HIGH-STRENGTH TESTOSTERONE UNDECANOATE COMPOSITIONS
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 C max to serum testosterone C ave 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 C ave range for a male subject is provided.
1 . A method for replacement therapy in a male having a condition associated with a deficiency or absence of endogenous testosterone said method comprising:
orally administering to said male a daily dosing regimen of a pharmaceutical composition comprising about 14 weight % (wt %) to about 35 wt % testosterone undecanoate and a carrier, that provides from about 450 mg to 480 mg of testosterone undecanoate to said male per day to provide a serum testosterone C ave in said male in the range of from about 300-1100 ng/dL.
2 . The method of claim 1 , wherein said carrier comprises a solubilizer and a dispersant.
3 . The method of claim 1 , wherein said carrier comprises a solidifying agent.
4 . The method of claim 1 , wherein said carrier comprises a monoglyceride.
5 . The method of claim 1 , wherein said carrier comprises a diglyceride.
6 . The method of claim 1 , wherein said carrier comprises a triglyceride.
7 . The method of claim 1 , wherein said carrier comprises a fatty acid.
8 . The method of claim 1 , wherein said carrier comprises medium chain monoglycerides and diglycerides.
9 . The method of claim 1 , wherein said carrier comprises a tocopherol.
10 . The method of claim 1 , wherein said carrier comprises a hydrophilic surfactant.
11 . The method of claim 1 , wherein said orally administering is twice-a-day.
12 . The method of claim 1 , wherein said pharmaceutical composition is disposed of in a capsule.
13 . The method of claim 1 , wherein said daily dosing regimen provides about 480 mg of testosterone undecanoate per day.
14 . The method of claim 1 , wherein said pharmaceutical composition has at least 5% of the testosterone undecanoate not dissolved and at least 35% dissolved in said carrier.
15 . A method for replacement therapy in a male having a condition associated with a deficiency or absence of endogenous testosterone said method comprising:
orally administering to said male a daily dosing regimen of a pharmaceutical composition comprising testosterone undecanoate and a carrier, said composition comprising from 50-86 weight % (wt %) solubilizer, that provides about 450 mg to 480 mg of testosterone undecanoate to said male per day to provide a serum testosterone Cave in said male in the range of from about 300-1100 ng/dL.
16 . The method of claim 15 , wherein said pharmaceutical composition is disposed of in a capsule.
17 . The method of claim 15 , wherein said orally administering is twice-a-day.
18 . The method of claim 15 , wherein said carrier has one or more of the following: a fatty acid, a monoglyceride, a diglyceride, a triglyceride, and a tocopherol.
19 . The method of claim 15 , wherein said carrier has a hydrophilic surfactant.
20 . The method of claim 15 , wherein said carrier has a solidifying agent.
21 . The method of claim 15 , wherein said about 480 mg of testosterone undecanoate is provided as two unit dosage forms in the morning and two unit dosage forms in the evening.
22 . The method of claim 17 , wherein said daily dosing regimen provides about 480 mg of testosterone undecanoate per day.
23 . A method for replacement therapy in a male having a condition associated with a deficiency or absence of endogenous testosterone said method comprising:
orally administering to said male twice-a-day with a meal two unit dosage forms of a pharmaceutical composition comprising testosterone undecanoate and a carrier, that provides about 450 mg to 480 mg of testosterone undecanoate to said male per day to provide a serum testosterone Cave in said male in the range of from about 300-1100 ng/dL.
24 . The method of claim 23 , wherein said pharmaceutical composition is disposed of in capsule.
25 . The method of claim 23 , wherein said daily dosing regimen provides about 480 mg of testosterone undecanoate per day.
26 . The method of claim 25 , wherein said carrier comprising a solubilizer.
27 . The method of claim 25 , wherein said carrier comprising a dispersant.