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  • 标题:Effect of Permeation Enhancers on the in Vitro Percutaneous Absorption of Pentazocine1)
  • 本地全文:下载
  • 作者:Takayuki Furuishi ; Sachiko Oda ; Hiroaki Saito
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2007
  • 卷号:30
  • 期号:7
  • 页码:1350-1353
  • DOI:10.1248/bpb.30.1350
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:The effect of permeation enhancers on the percutaneous absorption of pentazocine (PTZ) was investigated in excised hairless mice using Franz diffusion cells in vitro . The enhancing effect on the percutaneous absorption of PTZ from the isopropyl myristate (IPM) solution system was improved with glyceryl monocaprylate (GEFA-C8), which is a kind of glycerol ester of fatty acid (GEFA). The flux of PTZ through the skin was ca. 4 times higher compared with IPM alone, while a less enhancing effect of glyceryl dicaprylate (GEFA-DiC8) and glyceryl tricaprylate (GEFA-TriC8) on the skin permeation of PTZ was found. Moreover, maximum enhancement of PTZ flux was observed with glyceryl monocaproate (GEFA-C6) among various alkyl chains (C2—C18) of monoglycerides. These results indicated that the IPM solution system combination with GEFA may be used to develop a transdermal formulation with improved skin permeation of PTZ.
  • 关键词:pentazocine;permeation enhancer;isopropyl myristate;glycerol ester;hydrophilic-lipophilic balance (HLB)
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