US 12,290,523 B2
Formulation of long-acting levonorgestrel butanoate injectable depot suspension
Timothy J. McCormick, Wilmington, DE (US); Gustavo F. Doncel, Arlington, VA (US); Meredith Roberts Clark, Tuscaloosa, LA (US); and Jill Schwartz, Garrett Park, MD (US)
Assigned to Eastern Virginia Medical School, Norfolk, VA (US)
Appl. No. 16/079,811
Filed by Eastern Virginia Medical School, Norfolk, VA (US)
PCT Filed Feb. 23, 2017, PCT No. PCT/US2017/019092
§ 371(c)(1), (2) Date Aug. 24, 2018,
PCT Pub. No. WO2017/147274, PCT Pub. Date Aug. 31, 2017.
Claims priority of provisional application 62/299,257, filed on Aug. 24, 2018.
Prior Publication US 2019/0328749 A1, Oct. 31, 2019
Int. Cl. A61K 31/567 (2006.01); A61K 9/00 (2006.01); A61K 9/10 (2006.01); A61K 47/02 (2006.01); A61K 47/10 (2017.01); A61K 47/26 (2006.01); A61K 47/38 (2006.01)
CPC A61K 31/567 (2013.01) [A61K 9/0019 (2013.01); A61K 9/10 (2013.01); A61K 47/02 (2013.01); A61K 47/10 (2013.01); A61K 47/26 (2013.01); A61K 47/38 (2013.01)] 10 Claims
OG exemplary drawing
 
1. An injectable composition of Levonorgestrel Butanoate (LB),
wherein the composition is a sterile aqueous suspension comprising LB particles with a median (D50) particle size in the range of 13-50 μm,
wherein the composition comprises polysorbate 80 and sorbitan monopalmitate,
wherein polysorbate 80 is present in the composition at a concentration in the range of 0.05-2% w/v,
wherein sorbitan monopalmitate is present in the composition at a concentration in the range of 0.05-2% w/v,
wherein the composition shows a lack of particle size growth and aggregation over a two-year period when stored at 25° C. and 65% relative humidity, and
wherein the composition provides an extended duration of progestational action of at least 4 months.