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

Autor: J A, Simon, D E, Robinson, M C, Andrews, J R, Hildebrand, M L, Rocci, R E, Blake, G D, Hodgen
Rok vydání: 1993
Předmět:
Zdroj: Fertility and sterility. 60(1)
ISSN: 0015-0282
Popis: 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.Prospective, randomized, open label crossover protocol with 7 days between dosages.Academic institution.Fifteen normal postmenopausal women.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.Serum P concentrations were measured in all groups.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) (P0.05). 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.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.
Databáze: OpenAIRE