High-strength testosterone undecanoate compositions

摘要

The present disclosure is drawn to pharmaceutical compositions and oral dosage capsules containing testosterone undecanoate, as well as related methods. The capsule includes a capsule shell and a capsule fill. The capsule fill can include a solubilizer and about 14 wt % to about 35 wt % testosterone undecanoate based on the total capsule fill. The oral dosage capsule is such that when a single oral administration to a male subject of one or more capsules with a total testosterone undecanoate daily dose of about 350 mg to about 650 mg it provides a ratio of serum testosterone Cmax to serum testosterone Cave of about 2.7 or less. In yet another embodiment, a method for providing a serum concentration of testosterone within a target serum testosterone concentration Cave range for a male subject is provided.

主权项

1. A method of treating a hypogonadal male, said method comprising:
administering a daily dose of 430-460 mg or 632 mg of testosterone undecanoate to the hypogonadal male for a period of time, measuring the hypogonadal male's serum testosterone level after said period of time to determine the maintenance regime daily dose, and administering a maintenance regime that provides a daily dose of testosterone undecanoate that is within ±40% of the initial daily dose administered to the hypogonadal male, wherein the testosterone undecanoate is in a pharmaceutical composition comprising (a) a fatty acid, C8 to C22 fatty acid glyceride, or a combination thereof and (b) a polyoxylated hydrogenated vegetable oil, and wherein said method when performed with a group of hypogonadal males provides a) a serum testosterone Cmax of less than 1500 ng/dL in at least 85% of the hypogonadal males in the group; b) a serum testosterone Cmax of about 1800 ng/dL to about 2500 ng/dL in 5% or less of the hypogonadal males in the group; or c) a serum testosterone Cmax greater than 2500 ng/dL in about 1% or less of the hypogonadal males in the group.