17-hydroxyprogesterone ester containing oral compositions and related methods

摘要

The present invention provides for bioavailable oral dosage forms containing esters of 17-hydroxyprogesterone as well as related methods. The oral dosage forms can be formulated for pregnancy support and can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. In another embodiment, a pharmaceutically acceptable oral dosage form for pregnancy support is provided. The pharmaceutically acceptable oral dosage can include a therapeutically effective amount of an ester of 17-hydroxyprogesterone and a pharmaceutically acceptable carrier. The oral dosage form can, when measured using a USP Type-II dissolution apparatus in 900 mL of deionized water with 0.5 (w/v) of sodium lauryl sulfate at 50 RPM at 37° C., release at least 20 wt % of the dose of the ester of 17-hydroxyprogesterone after 60 minutes, or in the alternative release at least 20 wt % more after 60 minutes than an equivalently dosed oral dosage form without the carrier.

主权项

1. A method of treating a pregnant female subject at risk of preterm birth, said method comprising administering to the female subject a tablet or capsule oral pharmaceutical composition comprising: a therapeutically effective amount of 17-hydroxyprogesterone caproate with a mean particle diameter size of 50 micron or less and a pharmaceutically acceptable carrier
wherein (a) said pharmaceutically acceptable carrier includes (i) a poloxamer, a polyethylene glycol sorbitan fatty acid ester, a sorbitan fatty acid ester, a polyethylene glycol glycerol fatty acid ester, sodium lauryl sulfate, sodium dioctyl sulfosuccinate, a lecithin, a bile salt or a combination thereof; or (ii) a lipophilic additive and (b) said pharmaceutical composition, when measured using a USP Type-II dissolution apparatus in 900 mL of simulated intestinal fluid having 0.5% (w/v) of sodium lauryl sulfate at 50 RPM at 37° C., releases at least 20 wt % of the 17-hydroxyprogesterone caproate at 60 minutes.