PROGESTERONE FORMULATIONS HAVING A DESIRABLE PK PROFILE
This disclosure provides progesterone formulations, methods of using these formulations, and their related pharmacokinetic parameters. In particular embodiments, the formulations disclosed herein allow for a reduction in the amount of progesterone administered to a patient in need thereof, while still providing the benefits of a larger dosage amount.
1 - 15 . (canceled)
16 . A pharmaceutical composition for administering progesterone to a subject in need thereof, the composition comprising estradiol and 100 mg of progesterone, wherein the progesterone is partially solubilized in a solvent system comprising i) fatty acid mono- and di-esters of polyethylene glycol; and ii) a solubilizing agent comprising predominantly medium chain mono- and di-glycerides of caprylic/capric fatty acids, wherein upon administration to the subject in need thereof, the composition produces at least one of the following pharmacokinetic parameters in said subject:
i) a progesterone AUC 0-t in (ng/ml)*hr of from about 5 to about 500;
ii) a progesterone AUC 0-∞ in (ng/ml)*hr of from about 5 to about 500; or
iii) a progesterone C max in ng/ml of from about 3 to about 350.
17 . The pharmaceutical composition of claim 16 , wherein the fatty acid mono- and di-esters of polyethylene glycol are lauroyl polyoxyl-32 glycerides.
18 . The pharmaceutical composition of claim 16 , wherein the fatty acid mono- and di-esters of polyethylene glycol and the solubilizing agent are present in approximately a 99:1 weight ratio.
19 . A method for the treatment of one or more symptoms of menopause comprising administering the pharmaceutical composition of claim 16 .
20 . The method of claim 19 , wherein the one more symptoms of menopause are selected from the group consisting of vasomotor symptoms, sleep disturbances, mood changes, vulvo-vaginal atrophy, osteoporosis, and endometrial hyperplasia reduction.
21 . The method of claim 19 , wherein the one more symptoms of menopause are vasomotor symptoms.
22 . The method of claim 21 wherein the vasomotor symptoms are hot flashes.
23 . The method of claim 21 , wherein the vasomotor symptoms are night sweats.