US 12,377,049 B2
Fulvestrant pharmaceutical composition, preparation method therefor, and application thereof
Shuhuan Ying, Shanghai (CN); Hong Li, Shanghai (CN); Zhixiang Chen, Shanghai (CN); and Tingting Wang, Shanghai (CN)
Assigned to SHANGHAI BOCIMED PHARMACEUTICAL CO., LTD., Shanghai (CN)
Appl. No. 17/757,245
Filed by SHANGHAI BOCIMED PHARMACEUTICAL CO., LTD., Shanghai (CN)
PCT Filed Dec. 10, 2020, PCT No. PCT/CN2020/135311
§ 371(c)(1), (2) Date Jun. 13, 2022,
PCT Pub. No. WO2021/115389, PCT Pub. Date Jun. 17, 2021.
Claims priority of application No. 201911262544.4 (CN), filed on Dec. 11, 2019; and application No. 202010590154.6 (CN), filed on Jun. 24, 2020.
Prior Publication US 2022/0370359 A1, Nov. 24, 2022
Int. Cl. A61K 9/16 (2006.01); A61K 9/00 (2006.01); A61K 31/355 (2006.01); A61K 31/375 (2006.01); A61K 47/26 (2006.01); A61K 47/44 (2017.01); A61K 47/54 (2017.01)
CPC A61K 9/1641 (2013.01) [A61K 9/0019 (2013.01); A61K 31/355 (2013.01); A61K 31/375 (2013.01); A61K 47/26 (2013.01); A61K 47/44 (2013.01); A61K 47/547 (2017.08)] 10 Claims
 
1. A fulvestrant pharmaceutical composition comprising fulvestrant solid particles, a suspending agent, a wetting agent, an osmotic pressure regulator, a buffer, and a pH adjusting agent, wherein:
the fulvestrant solid particles have a particle size distribution having Dv(10) ranging from 0.600-2.000 μm, Dv(25) ranging from 1.000-3.000 μm, Dv(50) ranging from 0.800-4.000 μm, Dv(75) ranging from 1.000-4.000 μm, and Dv(90) ranging from 1.000-6.000 μm, provided that Dv(90) is not 1.000 μm, the particle size being determined using a laser particle analyzer with a dispersion medium: water, the refractive index of the dispersion medium: 1.333, the absorbance of the sample material: 0.01, and the refractive index of the sample material: 1.521;
the fulvestrant solid particles have a weight fraction of 10.00%-40.00%;
the suspending agent has a weight fraction of 0.20%-3.00% and is one or more selected from sodium carboxymethylcellulose, polyethylene glycol, and povidone;
the wetting agent has a weight fraction of 1.00%-3.00% and is one or more selected from poloxamer and tween; and
the osmotic pressure regulator has a weight fraction of 1.00%-3.00% and is one or more selected from sodium chloride, mannitol, and sucrose.