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The effect of food and formulation on the population pharmacokinetics of cholesteryl ester transferase protein inhibitor DRL-17822 in healthy male volunteers.

ABSTRACT: We aimed to characterise the population pharmacokinetics of cholesteryl ester transferase protein inhibitor DRL-17822 in healthy males and explore the effect of food and formulation on the oral absorption of DRL-17822 in 4 phase I studies. DRL-17822 was dosed orally (2-1000 mg) in 2 different drug formulations (nanocrystal formulation and amorphous solid dispersion formulation) after either an overnight fast, or a low-fat, continental or high-fat breakfast. A 2-compartment model with 6 transit absorption compartments best characterised the data. Additionally, a strong interaction of food and formulation on bioavailability was observed and parsimoniously characterised in the model by binning combinations of food state and formulation with similar bio-availabilities. The final model adequately characterised the pharmacokinetic data of DRL-17822 in healthy males including the complex interaction of food and drug formulation. The amorphous solid dispersion formulation has a lower food effect on bioavailability compared with the nanocrystal formulation.

SUBMITTER: Goulooze SC

PROVIDER: S-EPMC7495284 | biostudies-literature | 2020 Oct

REPOSITORIES: biostudies-literature

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The effect of food and formulation on the population pharmacokinetics of cholesteryl ester transferase protein inhibitor DRL-17822 in healthy male volunteers.

Goulooze Sebastiaan C SC Kruithof Annelieke C AC Alikunju Shanavas S Gautam Anirudh A Burggraaf Jacobus J Kamerling Ingrid M C IMC Stevens Jasper J

British journal of clinical pharmacology 20200420 10

We aimed to characterise the population pharmacokinetics of cholesteryl ester transferase protein inhibitor DRL-17822 in healthy males and explore the effect of food and formulation on the oral absorption of DRL-17822 in 4 phase I studies. DRL-17822 was dosed orally (2-1000 mg) in 2 different drug formulations (nanocrystal formulation and amorphous solid dispersion formulation) after either an overnight fast, or a low-fat, continental or high-fat breakfast. A 2-compartment model with 6 transit a ...[more]

PMID: 32250455

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Dataset Information

The effect of food and formulation on the population pharmacokinetics of cholesteryl ester transferase protein inhibitor DRL-17822 in healthy male volunteers.

Publications

The effect of food and formulation on the population pharmacokinetics of cholesteryl ester transferase protein inhibitor DRL-17822 in healthy male volunteers.

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