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 Citationer (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.

Originalsprog	Engelsk
Tidsskrift	European Journal of Pharmaceutics and Biopharmaceutics
Vol/bind	81
Udgave nummer	2
Sider (fra-til)	281-287
ISSN	0939-6411
DOI	https://doi.org/10.1016/j.ejpb.2012.03.005
Status	Udgivet - jun. 2012

Adgang til dokumentet

10.1016/j.ejpb.2012.03.005

Citationsformater

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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.",

author = "Rene Holm and Henrik T{\o}nsberg and J{\o}rgensen, {Erling B.} and Puyan Abedinpour and Shafiq Farsad and Anette M{\"u}llertz",

year = "2012",

month = jun,

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

language = "English",

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pages = "281--287",

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TY - JOUR

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

Abstract

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