	US 12,274,787 B2
	Sustained-release injection comprising deslorelin, and preparation method therefor
Heeyong Lee, Daejeon (KR); Eunyoung Seol, Daejeon (KR); Yongha Na, Daejeon (KR); and Juhan Lee, Daejeon (KR)
Assigned to G2GBIO, INC., Daejeon (KR)
Appl. No. 17/312,061
Filed by G2GBIO, INC., Daejeon (KR)
PCT Filed Dec. 17, 2019, PCT No. PCT/KR2019/017905 § 371(c)(1), (2) Date Jun. 9, 2021, PCT Pub. No. WO2020/130585, PCT Pub. Date Jun. 25, 2020.
Claims priority of application No. 10-2018-0163416 (KR), filed on Dec. 17, 2018.
Prior Publication US 2022/0023217 A1, Jan. 27, 2022
Int. Cl. A61K 38/09 (2006.01); A61K 9/16 (2006.01)

CPC A61K 9/1647 (2013.01) [A61K 9/1682 (2013.01); A61K 38/09 (2013.01)]

3 Claims

1. A microsphere injection formulation comprising:

(i) sustained-release microspheres comprising 5 to 25% by weight of deslorelin acetate based on the total weight of the microspheres, and two polymers consisting of polylactide (PLA) and poly (lactide-co-glycolide) (PLGA), or

(ii) two or three types of sustained-release microspheres, wherein the two or three types of microspheres comprise 5 to 25% by weight of deslorelin acetate based on the total weight of the microspheres, and one or two polymers which are independently contained in the two or three types of the microspheres,

wherein the one polymer in (ii) is PLGA or PLA, and the two polymers in (ii) consist of PLGA and PLA;

wherein the PLA in (i) and (ii) is included in an amount of 50 to 90% by weight based on the total weight of the polymers;

and the PLGA in (i) and (ii) has a lactide: glycolide molar ratio of 50:50 to 75:25;

wherein an intrinsic viscosity of the PLA and PLGA in (i) and (ii) is 0.16-1.2 dL/g and 0.14-0.44 dL/g, respectively;

an average particle size of the microsphere in (i) or (ii) is 10 μm to 100 μm;

a span value of the microsphere in (i) or (ii) is 1.2 or less; and

the microsphere releases less than 10% of deslorelin acetate on day 1, 25-60% on day 28, and more than 85% on day 182 after administration.