Methods of treating hot flashes with formulations for...

A - Human Necessities – 61 – K

Patent

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A61K 9/06 (2006.01) A61K 31/565 (2006.01)

Patent

CA 2646667

The present invention relates to transdermal or transmucosal formulations, methods of use for preparing medicaments for treating hot flashes and methods for treatment thereof by administering such formulations for transdermal or transmucosal administration of estrogen. The formulations are effective at surprisingly low daily doses, preferably the lowest effective dose of estrogen to treat hot flashes, namely about 0.45 to about 0.6 mg of estrogen per day in a delivery vehicle that includes a C2 to C4 alkanol, a polyalcohol, and a permeation enhancer of monoalkyl ether of diethylene glycol. The amount of estrogen which is administered produces an estimated nominal daily estrogen dose in a subject undergoing treatment of from about 10 to about 15 micrograms, and a serum estradiol level of between about 25 pg/ml to about 50 pg/ml.

L'invention porte sur une préparation transderdermique ou transmucosique, sur ses méthodes d'utilisation pour préparer des médicamrnts de traitement des bouffées de chaleur, et sur les méthodes de traitement associées consistant à administrer lesdites préparations d'oestrogènes par voie transderdermique ou transmucosique. Lesdites préparations sont efficace à des doses quotidiennes surprennamant faibles, et de préférence à la dose efficace la plus basse, soit entre environ 0,45 et environ 0,60 mg d'oestrogène par jour, dans un véhicule comportant de l'alkanol C2 à C4, un polyalcool, un éther monoalkylique et un accélérateur de pénétration de l'éther monoalkyliqueé de diéthylène glycol. La quantité d'oestrogène administrée quotidiennement produit chez le sujet traité une quantité d'oestrogène d'environ 10 à environ 15 mg, et une concentration sérique d'estradiol comprise entre environ 25 et environ 50 pg/ml.

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