Low-dosed solid oral dosage forms for hrt

Abstract

The present invention relates to a very low-dosed dosage form for hormone replacement therapy (HRT). More particularly, the present invention concerns a solid oral dosage form comprising about 0.5 mg estradiol and about 0.25 mg drospirenone, and at least one pharmaceutically acceptable excipient. Despite the very low E2 and DRSP doses it has surprisingly been found that a high proportion of the women suffering from moderate to severe hot flushes actually respond to this treatment. Accordingly, the dosage form of the invention may be used as maintenance HRT or may be used already when HRT is initiated.

Description

FIELD OF THE INVENTION[0001]The present invention relates to a very low-dosed dosage form for hormone replacement therapy (HRT). More particularly, the present invention concerns a solid oral dosage form comprising about 0.5 mg estradiol (abbreviated “E2”) and about 0.25 mg drospirenone (abbreviated “DRSP”), and at least one pharmaceutically acceptable excipient. Despite the very low E2 and DRSP doses it has surprisingly been found that a high proportion of the women suffering from moderate to severe hot flushes actually respond to this treatment. Accordingly, the dosage form of the invention may be used as maintenance HRT or may be used already when HRT is initiated.BACKGROUND OF THE INVENTION[0002]Estrogens, and in particular E2, have been used for decades for treating estrogen deficiency symptoms, i.e. vasomotor symptoms. Hot flushes are the most common and bothersome clinical symptom of menopause, affecting approximately 75% of postmenopausal women (Sterns et al. Lancet 2002; 36...

AI Technical Summary

Benefits of technology

The present inventor has discovered that a low dose of E2 combined with a low dose of DRSP can provide effective relief of moderate to severe hot flushes in postmenopausal women. This low-dosagedosage form can be used as treatment or maintenance therapy and also improves bleeding behavior. The invention provides a solid oral dosage form for lowering the frequency of breakthrough bleedings or increasing the incidence rate of amenorrhea in women. The method involves administering the dosage form to women in need.

Problems solved by technology

Menopausal symptoms cause discomfort and distress, ranging from tolerable to, at times, severe enough to affect a woman's quality of life.

Also, the loss of endogenous estrogen during menopause accelerates the risk for chronic diseases, such as osteoporosis (Slemenda et al.

Conversely, a higher dose of 2 mg E2 is effective for symptom relief, but is associated with increased estrogen-related adverse events.