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Synthesis and Enhancing Effect of 5,9-Dimethyl-1-decanol on the Transport of 5-Fluorouracil and Tramadol Hydrochloride Across the Excised Rat Skin

Hanif Raja, Ping Qineng*, Mo Fenzhu, Liu Guojie   

  1. Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009
  • Received:1997-12-25 Revised:1998-05-24 Online:1999-03-15 Published:1999-03-15
  • Contact: Ping Qineng*

Abstract: New alcohol derivative of tetrahydrogeraniol (THG), an acyclic monoterpene,has been synthesized by reacting THG with Grignard reagent and ethylene oxide. The enhancingeffect of the synthesized derivative, 5,9-dimethyl-1-decanol (DIMDOL) on the penetration of 5-fluorouracil (5-FU) and tramadol hydrochloridc across the excised rat skin was studied by an in vitropermeation technique using two chamber diffusion cells. Azone and THG were used as standardenhancers for comparison. DIMDOL enhanced the permeability of 5-FU and tramadol hydrochloride18.60 fold and 73.19 fold across full-thickness skin with a lag time of 3. 35 h and 1.20 h respectively.Increased partition coefficient and diffusion coefficient values were obtained by this enhancer. Theseresults suggest that DIMDOL mainly affects the stratum corneum and interacts with both lipid-richlayers and keratin-rich layers.

Key words: 5-Fluorouracil, Tramadol hydlochloride, 5,9-Dimethyl-1-dccanol, Azone, Tetrahydrogeraniol, Percutaneous absorption

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