Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China.
Drug Deliv Transl Res. 2017 Oct;7(5):617-624. doi: 10.1007/s13346-017-0392-5.
The tissue distribution and percutaneous drug absorption of indomethacin (IND) patches were studied using commercial IND as a comparison. The concentration of IND in skin, plasma, and muscle in mice was measured by LC-MS/MS, and the IND concentration in the dermis of rats was also monitored by microdialysis. After percutaneous administration, the "double-peak" phenomenon occurred in different tissues, and the IND concentration was ranked as skin first, followed by plasma and then muscle. In particular, skin acted as a reservoir for drug release, and the "secondary hump" in tissue distribution was attributed to the subsequent release of lipophilic IND in skin. It was concluded that examination of the tissue distribution and application of a microdialysis technique provided an effective means of evaluating indomethacin pharmacokinetics.
本研究采用市售吲哚美辛（IND）贴剂作为对照，考察了 IND 贴剂的组织分布和经皮吸收。采用 LC-MS/MS 测定了小鼠皮肤、血浆和肌肉中的 IND 浓度，并用微透析法监测了大鼠真皮中的 IND 浓度。经皮给药后，不同组织中出现“双峰”现象，IND 浓度依次为皮肤、血浆和肌肉。皮肤作为药物释放的储库，组织分布中的“二次驼峰”归因于皮肤中脂溶性 IND 的后续释放。研究认为，组织分布研究和微透析技术的应用为评价吲哚美辛的药代动力学提供了有效的手段。
