US 11,969,434 B1
Oral allopregnanolone compositions and methods of use
Jonathan Ogle, Salt Lake City, UT (US); Benjamin J. Bruno, Salt Lake City, UT (US); Kongnara Papangkorn, Salt Lake City, UT (US); Samuel Akapo, Salt Lake City, UT (US); Joel Frank, Salt Lake City, UT (US); Nachiappan Chidambaram, Salt Lake City, UT (US); and Mahesh V. Patel, Salt Lake City, UT (US)
Filed by Lipocine Inc., Salt Lake City, UT (US)
Filed on Aug. 29, 2022, as Appl. No. 17/823,080.
Int. Cl. A61K 31/57 (2006.01); A61K 9/00 (2006.01); A61K 9/14 (2006.01); A61K 31/557 (2006.01); A61P 15/06 (2006.01); A61P 21/00 (2006.01)
CPC A61K 31/57 (2013.01) [A61K 9/0053 (2013.01); A61K 9/14 (2013.01); A61K 31/557 (2013.01); A61P 15/06 (2018.01); A61P 21/00 (2018.01)] 33 Claims
OG exemplary drawing
 
1. An oral pharmaceutical composition for use in treating a CNS disorder, said composition comprising at least about 3% w/w of allopregnanolone, at least about 7% w/w of a hydrophilic additive, and at least about 0.9% w/w of a lipophilic additive,
wherein said hydrophilic additive comprises at least one of polysorbate 80, polyoxyl 40 hydrogenated castor oil, sodium lauryl sulfate, sodium docusate, polyethylene glycol 1000 tocopherol succinate, PEG 400, and a poloxamer, and
wherein said lipophilic additive comprises at least one of glyceryl monocaprylate, glyceryl monocaprylocaprate, α-tocopherol, sterol, a sterol derivative, stearic acid, a glyceride of coconut oil, and a sorbitan fatty acid ester, and
wherein administration of said composition to a subject results in said subject at least one of:
a dose normalized minimum AUC0-24 of at least one of about 0.60 h/L, about 0.65 h/L, about 0.70 h/L, about 0.75 h/L, about 0.80 h/L, about 0.85 h/L, about 0.90 h/L, about 0.95 h/L, about 1.00 h/L, about 1.10 h/L, and about 1.20 h/L, and
a minimum AUC0-24 of at least one of about 18 ng*h/mL, about 19 ng*h/mL, and about 20 ng*h/mL.