性释放液平均回收率为99.4％,RSD为1.2％(n=9).亲脂性释放液平均回收率为99.0％,RSD为1.3％(n=9).两组制剂12 h内不同时段透皮吸收累积量差异无统计学意义.自制样品与参比制剂在亲水性释放液中药物渗透释放近似符合零级释药方程;在亲脂性释放液中药物渗透释放符合Higuchi方程.结论 莫匹罗星软膏中药物的释放在亲水性介质中呈零级动力学模式,在亲脂性介质中符合Higchi方程动力学模式.%Objective To compare the percutaneous absorption of experimentally prepared mupirocin ointment and commercially sold mupirocin ointment, and to study the dynamics mode of transdermal absorption of mupirocin ointment. Methods Inerstil ODS-SP column (4.6 mm× 150 mm,5 μm) was used with a mixture of 0.1 mol·L-1 sodium dihydrogen phosphate buffer solution (pH value was adjusted to 6.3 by 0.1 mol·L-1 sodium hydroxide solution) and acetonitrile (75:25) as a mobile phase by HPLC.The detection wavelength was set at 230 nm.The flow rate was 1.0 mL·min-1 .Improved Franz type diffusion cells were used for in vitro permeation studies and excised Obama Suckling pig skins in vitro were used as the transdermal barrier.The concentration of the receptor solution was determined by HPLC to investigate its cumulative permeation quantities at different time and the two sets of ointment were compared. Results The average recovery rate of hydrophilic medium was 99.4％,and RSD was 1.2％(n= 9).The average recovery rate of lipophilic medium was 99.0％,and RSD was 1.3％(n= 9).There was no significant difference of the concentration between two ointment within 12 h.The osmotic release of the drug of the sample and the reference preparation, which were in hydrophilic medium, was similar to that of the Zero equation, and roughly Higuchi equation in the lipophilic medium. Conclusion The results showed that the release behavior of mupirocin ointment followed Zero equation in the hydrophilic medium,and Higchi equation in the lipophilic medium.