Influence of bile on the absorption of halofantrine from lipid-based formulations

Rene Holm; Henrik Tønsberg; Erling B. Jørgensen; Puyan Abedinpour; Shafiq Farsad; Anette Müllertz

doi:10.1016/j.ejpb.2012.03.005

Influence of bile on the absorption of halofantrine from lipid-based formulations

Rene Holm, Henrik Tønsberg, Erling B. Jørgensen, Puyan Abedinpour, Shafiq Farsad, Anette Müllertz

16 Citations (Scopus)

Abstract

The bioavailability of the poorly soluble model drug halofantrine, dosed in a soy bean oil solution or in a self-nanoemulsifying drug delivery system (SNEDDS), at two levels of lipid, was assessed in rats. Three rat models were used: intact rats, sham-operated rats and bile duct cannulated rats. The study showed no difference in the pharmacokinetic parameters between intact and sham-operated rats. T_max increased with lipid load for both oil solution and SNEDDS, whereas C_max and the absolute bioavailability were significantly higher for the SNEDDS at both lipid dosing levels. Bile duct cannulation of the rats reduced the C_max and the absolute bioavailability of halofantrine significantly, by a factor of 2, for all 4 treatments. These data clearly demonstrate that bile has an importance for the absorption of drugs from lipid-based formulations independent of the type.

Original language	English
Journal	European Journal of Pharmaceutics and Biopharmaceutics
Volume	81
Issue number	2
Pages (from-to)	281-287
ISSN	0939-6411
DOIs	https://doi.org/10.1016/j.ejpb.2012.03.005
Publication status	Published - Jun 2012

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title = "Influence of bile on the absorption of halofantrine from lipid-based formulations",

abstract = "The bioavailability of the poorly soluble model drug halofantrine, dosed in a soy bean oil solution or in a self-nanoemulsifying drug delivery system (SNEDDS), at two levels of lipid, was assessed in rats. Three rat models were used: intact rats, sham-operated rats and bile duct cannulated rats. The study showed no difference in the pharmacokinetic parameters between intact and sham-operated rats. Tmax increased with lipid load for both oil solution and SNEDDS, whereas Cmax and the absolute bioavailability were significantly higher for the SNEDDS at both lipid dosing levels. Bile duct cannulation of the rats reduced the Cmax and the absolute bioavailability of halofantrine significantly, by a factor of 2, for all 4 treatments. These data clearly demonstrate that bile has an importance for the absorption of drugs from lipid-based formulations independent of the type.",

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year = "2012",

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doi = "10.1016/j.ejpb.2012.03.005",

language = "English",

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T1 - Influence of bile on the absorption of halofantrine from lipid-based formulations

AU - Holm, Rene

AU - Tønsberg, Henrik

AU - Jørgensen, Erling B.

AU - Abedinpour, Puyan

AU - Farsad, Shafiq

AU - Müllertz, Anette

PY - 2012/6

Y1 - 2012/6

N2 - The bioavailability of the poorly soluble model drug halofantrine, dosed in a soy bean oil solution or in a self-nanoemulsifying drug delivery system (SNEDDS), at two levels of lipid, was assessed in rats. Three rat models were used: intact rats, sham-operated rats and bile duct cannulated rats. The study showed no difference in the pharmacokinetic parameters between intact and sham-operated rats. Tmax increased with lipid load for both oil solution and SNEDDS, whereas Cmax and the absolute bioavailability were significantly higher for the SNEDDS at both lipid dosing levels. Bile duct cannulation of the rats reduced the Cmax and the absolute bioavailability of halofantrine significantly, by a factor of 2, for all 4 treatments. These data clearly demonstrate that bile has an importance for the absorption of drugs from lipid-based formulations independent of the type.

AB - The bioavailability of the poorly soluble model drug halofantrine, dosed in a soy bean oil solution or in a self-nanoemulsifying drug delivery system (SNEDDS), at two levels of lipid, was assessed in rats. Three rat models were used: intact rats, sham-operated rats and bile duct cannulated rats. The study showed no difference in the pharmacokinetic parameters between intact and sham-operated rats. Tmax increased with lipid load for both oil solution and SNEDDS, whereas Cmax and the absolute bioavailability were significantly higher for the SNEDDS at both lipid dosing levels. Bile duct cannulation of the rats reduced the Cmax and the absolute bioavailability of halofantrine significantly, by a factor of 2, for all 4 treatments. These data clearly demonstrate that bile has an importance for the absorption of drugs from lipid-based formulations independent of the type.

U2 - 10.1016/j.ejpb.2012.03.005

DO - 10.1016/j.ejpb.2012.03.005

M3 - Journal article

C2 - 22465095

SN - 0939-6411

VL - 81

SP - 281

EP - 287

JO - European Journal of Pharmaceutics and Biopharmaceutics

JF - European Journal of Pharmaceutics and Biopharmaceutics

IS - 2

ER -

Influence of bile on the absorption of halofantrine from lipid-based formulations

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