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Pharmaceutisch Weekblad

, Volume 2, Issue 1, pp 253–261 | Cite as

Physico-chemical aspects of metabolically induced changes at the basic centre of two anti-emetics; relationship with in vivo membrane penetration

  • G. Huizing
  • A. H. Beckett
Original Articles

Abstract

Partition coefficients in three solvent systems (1-octanol/ 0.1N NaOH,n-heptane/0.1N NaOH and toluene/0.1N NaOH), ionisation constants and thin-layer and reverse phase high pressure liquid chromatography retention data were determined for metoclopramide, its mono- and di-N-dealkylated metabolites, and for clebopride and its N-debenzylated metabolic product. Values for the additive-constitutive parameters π, ΔR m andx were calculated for the alkyl substituents at the basic centre of the two drugs, and the results are discussed.

The relationship between these physico-chemical parameters and thein vivo membrane penetrating capacity (this capacity was determined using buccal absorption measurements) is discussed.

Keywords

Partition Coefficient Metoclopramide High Pressure Liquid Chromatography Metabolic Product Retention Data 
These keywords were added by machine and not by the authors. This process is experimental and the keywords may be updated as the learning algorithm improves.

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Copyright information

© Bohn, Scheltema & Holkema 1980

Authors and Affiliations

  • G. Huizing
    • 1
  • A. H. Beckett
    • 1
  1. 1.Department of Pharmacy, Chelsea CollegeUniversity of LondonLondonUK

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