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  • 标题:Effect of Lipophilicity on in Vivo Iontophoretic Delivery. I. NSAIDs
  • 本地全文:下载
  • 作者:Yoshikazu TASHIRO ; Shozo SHICHIBE ; Yasuki KATO
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2001
  • 卷号:24
  • 期号:3
  • 页码:278-283
  • DOI:10.1248/bpb.24.278
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The effect of drug lipophilicity on in vivo iontophoretic transdermal absorption was evaluated. Non-steroidal anti-inflammatory drugs (NSAIDs) were selected as model drugs with a wide range of lipophilicity: salicylic acid (SA), ketoprofen (KP), naproxen (NP) and indomethacin (IM). Cathodal iontophoresis of NSAIDs was conducted in rats (0.625 mA/cm2; 90 min), and drug concentrations in skin, cutaneous vein and systemic vein were determined. Skin concentrations of NSAIDS were higher in the case of lipophilic drugs (SA=KP=NPKP=NP>IM). Additionally, the dependence of drug lipophilicity on systemic plasma concentration was similar to cutaneous plasma concentration. The transfer rate from skin to cutaneous vein (RSC) was calculated from the arterio-venous plasma concentration difference of drug in the skin. Normalized RSC by skin concentration (RSC/XS) yielded a negative correlation with the logarithm of n-octanol/buffer partition coefficient (Log P at pH 7.4), suggesting that transfer of NSAIDs from skin to cutaneous vein decreased with increasing lipophilicity (SA>KP=NP>IM). This correlation means that drug partitioning between stratum corneum and viable epidermis might be a dominant step.
  • 关键词:transdermal delivery;iontophoresis;lipophilicity;non-steroidal anti-inflammatory drug
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