The effect of drug lipophilicity and lipid vehicles on the lymphatic absorption of various testosterone esters

T. Noguchi, W. N.A. Charman, V. J. Stella

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Abstract

Mesenteric lymph was collected from non-restrained unanesthetized rats following oral administration of several different testosterone esters dissolved in various non-polar lipid vehicles. A good correlation was observed between the differing amounts of the testosterone esters appearing in intestinal lymph (24 h post-dosing) and their respective n-heptane/water partition coefficients. There appeared to be a significant vehicle effect on lymphatic absorption when monitoring the lymphatic transport of testosterone undecanoate after its oral administration in various lipid vehicles. Lymphatic absorption of testosterone undecanoate was greatest when administered in oleic acid (C18:1) and long-chain unsaturated triglyceride vehicles. However, mixtures of oleic acid-monoolein (representing a synthetic digestion mixture of a triglyceride) failed to improve, and in fact decreased, the lymphatic absorption of testosterone undecanoate relative to an oleic acid vehicle. Although the extent of lymphatic absorption of testosterone undecanoate was very small, it did appear to be the major determinant of the bioavailability of orally administered testosterone undecanoate.

Original languageEnglish
Pages (from-to)173-184
Number of pages12
JournalInternational Journal of Pharmaceutics
Volume24
Issue number2-3
DOIs
Publication statusPublished - 1 Jan 1985
Externally publishedYes

Keywords

  • lipophilicity
  • lymphatic absorption
  • testosterone esters
  • vehicle effect

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