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ABSTRACT
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.
Key words: SEX HORMONES, TROCHE, BUCCAL DELIVERY, POSTMENOPAUSAL SYMPTOMS
INTRODUCTION
Hormone replacement therapy (HRT) for women has increased in popularity during the past 50 years. It is estimated that about 30% of Australian women over the age of 50 are now using hormones to relieve postmenopausal symptoms, or to reduce the risk of problems such as osteoporosis, genitourinary changes or neurological disorders1. However, some reassessment is likely in view of the recently published Women's Health Initiative study2.
A number of HRT regimens have been devised for the management of symptoms of the postmenopause, with variable success. Most treatments have been based on the use of natural 17beta-estradiol, conjugated equine estrogen or other conjugated estrogens, in combination with a group of synthesized progestogens such as norethisterone, levonorgestrel, medroxyprogesterone acetate and dydrogesterone. While these combination regimens have been successful in controlling symptoms, a number of side-effects or complications may occur, which have variously been attributed to the type or dose of estrogen used, or to the type or dose of synthetic progestogen administered. Some physicians have noted that progestogens are often associated with an increased rate of mastalgia, bloating, weight gain, irritability, mood...