0.03%他克莫司软膏的体外透皮吸收研究

Study on Percutaneous Absorption in vitro of 0.03% Tacrolimus Ointment

目的:研究0.03%他克莫司软膏经离体裸鼠皮的透皮吸收情况,并比较国产受试制剂与进口参比制剂的差异。方法:采用改良Franz扩散池法进行体外透皮试验,以高效液相色谱-质谱法(HPLC-MS)测定国产受试制剂和进口参比制剂0.03%他克莫司软膏的体外透皮渗透量、渗透速率和滞后时间。结果:受试制剂与参比制剂的24 h体外透皮累积渗透量分别为(3 907±1 191)、(3 896±1 064)ng/cm2,渗透速率分别为186.7、182.9 ng/(cm^2·h),滞后时间分别为1.95、2.00 h,二者差异无统计学意义(P>0.05)。结论:受试制剂有良好的透皮性能,其在裸鼠离体皮肤的透皮吸收性能与参比制剂相当。

OBJECTIVE：To study the percutaneous absorption of 0.03% Tacrolimus ointment,and to compare the difference of domestic test preparation and imported reference preparation. METHODS：Modified Franz diffusion cells were adopted in transdermal test in vitro;HPLC-MS method was used to determine permeation amount and rate in vitro,delay time of domestic test preparation and imported reference preparation 0.03% Tacrolimus ointment. RESULTS：24 h in vitro permeation amount of test and reference preparations were（3 907±1 191）and（3 896±1 064）ng/cm2;permeation rates were 186.7 and 182.9 ng/（cm2·h）;delay time were 1.95 and 2.00 h,respectively（P〉0.05）. CONCLUSIONS：Test preparation shows good percutaneous property,and is similar to reference preparation in penetration absorbency through nude mice skin.