Examination of some factors responsible for a food‐induced increase in absorption of atovaquone.
Open accessAbstract
1. Atovaquone is a potent antiprotozoal slowly and irregularly absorbed after administration as tablets to fasting volunteers. A series of studies was performed to investigate the effects of food, bile and formulation on atovaquone absorption. 2. In 18 healthy male volunteers, a high‐fat breakfast administered 45 min before 500 mg atovaquone as tablets increased AUC by 3.3‐fold (95% CI 2.8‐4.0) and Cmax 5.3‐fold (4.3‐6.6) compared with fasting. 3. The absorption of atovaquone from tablets was examined in 12 healthy male volunteers after an overnight fast, following toast alone, toast with 28 g butter (LOFAT), or toast with 56 g butter (HIFAT). Compared with absorption when fasted, toast had no significant effect but LOFAT increased AUC 3.0‐fold (2.1‐4.2) and Cmax 3.9‐fold (2.6‐5.8). HIFAT increased AUC 3.9‐fold (2.7‐5.5) and Cmax 5.6‐fold (3.8‐8.4). 4. The absorption of atovaquone was examined in nine healthy fasting male volunteers from tablets, an aqueous suspension, and an oily solution/suspension in miglyol (fractionated coconut oil). Compared with tablets, AUC following the aqueous suspension was increased 1.7‐fold (1.0‐2.7) and Cmax 2.4‐fold (1.7‐ 3.5). Following miglyol, AUC was increased to the same extent but Cmax was only increased 1.8‐fold (1.2‐2.6). 5. Atovaquone absorption was examined in eight healthy fasting male volunteers following an i.v. infusion of cholecystokinin octapeptide (CCK‐OP) which decreased gallbladder volume by 82% (73%‐90%) on occasion 1 or saline on occasion 2. AUC(0,12) was increased following CCK‐OP by 1.6‐fold (1.1‐2.4) and Cmax by 1.5‐fold (0.98‐2.4).(ABSTRACT TRUNCATED AT 250 WORDS)
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It is likely that the effect of food on improving absorption for compounds with low aqueous solubility is related to the amount of fat in the meal.
“it is likely that the effect of food on improving absorption for compounds with low aqueous solubility is related to the amount of fat in the meal.”
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Cites
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Self-citation
- Authors
- Rolan, P., Mercer, A., Weatherley, B., Holdich, T., Meire, H., Peck, R., Ridout, G., & Posner, J.
- Affiliations
- Wellcome Trust (GB)
- ORCID
- Posner, J
- Venue
- British Journal of Clinical Pharmacology
- Publisher
- Wiley
- Published
- 1994-01
- Volume
- 37
- Issue
- 1
- Pages
- 13-20
- ISSN
- 0306-5251 (ISSN-L)
- 1365-2125
- PMC
- PMC1364703
- OpenAlex
- W1996353358
- Cited by
- 123
- References
- 21
- Citations by year
- 2026: 3 · 2025: 1 · 2024: 2 · 2023: 3 · 2022: 2 · 2021: 1 · 2020: 2 · 2019: 2 · 2018: 4 · 2017: 3 · 2016: 3 · 2015: 3 · 2014: 4 · 2013: 3 · 2012: 3
- FWCI
- 6.26
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- British Journal of Clinical Pharmacology (publishedVersion)
- PubMed Central (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Drug Solubulity and Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmacology › Pharmacogenetics and Drug Metabolism
- Health Sciences › Medicine › Pediatrics, Perinatology and Child Health › Pharmaceutical studies and practices
- Keywords
- atovaquone, drug absorption, food effect, high-fat meal, tablet formulation, Miglyol, aqueous suspensions, cholecystokinin octapeptide, bile, antiprotozoal agents, bioavailability
- MeSH terms
- Adult, Chromatography, High Pressure Liquid, Dietary Fats, Fasting, Food, Humans, Infusions, Intravenous, Intestinal Absorption, Male, Middle Aged, Naphthoquinones, Sincalide, Suspensions, Tablets, Atovaquone
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