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Titolo:
EXAMINATION OF SOME FACTORS RESPONSIBLE FOR A FOOD-INDUCED INCREASE IN ABSORPTION OF ATOVAQUONE
Autore:
ROLAN PE; MERCER AJ; WEATHERLEY BC; HOLDICH T; MEIRE H; PECK RW; RIDOUT G; POSNER J;
Indirizzi:
WELLCOME RES LABS,LANGLEY COURT BECKENHAM BR3 3BS KENT ENGLAND UNIV LONDON KINGS COLL HOSP,DEPT RADIOL LONDON SE5 9RS ENGLAND
Titolo Testata:
British journal of clinical pharmacology
fascicolo: 1, volume: 37, anno: 1994,
pagine: 13 - 20
SICI:
0306-5251(1994)37:1<13:EOSFRF>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
566C80; HYDROXYNAPHTHOQUINONE; PHARMACOKINETICS; GRISEOFULVIN;
Keywords:
ATOVAQUONE; 566C80; ABSORPTION; MIGLYOL; CHOLECYSTOKININ; FOOD;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
23
Recensione:
Indirizzi per estratti:
Citazione:
P.E. Rolan et al., "EXAMINATION OF SOME FACTORS RESPONSIBLE FOR A FOOD-INDUCED INCREASE IN ABSORPTION OF ATOVAQUONE", British journal of clinical pharmacology, 37(1), 1994, pp. 13-20

Abstract

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 C(max) 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 with56 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 C(max) 3.9-fold (2.6-5.8). HIFAT increased AUC 3.9-fold (2.7-5.5) and C(max) 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 C(max) 2.4-fold (1.7-3.5). Following miglyol, AUC was increased to the same extent but C(max) 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 by82% (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 C(max) by 1.5-fold (0.98-2.4). However, total AUC was not significantly increased (mean ratio 1.2, 95% CI 0.85-1.8). 6 In four healthy male volunteers who received 750 mg atovaquone containing 100 muCi [C-14]-atovaquone as a suspension following a high-fat meal, no drug was detected in chylomicronsseparated from plasma. 7 The substantial increase in absorption of atovaquone from tablets after a fatty meal can be accounted for quantitatively by the fat content of the meal. Absorption from suspensions in water and miglyol was superior to that from tablets but both were inferior to the tablets following a high fat meal. Bile release may make some contribution to the food effect. Food probably increases atovaquone absorption by increasing its solubility in the gut lumen.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 30/11/20 alle ore 00:35:43