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Pharmaceutisch Weekblad

, Volume 10, Issue 5, pp 189–192 | Cite as

Comparison of penetration-enhancing ability of laurocapram, N-methyl-2-pyrrolidone and dodecyl-L-pyroglutamate

  • Jan Příborský
  • Kozo Takayama
  • Tsuneji Nagai
  • Danuše Waitzová
  • Jiří Elis
  • Yuji Makino
  • Yoshiki Suzuki
Original Articles

Abstract

The study reports on penetration enhancers used to improve drug absorption through the skin. All experiments were carried out in permeation cellsin vitro. Insulin (2.5 mg/ml) and Brilliant Blue (50.0 mg/ml) served as model drugs. They were formulated into a 40% solution of propylene glycol with increasing concentrations ofN-methyl-2-pyrrolidone (NMP) (0.0 to 20.0%), dodecylazacycloheptan-2-one (laurocapram) and a new compound dodecyl-l-pyroglutamate (DLP; 0.0 to 0.5%). The maximum amount of insulin permeated within 24 h was almost 200 μU/ml in the case of 0.1% laurocapram, while in the case of 0.1% DLP it was approximately half of that. The optimum concentration of NMP was 12.0%. Experiments performed with Brilliant Blue showed no significant difference among formulations containing either 6.0, 12.0 or 20.0% of NMP. When NMP was omitted, flux, permeability as well as the maximum concentration estimated after 26 h reached 50% of the values obtained with NMP. The lag time was twice as long in this case in comparison with the formulations containing NMP.

Keywords

Absorption, transdermal Brilliant Blue Dodecyl-l-pyroglutamate Insulin Laurocapram N-Methyl-2-pyrrolidone Permeability, enhancement 

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Copyright information

© Bohn, Scheltema & Holkema 1988

Authors and Affiliations

  • Jan Příborský
    • 1
    • 2
  • Kozo Takayama
    • 1
  • Tsuneji Nagai
    • 1
  • Danuše Waitzová
    • 3
  • Jiří Elis
    • 3
  • Yuji Makino
    • 3
  • Yoshiki Suzuki
    • 3
  1. 1.Faculty of Pharmaceutical SciencesHoshi UniversityTokyoJapan
  2. 2.State Institute for Drug ControlPraha 10Czechoslovakia
  3. 3.Teijin Ltd.Institute for Biomedical ResearchTokyoJapan

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