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The absorption of oral micronized progesterone: the effect of food, dose proportionality, and comparison with intramuscular progesterone

Simon JA et al., 1993

Fertility and sterility, 60(1), 26-33

DOI 10.1016/s0015-0282(16)56031-2 PMID 8513955 Source

Abstract

Objectives

To examine the effects of food ingestion and administered dose on the absorption of oral micronized P (Utrogestan; Besins-Iscovesco, Paris, France) and to compare the bioavailability of intramuscular versus oral routes of administration.

Design

Prospective, randomized, open label crossover protocol with 7 days between dosages.

Setting

Academic institution.

Participants

Fifteen normal postmenopausal women.

Interventions

All subjects participated in three separate protocols: [1] micronized P (200 mg) or placebo under fasting or nonfasting conditions once daily for 5 days; [2] micronized P (100, 200, or 300 mg) once daily under fasting conditions for 5 days; and [3] micronized P (200 mg) or intramuscular P (50 mg in oil) administered once daily for 2 days.

Main outcome measures

Serum P concentrations were measured in all groups.

Results

Concomitant food ingestion increased the area under the serum P concentration versus time curve (AUC0 to 24) and the maximum serum P concentration (Cmax) without affecting time to maximum serum concentration (Tmax) (P < 0.05). Micronized P absorption and elimination were first-order processes and exhibited dose-independent pharmacokinetics between 100 and 300 mg. After intramuscular P, Cmax was higher and Tmax occurred later compared with the oral P preparation. Oral P had lower relative bioavailability (8.6%) than intramuscular P.

Conclusions

Absorption of micronized P was enhanced twofold in the presence of food. Both absorption and elimination were dose-independent, dose proportionality being confirmed. Bioavailability of the oral P was approximately 10% compared with intramuscular P.

Topics

Reproductive Endocrinology > Progesterone > SupplementationReproductive Endocrinology > Luteal Phase > SupportRRM Methods > NaProTECHNOLOGY > Protocol
oral micronized progesterone absorption, progesterone bioavailability food effect, prometrium pharmacokinetics, oral versus intramuscular progesterone, progesterone supplementation timing, luteal phase support dosing, micronized progesterone dose proportionality, progesterone with food absorption, optimal progesterone administration, naprotechnology progesterone protocol, serum progesterone levels oral

Cite this article

Simon, J. A., Robinson, D. E., Andrews, M. C., Hildebrand JR 3rd, Rocci ML Jr, Blake, R. E., & Hodgen, G. D. (1993). The absorption of oral micronized progesterone: the effect of food, dose proportionality, and comparison with intramuscular progesterone. *Fertility and sterility*, *60*(1), 26-33. https://doi.org/10.1016/s0015-0282(16)56031-2

Keywords

Administration, Oral, Adult, Aged, Biological Availability, Drug Compounding, Eating, Fasting, Female, Half-Life, Humans, Injections, Intramuscular, Intestinal Absorption, Menopause, Middle Aged, Progesterone, Prospective Studies

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