title: Nasally-administered progesterone: comparison of ointment and spray formulations.
abstract: The aim of the study was to compare the bioavailability and clinical usefulness of progesterone (P) administered nasally in spray or ointment form. Twenty healthy post-menopausal women were randomly allocated to treatment by either intranasal spray (4 doses of an oil-based P solution at a concentration of 2 mg/0.1 ml, corresponding to a total dose of approximately 11 mg of P) or an ointment (quantity 0.1 ml, P concentration 20 mg/0.1 ml). Circulating P levels were calculated at various time intervals following administration. The spray formulation yielded a mean maximum concentration (CMax) of 3.75 ng/ml after 60 min (TMax) and the area under the curve (AUC) 0-720 min was 1481.6 +/- 343 ng.h/ml. The ointment yielded a mean CMax of 1.19 ng/ml at TMax = 30 min, the AUC 0-720 value being 404.35 +/- 148 ng.h/ml. The study findings confirmed that the intranasal route is a potentially useful alternative for the administration of natural sex steroid hormones, making it possible to avoid first-pass liver metabolism. P administered by spray showed greater bioavailability than it did when administered in ointment form, while both formulations seemed to be acceptable to patients and were probably clinically safe.
authors.affiliation: Department of Obstetrics and Gynaecology, University of Bari, Italy.
authors.forename: E
authors.initials: E
authors.lastname: Cicinelli
authors.forename: G
authors.initials: G
authors.lastname: Ragno
authors.forename: I
authors.initials: I
authors.lastname: Cagnazzo
authors.forename: F
authors.initials: F
authors.lastname: Fanelli
authors.forename: C
authors.initials: C
authors.lastname: Vetuschi
authors.forename: F P
authors.initials: FP
authors.lastname: Cantatore
mesh_terms: D000281:Administration, Intranasal; D000336:Aerosols; D001682:Biological Availability; D005260:Female; D006801:Humans; D008875:Middle Aged; D009824:Ointments; D011374:Progesterone / Q000008:administration & dosage* / Q000493:pharmacokinetics
chemical_list: D000336:Aerosols; D009824:Ointments; D011374:Progesterone