吡罗昔康口服和局部给药后药物动力学和局部组织的分布

目的 研究大鼠吡罗昔康局部给药的药物传递和机理。方法 大鼠分别局部给药和口服4mg吡罗昔康后，用HPLC法测定局部给药部位的皮肤、肌肉、关节和血液的药物浓度。结果 口服给药后，Tjoint/Plasma和Tmus/Plasma比值保持恒定，大部分的时间其值介于0．06和0．2。比较而言，局部给药后，Tjoint/Plasma和Tmus/Plasma比值分别介于0．2到1．26和1．89到5．4之间。比值远远大于口服给药。结论 数据表明局部给药后，到达局部深层组织的吡罗昔康来自于药物的直接渗透；当药物的靶向部位在局部时局部给药优于口服给药。

Pharmacokinetics and Local Tissue Disposition of Piroxicam Following Topical and Oral Application in Rats

Objective To investigate the drug delivery and mechanism of topical administration of piroxicam in rats Methods Four milligrams of piroxicam were administered to Wistar rats by either oral or topical routes The drug concentrations in plasma, local tissues were determined by HPLC Results After oral application, the T joint /Plasma and T muscle / Plasma ratios kept unchanged During most of the experimental time(0-24 h), the values varied between 0 06 and 0 2 In contrast, the T joint /Plasma and T muscle / Plasma ratios after local application varied from 0 2 to 1 26 and from 1 89 to 5 4 respectively and were much higher than the ones by oral application Conclusion The results showed that most piroxicam reaching the local deep tissues was attributed to the direct penetration and topical delivery is superior to oral application when the drug's target is local tissues under skin.