US 11,951,104 B2
Aripiprazole sustained-release microsphere and preparation method therefor
Bin Chen, Zhuhai (CN); Xia Yin, Zhuhai (CN); Yanqing Wang, Zhuhai (CN); Peng Xu, Zhuhai (CN); Yuda Yang, Zhuhai (CN); Miaoli Chen, Zhuhai (CN); Weilun Ye, Zhuhai (CN); Linyan Lv, Zhuhai (CN); Huijuan Xu, Zhuhai (CN); Wenqi Lu, Zhuhai (CN); Xiangsheng Kong, Zhuhai (CN); and Xiaoman Jiang, Zhuhai (CN)
Assigned to ZHUHAI LIVZON MICROSPHERE TECHNOLOGY CO. LTD., Guangdong (CN)
Appl. No. 17/055,540
Filed by LIVZON PHARMACEUTICAL GROUP INC, Zhuhai (CN)
PCT Filed Jun. 8, 2018, PCT No. PCT/CN2018/090345
§ 371(c)(1), (2) Date Nov. 13, 2020,
PCT Pub. No. WO2019/218409, PCT Pub. Date Nov. 21, 2019.
Claims priority of application No. 201810468934.6 (CN), filed on May 16, 2018.
Prior Publication US 2021/0196709 A1, Jul. 1, 2021
Int. Cl. A61K 31/496 (2006.01); A61K 9/00 (2006.01); A61K 9/16 (2006.01); A61K 47/26 (2006.01); A61K 47/34 (2017.01); A61K 47/38 (2006.01)
CPC A61K 31/496 (2013.01) [A61K 9/0019 (2013.01); A61K 9/1694 (2013.01); A61K 47/26 (2013.01); A61K 47/34 (2013.01); A61K 47/38 (2013.01)] 4 Claims
OG exemplary drawing
 
1. An aripiprazole sustained-release microsphere, comprising aripiprazole or salts thereof and poly(lactide-co-glycolide) copolymer; wherein,
the microsphere is in a spherical reticulate skeleton structure, small reticular holes are distributed in the sphere; and the aripiprazole or salts thereof are filled in the holes;
the microsphere has a mean particle size of less than 20 μm; the aripiprazole or salts thereof has a content of 71%-80% of a total weight of the microsphere;
wherein, the poly(lactide-co-glycolide) copolymer has an intrinsic viscosity of 0.2-0.55 dL/g; a polydispersity index of 1.0-3.0; and a weight-average molecular weight of 15000-60000; and
a molar ratio of lactide to glycolide in the poly(lactide-co-glycolide) copolymer is 50:50-65:35.