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Enhancement of oral moxidectin bioavailability in rabbits by lipid co-administration

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Abstract

Moxidectin is a member of the macrocyclic lactone family of drugs widely used for the control of internal and external parasites. Because moxidectin is highly lipophilic, we suspect that lymphatic transport influences the intestinal absorption of oral formulations of the drug. We studied the influence of lipid co-administration on the pharmacokinetics of an oral formulation of moxidectin in rabbits. Ten rabbits were orally administered 0.3 mg kg−1 moxidectin with or without sunflower oil. Moxidectin and triglyceride were analyzed in plasma over 23 days. Sunflower oil co-administration significantly increased the area under the plasma concentration–time curve of moxidectin (98%, P<0.05) and prolonged its mean residence time from 1.52 days to 2.12 days (P<0.04). Simultaneously, an increase in plasma triglyceride was observed in response to oil administration. It is suggested that lipid administration increases the systemic availability of oral moxidectin by enhancing the extent of intestinal lymphatic transport of the drug. Lipid-based formulations should improve the bioavailability of moxidectin in rabbits.

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Acknowledgements

We are grateful to Jean-François Sutra for technical advice. The experiments comply with the current laws of the country in which the experiment was performed.

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  1. Laboratoire de Pharmacologie–Toxicologie, INRA–Toulouse, B.P. 3, 31931 Cedex 9, Toulouse, France

    Mohamad Firas Bassissi, Anne Lespine & Michel Alvinerie

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  1. Mohamad Firas Bassissi
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  2. Anne Lespine
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  3. Michel Alvinerie
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Correspondence to Michel Alvinerie.

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Bassissi, M.F., Lespine, A. & Alvinerie, M. Enhancement of oral moxidectin bioavailability in rabbits by lipid co-administration. Parasitol Res 94, 188–192 (2004). https://doi.org/10.1007/s00436-004-1192-7

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  • DOI: https://doi.org/10.1007/s00436-004-1192-7

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