Adsorption of the decapeptide Cetrorelix depends both on the composition of dissolution medium and the type of solid surface

Eur J Pharm Sci. 2004 Feb;21(2-3):191-6. doi: 10.1016/j.ejps.2003.10.008.

Abstract

High performance liquid chromatography (HPLC) analysis of increasing amounts of the decapeptide Cetrorelix, a potent antagonist of the luteinising hormone-releasing hormone, in distilled water resulted in a poor and variable response when solutions of low concentration (0.2-4microg/ml) were analysed. Rinsing experiments revealed loss of analyte due to adsorption to the vial surfaces as the main reason for this. The adsorption of Cetrorelix was found to follow a Langmuir isotherm reaching a plateau at 0.4microg/cm(2) and to be influenced by both the dissolution medium and the type of vial used. The adsorption tendency of Cetrorelix was reduced by: (a) a more lipophilic solvent (ethanol), (b) a more acidic pH (acetic acid) inducing repulsive charges (c) a micellar solution of various tensides. With all of these media the HPLC response was higher (up to five times) and less variable. Adsorption of Cetrorelix to solid surfaces decreased in the rank order: glass > polypropylene = polyethylene > poly-(tetrafluoroethylene), with considerable differences between the glass vials of various suppliers.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetic Acid / chemistry
  • Adsorption
  • Chromatography, High Pressure Liquid
  • Drug Packaging
  • Ethanol / chemistry
  • Glass / chemistry
  • Gonadotropin-Releasing Hormone / analogs & derivatives*
  • Gonadotropin-Releasing Hormone / antagonists & inhibitors*
  • Gonadotropin-Releasing Hormone / chemistry*
  • Hydrogen-Ion Concentration
  • Octoxynol / chemistry
  • Polypropylenes / chemistry
  • Polytetrafluoroethylene / chemistry
  • Solubility
  • Solvents / chemistry*
  • Surface Properties
  • Water / chemistry

Substances

  • Polypropylenes
  • Solvents
  • Water
  • Gonadotropin-Releasing Hormone
  • Ethanol
  • Polytetrafluoroethylene
  • Octoxynol
  • cetrorelix
  • Acetic Acid