(19)
(11) EP 3 607 940 A8

(12) CORRECTED EUROPEAN PATENT APPLICATION
published in accordance with Art. 153(4) EPC

(15) Correction information:
Corrected version no 1 (W1 A1)

(48) Corrigendum issued on:
01.04.2020 Bulletin 2020/14

(43) Date of publication:
12.02.2020 Bulletin 2020/07

(21) Application number: 18917042.6

(22) Date of filing: 08.06.2018
(51) International Patent Classification (IPC): 
A61K 9/50(2006.01)
A61K 47/34(2017.01)
A61P 25/18(2006.01)
 A61K 31/496(2006.01)
A61K 9/10(2006.01)
(86) International application number:
PCT/CN2018/090345
(87) International publication number:
WO 2019/218409 (21.11.2019 Gazette 2019/47)
(84) Designated Contracting States:
AL AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO RS SE SI SK SM TR
Designated Extension States:
BA ME
Designated Validation States:
KH MA MD TN

(30) Priority: 16.05.2018 CN 201810468934

(71) Applicant: Livzon Pharmaceutical Group Inc.
Zhuhai, Guangdong 519020 (CN)

(72) Inventors:
  • LU, Wenqi
    Zhuhai City Guangdong 519090 (CN)
  • CHEN, Bin
    Zhuhai City Guangdong 519090 (CN)
  • KONG, Xiangsheng
    Zhuhai City Guangdong 519090 (CN)
  • XU, Peng
    Zhuhai City Guangdong 519090 (CN)
  • WANG, Yanqing
    Zhuhai City Guangdong 519090 (CN)
  • REN, Bing
    Zhuhai City Guangdong 519090 (CN)
  • CHEN, Miaoli
    Zhuhai City Guangdong 519090 (CN)
  • CHEN, Yanhua
    Zhuhai City Guangdong 519090 (CN)
  • JIANG, Xiaoman
    Zhuhai City Guangdong 519090 (CN)

(74) Representative: Uexküll & Stolberg 
Partnerschaft von Patent- und Rechtsanwälten mbB Beselerstraße 4
22607 Hamburg
22607 Hamburg (DE)

   


(54) ARIPIPRAZOLE SUSTAINED-RELEASE MICROSPHERE AND PREPARATION METHOD THEREFOR


(57) The present invention provides an aripiprazole sustained release microsphere and a preparation method thereof, and the microsphere comprises aripiprazole and poly(lactide-co-glycolide), wherein the microsphere shows a spherical network framework structure with reticular pores being distributed over the spherical surface, and aripiprazole is filled in the pores. The microsphere has an average particle size of less than 20 µm, and the content of aripiprazole is 65%-80% of the total weight of the microsphere. Since the aripiprazole sustained release microsphere of the present invention has an average particle size of less than 20 µm, it is applicable to a 5-gauge needle, thereby reducing pain in patients. In addition, the microsphere of the present invention can quickly reach an effective drug concentration in the early stage of administration without the need for oral administration to achieve the therapeutic effect, and does not generate a burst release effect.