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


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.


Partition Coefficient Metoclopramide High Pressure Liquid Chromatography Metabolic Product Retention Data 
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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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