US 12,433,841 B2
Injectable controlled-release formulations of progestogen drugs
Zengli Fu, Kendall Park, NJ (US); Sydney Ugwu, North Brunswick, NJ (US); and James He, Green Brook, NJ (US)
Assigned to FORDOZ Pharma Corp., East Windsor, NJ (US)
Appl. No. 17/791,977
Filed by FORDOZ Pharma Corp., East Windsor, NJ (US)
PCT Filed Feb. 15, 2021, PCT No. PCT/US2021/018093
§ 371(c)(1), (2) Date Jul. 11, 2022,
PCT Pub. No. WO2021/173373, PCT Pub. Date Sep. 2, 2021.
Claims priority of provisional application 62/981,748, filed on Feb. 26, 2020.
Prior Publication US 2023/0057790 A1, Feb. 23, 2023
Int. Cl. A61K 9/16 (2006.01); A61K 9/00 (2006.01); A61K 31/57 (2006.01)
CPC A61K 9/1647 (2013.01) [A61K 9/0019 (2013.01); A61K 31/57 (2013.01)] 13 Claims
OG exemplary drawing
 
1. An injectable sustained-release formulation, comprising:
(a) microspheres comprising progesterone and a biodegradable composition comprising one or more poly(lactic-co-glycolic acid) copolymers (PLGA), and
(b) a diluent solution in which the microspheres are suspended wherein the one or more PLGA copolymers is a PLGA copolymer with a molar ratio of lactide to glycolide of about 50:50, about 75:25 or is a combination of PLGA copolymers with a molar ratio of lactide to glycolide of about 50:50 and 75:25 and a molecular weight in the range between 4 kD and 75 kD;
wherein the progesterone is present in an amount of between about 35% and about 50% by weight of the microspheres; and
the microspheres encapsulating the progesterone have a mean diameter of between about 50 μm and about 100 μm; and
wherein an in vitro release profile graph of the microspheres exhibits a linear correlation coefficient equal to or greater than 0.75 from a 0,0 time point to a 70% progesterone release point on the graph when the in vitro release profile is determined by placing approximately 20-25 mg of the microspheres in a container comprising about 200 mL of a release medium comprising a phosphate-buffered saline solution with 0.5% of sodium dodecyl sulfate, 0.02% sodium azide, and a pH of about 7.40 and placing the container with the microspheres and release medium in a 37° C. water bath shaking at a speed of about 90 RPM.