他克莫司软膏的体外透皮吸收研究

Percutaneous absorption of Tacrolimus ointment in vitro

目的研究他克莫司软膏对离体巴马香猪皮的透皮吸收情况,并比较他克莫司软膏的供试制剂与参比制剂的体外透皮渗透量和渗透速率。方法采用改良Franz扩散池法,用反相HPLC法定量测定接受室溶液中他克莫司浓度及皮内滞留药物。结果他克莫司经离体巴马香猪皮的透过率随时间的延长而增加;48 h内,他克莫司软膏的供试制剂与参比制剂经离体巴马香猪皮的累积透过量分别为22.87±1.31、21.61±2.26μg·cm-2,平均渗透速率分别为0.7669、0.7149μg·cm-2·h-1。结论在透皮吸收研究中,他克莫司软膏的供试制剂与参比制剂的透皮渗透程度和渗透速率差异无统计学意义。

OBJECTIVE To investigate the percutaueous absorption of Tacrolimus ointment through the skin of Bama miniature pig, and compare in vitro permeation of the test and reference preparation. METHODS The concentrations of Tacrolimus in samples and skin tissues were determined by HPLC under the model of Franz diffusion cells in vitro. RESULTS The permeability of Tacrolimus across the skins of Bama miniature pig was time - dependently increased. The accumulation of infiltration capacity of test and reference ointments across Bama miniature pig skins within 48 h were 22.87 ± 1.31 and 21.61±2.26 μg-cm-2 ,respectively. Mean permeation velocity were 0. 7669 and 0.7149 μg-cm-2 .h-1. CONCLUSION The penetration absorbency through Bama miniature pig skins of test Tacrolimus ointment is similar to reference preparation.