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 - 42 . (canceled)
43 . A pharmaceutical composition for oral administration comprising (a) 14-35% loading of 120 to 300 mg testosterone undecanoate and (b) a fatty acid, C8 to C22 fatty acid glyceride, or combination thereof.
44 . The pharmaceutical composition of claim 1 further comprising a polyoxyethylene hydrogenated vegetable oil.
45 . The pharmaceutical composition of claim 1 comprising a solidifying agent.
46 . The pharmaceutical composition of claim 1 wherein at least 40 wt % of the testosterone undecanoate is released in the first 30 minutes, when measured using about 1000 mL of 8% w/v Triton X-100 in water maintained at about 37±1° C. in a USP-Type II dissolution apparatus set at 100 rpm.
47 . The pharmaceutical composition of claim 1 that provides a serum total testosterone Cavg ranging about 400 ng/dL to about 600 ng/dL when administered as one or two unit dosage forms twice daily.
48 . The pharmaceutical composition of claim 1 comprising 158 mg testosterone undecanoate.
49 . The pharmaceutical composition of claim 1 comprising 225 mg testosterone undecanoate.
50 . The pharmaceutical composition of claim 1 wherein the fatty acid, C8 to C22 fatty acid glyceride, or combination thereof comprises from about 50% to about 86% of the pharmaceutical composition.
51 . The pharmaceutical composition of claim 1 wherein said C8 to C22 fatty acid glyceride is a glyceride of capric acid, caprylic acid, undecanoic acid, lauric acid, myristic acid, palmitic acid, stearic acid, oleic acid, linoleic acid, linolenic acid or mixtures thereof.
52 . A pharmaceutical composition comprising (a) 14-35% loading of 225 mg testosterone undecanoate and (b) a fatty acid, C8 to C22 fatty acid glyceride, or combination thereof.
53 . The pharmaceutical composition of claim 1 further comprising a polyoxylated hydrogenated vegetable oil.
54 . The pharmaceutical composition of claim 1 comprising a solidifying agent.
55 . The pharmaceutical composition of claim 1 wherein at least 40 Wt % of the testosterone undecanoate is released in the first 30 minutes, when measured using about 1000 mL of 8% w/v Triton X-100 in water maintained at about 37±1° C. in a USP-Type II dissolution apparatus set at 100 rpm.
56 . The pharmaceutical composition of claim 1 that provides a serum total testosterone Cavg ranging about 400 ng/dL to about 600 ng/dL when administered as one or two unit dosage forms twice daily.
57 . The pharmaceutical composition of claim 52 wherein the fatty acid, C8 to C22 fatty acid glyceride, or combination thereof comprises from about 50% to about 86% of the pharmaceutical composition.
58 . A pharmaceutical composition comprising (a) 15-30% loading of 150 mg to 250 mg testosterone undecanoate and (b) a fatty acid, C8 to C22 fatty acid glyceride, or combination thereof.
59 . The pharmaceutical composition of claim 57 further comprising a polyoxylated hydrogenated vegetable oil.
60 . The pharmaceutical composition of claim 57 comprising a solidifying agent.
61 . The pharmaceutical composition of claim 57 wherein at least 40 wt % of the testosterone undecanoate is released in the first 30 minutes, when measured using about 1000 mL of 8% w/v Triton X-100 in water maintained at about 37±1° C. in a USP-Type II dissolution apparatus set at 100 rpm.
62 . The pharmaceutical composition of claim 57 that provides a serum total testosterone mean Cavg ranging about 400 ng/dL to about 600 ng/dL when administered as one or two unit dosage forms twice daily to a population of hypogonadal males.