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Food effect on the bioavailability of two distinct formulations of megestrol acetate oral suspension.

Deschamps B, Musaji N, Gillespie JA - Int J Nanomedicine (2009)

Bottom Line: In fasting subjects, the area under the curve was 12,095 ng.h/mL for MA-ES, and 8,942 ng.h/mL for MAOS.In fed subjects, the absorption of the two formulations was comparable.Bioavailability and absorption are greater for MA-ES than MAOS in fasting subjects.

View Article: PubMed Central - PubMed

Affiliation: SFBC Anapharm, Montreal, Canada.

ABSTRACT

Objective: Megestrol acetate oral suspension (MAOS) is an appetite stimulant indicated for cachexia in patients with AIDS. It is available in its original formulation, Megace (MAOS), and as a nanocrystal dispersion, Megace ES (MA-ES). Three studies were conducted to evaluate the pharmacokinetic properties of these formulations under fed and fasting conditions.

Methods: An open-label, crossover trial was conducted in 24 healthy males randomized to MA-ES 625 mg/5 mL given with a high-calorie, high-fat meal, or after an overnight fast. Blood samples were drawn at multiple time points and pharmacokinetic parameters were determined. Two separate, open-label reference studies evaluated MAOS 800 mg/20 mL in 40 fed or 40 fasting healthy male volunteers.

Results: In fasting MA-ES subjects, the average maximum concentration (C(max)) was 30% less than the fed C(max) value. For MAOS, fasting C(max) was 86% less than fed C(max). In fasting subjects, the area under the curve was 12,095 ng.h/mL for MA-ES, and 8,942 ng.h/mL for MAOS. In fed subjects, the absorption of the two formulations was comparable.

Conclusion: Bioavailability and absorption are greater for MA-ES than MAOS in fasting subjects. MA-ES may be a preferred formulation of megestrol acetate when managing cachectic patients whose caloric intake is reduced.

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Related in: MedlinePlus

Food effect differences between a nanocrystal dispersion of megestrol acetate (MA-ES) 625 mg/5 mL and a micronized formulation of megestrol acetate oral suspension (MAOS) 800 mg/20 mL.a800 to 1000 calories, ∼50% fat.bData in fed subjects from Study 1, MA-ES (N = 23), and Study 2, MAOS (N = 32).cData in fasting subjects from Study 1, MA-ES (N = 23), and Study 3, MAOS (N = 36).
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f4-ijn-4-185: Food effect differences between a nanocrystal dispersion of megestrol acetate (MA-ES) 625 mg/5 mL and a micronized formulation of megestrol acetate oral suspension (MAOS) 800 mg/20 mL.a800 to 1000 calories, ∼50% fat.bData in fed subjects from Study 1, MA-ES (N = 23), and Study 2, MAOS (N = 32).cData in fasting subjects from Study 1, MA-ES (N = 23), and Study 3, MAOS (N = 36).

Mentions: As shown in Figure 4, single doses of MA-ES 625 mg/5 mL and MAOS 800 mg/20 mL have comparable bioavailability under fed conditions, but under fasting conditions the bioavailability of MA-ES is greater than that of MAOS.


Food effect on the bioavailability of two distinct formulations of megestrol acetate oral suspension.

Deschamps B, Musaji N, Gillespie JA - Int J Nanomedicine (2009)

Food effect differences between a nanocrystal dispersion of megestrol acetate (MA-ES) 625 mg/5 mL and a micronized formulation of megestrol acetate oral suspension (MAOS) 800 mg/20 mL.a800 to 1000 calories, ∼50% fat.bData in fed subjects from Study 1, MA-ES (N = 23), and Study 2, MAOS (N = 32).cData in fasting subjects from Study 1, MA-ES (N = 23), and Study 3, MAOS (N = 36).
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Related In: Results  -  Collection

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getmorefigures.php?uid=PMC2747353&req=5

f4-ijn-4-185: Food effect differences between a nanocrystal dispersion of megestrol acetate (MA-ES) 625 mg/5 mL and a micronized formulation of megestrol acetate oral suspension (MAOS) 800 mg/20 mL.a800 to 1000 calories, ∼50% fat.bData in fed subjects from Study 1, MA-ES (N = 23), and Study 2, MAOS (N = 32).cData in fasting subjects from Study 1, MA-ES (N = 23), and Study 3, MAOS (N = 36).
Mentions: As shown in Figure 4, single doses of MA-ES 625 mg/5 mL and MAOS 800 mg/20 mL have comparable bioavailability under fed conditions, but under fasting conditions the bioavailability of MA-ES is greater than that of MAOS.

Bottom Line: In fasting subjects, the area under the curve was 12,095 ng.h/mL for MA-ES, and 8,942 ng.h/mL for MAOS.In fed subjects, the absorption of the two formulations was comparable.Bioavailability and absorption are greater for MA-ES than MAOS in fasting subjects.

View Article: PubMed Central - PubMed

Affiliation: SFBC Anapharm, Montreal, Canada.

ABSTRACT

Objective: Megestrol acetate oral suspension (MAOS) is an appetite stimulant indicated for cachexia in patients with AIDS. It is available in its original formulation, Megace (MAOS), and as a nanocrystal dispersion, Megace ES (MA-ES). Three studies were conducted to evaluate the pharmacokinetic properties of these formulations under fed and fasting conditions.

Methods: An open-label, crossover trial was conducted in 24 healthy males randomized to MA-ES 625 mg/5 mL given with a high-calorie, high-fat meal, or after an overnight fast. Blood samples were drawn at multiple time points and pharmacokinetic parameters were determined. Two separate, open-label reference studies evaluated MAOS 800 mg/20 mL in 40 fed or 40 fasting healthy male volunteers.

Results: In fasting MA-ES subjects, the average maximum concentration (C(max)) was 30% less than the fed C(max) value. For MAOS, fasting C(max) was 86% less than fed C(max). In fasting subjects, the area under the curve was 12,095 ng.h/mL for MA-ES, and 8,942 ng.h/mL for MAOS. In fed subjects, the absorption of the two formulations was comparable.

Conclusion: Bioavailability and absorption are greater for MA-ES than MAOS in fasting subjects. MA-ES may be a preferred formulation of megestrol acetate when managing cachectic patients whose caloric intake is reduced.

Show MeSH
Related in: MedlinePlus