Pharmacokinetics of estradiol, progesterone, testosterone and dehydroepiandrosterone after transbuccal administration to postmenopausal women.

OBJECTIVE

To evaluate the pharmacokinetic profiles of estradiol, progesterone, testosterone and dehydroepiandrosterone in postmenopausal women following single and multiple dosing using a troche and the transbuccal route of administration.

METHODS

Each troche contained estradiol (0.5 mg), progesterone (200 mg), testosterone (2.0 mg) and dehydroepiandrosterone (10 mg). A half troche was administered to each of six women and the plasma concentration-time profiles determined over 24 h. Thereafter, a one-half troche was taken twice daily for 2 weeks and concentrations determined over a dosage interval (12 h). Blood and saliva samples were collected at specified time intervals on the first day and again after 2 weeks.

RESULTS

Each of the hormones was readily absorbed via the buccal mucous membrane. Peak plasma concentrations of estradiol and progesterone were comparable to those found normally in young menstruating women.

CONCLUSION

The transbuccal route is a novel approach to provide therapy for the management of menopause-related symptoms of postmenopausal women without the need to resort to conjugated or synthesized hormones, and may overcome the poor or erratic systemic availability associated with other routes of administration.