US 11,717,555 B2
Pharmaceutical compositions having a selected release duration
Yuhua Li, Landenberg, PA (US); and Andrew Guarino, Newark, DE (US)
Assigned to Foresee Pharmaceuticals Co., Ltd., Taipei (TW)
Appl. No. 16/954,984
Filed by Foresee Pharmaceuticals Co., Ltd., Taipei (TW)
PCT Filed Dec. 18, 2017, PCT No. PCT/US2017/066968
§ 371(c)(1), (2) Date Jun. 17, 2020,
PCT Pub. No. WO2019/125358, PCT Pub. Date Jun. 27, 2019.
Prior Publication US 2020/0390849 A1, Dec. 17, 2020
Int. Cl. A61K 38/09 (2006.01); A61K 47/34 (2017.01); A61K 9/00 (2006.01); A61K 47/22 (2006.01)
CPC A61K 38/09 (2013.01) [A61K 9/0024 (2013.01); A61K 47/22 (2013.01); A61K 47/34 (2013.01)] 15 Claims
 
1. A pharmaceutical composition comprising:
a) a combination of a strong acid salt and a weak acid salt of a luteinizing hormone releasing hormone (LHRH) agonist wherein the molar ratio of (strong acid salt anion+weak acid salt anion) to the LHRH agonist is ≤2:1 and the molar ratio of the strong acid salt anion to the LHRH agonist is from 1:1 to less than 2:1;
b) a biodegradable polymer selected from the group consisting of a homopolymer polylatic acid (PLA), and a copolymer poly (lactic acid-co-glycolic acid) (PLGA), wherein the ratio of lactic acid:glycolic acid of the copolymer is from 50:50 to 100:0; and
c) N-methyl-2-pyrrolidone (NMP),
wherein:
the pharmaceutical composition has a selected release duration ranging from one month to 6 months, which correlates with ratios of the strong acid salt anion and the weak acid salt anion of the LHRH agonist;
the LHRH agonist is selected from the group consisting of leuprolide, triptorelin, and goserelin; and
the strong acid is methanesulfonic acid or hydrochloric acid, and the weak acid is acetic acid or formic acid.