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Title:
COMPOSITIONS OF DISPERSED PHASE FOR PREPARATION OF APIXABAN-LOADED MICROSPHERES AND BIOCOMPATIBLE POLYMER-BASED APIXABAN-LOADED MICROSPHERES PREPARED THEREFROM
Document Type and Number:
WIPO Patent Application WO/2020/197185
Kind Code:
A1
Abstract:
The present invention relates to a composition of dispersed phase for the preparation of Apixaban-loaded microspheres and biocompatible polymer-based Apixaban-loaded microspheres prepared therefrom. Specifically, the present invention relates to a composition of dispersed phase for the preparation of Apixaban-loaded microspheres, comprising i) Apixaban or a pharmaceutically acceptable salt thereof; ii) a biocompatible polymer; iii) a fatty acid or triglyceride; and iv) a halogen organic solvent; and biocompatible polymer-based Apixaban-loaded microspheres. The composition of dispersed phase for the preparation of Apixaban-loaded microspheres shows excellent stability and thus can be useful for the preparation of Apixaban-loaded microspheres. Additionally, the biocompatible polymer-based Apixaban-loaded microspheres can be contained in pharmaceutical compositions to be used as a therapeutic agent, because the Apixaban can be stably encapsulated therein in high contents and the initial drug release thereof can be suppressed.

Inventors:
JEONG DOOYONG (KR)
LEE SANG-HWI (KR)
KIM MIJUNG (KR)
KIM YE-JI (KR)
JOO SO KYOUNG (KR)
PARK JAE HYUNG (KR)
KIM SAE JONG (KR)
Application Number:
PCT/KR2020/003876
Publication Date:
October 01, 2020
Filing Date:
March 20, 2020
Export Citation:
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Assignee:
MEDIFORUM PHARM (KR)
International Classes:
A61K9/16; A61K9/00; A61K31/437; A61K47/12; A61K47/14
Foreign References:
US20170202826A12017-07-20
KR102045721B12019-11-18
KR102044676B12019-11-14
Other References:
CHU, DAFENG et al., “Poly(lactic-co-glycolic acid) microspheres for the controlled release of huperzine A: in vitro and in vivo studies and the application in the treatment of the impaired memory of mice.” Chem. Pharm. Bull. 2007, Vol. 55, No. 4, pp. 625-628 See abstract; and page 625.
SIMA REZVANTALAB, KESHAVARZ MORAVEJI MOSTAFA: "Microfluidic assisted synthesis of PLGA drug delivery systems", RSC ADVANCES, vol. 9, no. 4, 15 January 2019 (2019-01-15), pages 2055 - 2072, XP055736562, DOI: 10.1039/C8RA08972H
See also references of EP 3946273A4
Attorney, Agent or Firm:
HANOL INTELLECTUAL PROPERTY AND LAW (KR)
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