伊曲康唑脂质体在小鼠体内的组织分布

Tissue Distribution of Itraconazole Liposomes in Mice

目的考察伊曲康唑脂质体在小鼠体内的组织分布。方法昆明种小鼠尾静脉注射伊曲康唑脂质体及伊曲康唑注射液(15mg·kg-1),采用LC-MS/MS测定组织中不同时间的药物浓度。结果与伊曲康唑注射液相比,伊曲康唑脂质体在小鼠肝、脾组织中的分布显著增加,AUC分别为注射液的1.95和3.47倍;伊曲康唑脂质体在心、肾中的分布显著降低,AUC分别为注射液的29.9%和40.9%;伊曲康唑脂质体延长了药物在血浆中的滞留时间,MRT为对照组的2.7倍。结论与注射液组相比,伊曲康唑脂质体在血浆和心、肝、脾、肾组织中分布具有显著性差异。

OBJECTIVE To investigate in vivo tissue distribution of itraconazole liposomes in mice. METHODS Intraconazole liposomes and intraconazole injections were administmed by intravenous injection in mice （15 mg itraconazole per kg body weight） and the distribution of itraconazole in the organs at different time points was measured by LC-MS/MS. RESULTS Compared with itraconazole injections, itraconazole liposmoes showed higher tissue distribution in liver and spleen significantly and the AUC were as 1.97 and 3.47 times as that of itraconazole injections; itraconazole liposomes in heart and kidney were decreased remarkably and the AUC were 29.9% and 40.9% as that of itraconazole injections respectively. Compared with itraconazole injections, itraconazole liposomes prolonged the circulation time in plasma. The MRT of liposomes was 2.7 times as that of itraconazole injections. CONCLUSION There is significant difference in plasma, heart, liver, spleen and kidney tissue distribution of mice between itraconazole liposomes and itraconazole injections.