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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(英文)

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

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【作者】 李英剑; 潘妍; 徐晖; 魏刚; 郝劲松; 郑俊民;

【Author】 Li Yingjian 1* , Pan Yan 1, Xu Hui 1, Wei Gang 1, Hao Jingsong 2 and Zheng Junmin 11 School of Pharmacy, Shenyang Pharmaceutical University, Shengyang 110016; 2 Department of Pharmacy, National University of Singapore, Singapore 119260

【机构】 新加坡国立大学药学院; 沈阳药科大学; 新加坡国立大学药学院 新加坡119260; 新加坡119260; 沈阳110016; 新加坡119260;

【摘要】 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 0 6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 2 6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。

【Abstract】 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.

  • 【文献出处】 Journal of Chinese Pharmaceutical Sciences ,中国药学(英文版) , 编辑部邮箱 ,2002年03期
  • 【分类号】R969.1
  • 【被引频次】2
  • 【下载频次】165
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