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| Asian Journal of Pharmaceutical Sciences 2008, 3(3): 122-130 ISSN: 1818-0876 CN: |
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Formation of flurbiprofen-ethanolamine complexes
and their in vitro permeation across rat skin
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Caixia Feng1, Yanli Yang1, Ruolan Xiao1, enyan Qin1, Hui Song2, Xing Tang1, Hui Xu1,*
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1School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 110016, China
2School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang 110016, China
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Received
2007-10-22
; Revised
2008-1-14
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Accepted
2008-4-30
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Online
2008-6-30
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Abstract
Purpose: The purpose of this study was to prepare flurbiprofen (Flu) ethanolamine complexes (Flu-EAs) with appropriate physico-
chemical properties, and investigate their transdermal permeability. Methods: Flurbiprofen monoethanolamine (Flu-MEA) and flurbiprofen triethanolamine (Flu-TEA) complexes were prepared and characterized by DSC and FTIR measurements. The in vitro permeation properties of Flu and Flu-EAs through full-thickness rat skin were investigated using side-by-side diffusion cell systems and with various commonly used pharmaceutical plasticizers or penetration enhancers as the solvents to dissolve the drugs. Results: Flu-MEA and Flu-TEA had lower melting temperatures and octanol/water partition coefficients. The transdermal permeability of the salts was obviously higher than Flu in all the plasticizers and enhancers used. The transdermal permeability of Flu and Flu-EAs in plasticizers was in order of DBS > DBP > TEC > PEG400. The mixtures of penetration enhancers containing Azone provided better enhancing ability for both Flu and Flu-EAs. Conclusion: The in vitro transdermal permeability of Flu can be effectively improved through complex-formation of Flu with monoethanolamine or triethanolamine.
Keywords:
Flurbiprofen
Ethanolamine
Transdermal permeation
Plasticizer
Penetration enhancer
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