Title:
DRONEDARONE HYDROCHLORIDE INJECTION COMPOSITION, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
Document Type and Number:
WIPO Patent Application WO/2023/019993
Kind Code:
A1
Abstract:
The present invention relates to a dronedarone hydrochloride injection composition, a preparation method therefor and an application thereof, and specifically provides a dronedarone hydrochloride injection composition, which comprises dronedarone hydrochloride, cyclodextrin, an isoosmotic adjusting agent, a pH adjusting agent, an antioxidant, and water for injection. The cyclodextrin does not comprise β-cyclodextrin without a substituent. The dronedarone hydrochloride-cyclodextrin inclusion compound is good in stability, has greatly improved solubility in water, has the solubility improved by about 90 times compared with the solubility of dronedarone hydrochloride, has high bioavailability, and is suitable for industrial production. Moreover, the preparation operation of the dronedarone hydrochloride inclusion compound is simple, and it is easy for the prepared dronedarone hydrochloride inclusion compound to be prepared into a preparation. The prepared dronedarone hydrochloride injection is good in stability, and can be used for cardiac arrhythmia patients who are not suitable for oral administration.
Inventors:
GUO ZHEN (CN)
FU JUN (CN)
LU PENGCHENG (CN)
WANG TINGTING (CN)
YING SHUHUAN (CN)
FU JUN (CN)
LU PENGCHENG (CN)
WANG TINGTING (CN)
YING SHUHUAN (CN)
Application Number:
PCT/CN2022/087977
Publication Date:
February 23, 2023
Filing Date:
April 20, 2022
Export Citation:
Assignee:
SHANGHAI BOCIMED PHARMACEUTICAL CO LTD (CN)
SHANGHAI BOCIMED PHARMACEUTICAL RES CO LTD (CN)
SHANGHAI BOCIMED PHARMACEUTICAL RES CO LTD (CN)
International Classes:
A61K31/343; A61K47/69; A61P9/06
Other References:
MARCOLINO ANA ISA PEDROSO, MACEDO LETÍCIA BUENO, NOGUEIRA-LIBRELOTTO DANIELE RUBERT, FERNANDES JOANA RODRIGUES, BENDER CAROLINE RA: "Preparation, characterization and in vitro cytotoxicity study of dronedarone hydrochloride inclusion complexes", MATERIALS SCIENCE AND ENGINEERING C, ELSEVIER SCIENCE S.A., CH, vol. 100, 1 July 2019 (2019-07-01), CH , pages 48 - 61, XP055922931, ISSN: 0928-4931, DOI: 10.1016/j.msec.2019.02.097
MARCOLINO ANA ISA PEDROSO, MACEDO LETÍCIA BUENO, NOGUEIRA-LIBRELOTTO DANIELE RUBERT, VINARDELL MARÍA PILAR, ROLIM CLARICE MADALENA: "Comparative evaluation of the hepatotoxicity, phototoxicity and photosensitizing potential of dronedarone hydrochloride and its cyclodextrin-based inclusion complexes", PHOTOCHEMICAL & PHOTOBIOLOGICAL SCIENCES, ROYAL SOCIETY OF CHEMISTRY , CAMBRIDGE, GB, vol. 18, no. 6, 12 June 2019 (2019-06-12), GB , pages 1565 - 1575, XP055922935, ISSN: 1474-905X, DOI: 10.1039/C8PP00559A
MARCOLINO ANA ISA PEDROSO, MACEDO LETÍCIA BUENO, NOGUEIRA-LIBRELOTTO DANIELE RUBERT, VINARDELL MARÍA PILAR, ROLIM CLARICE MADALENA: "Comparative evaluation of the hepatotoxicity, phototoxicity and photosensitizing potential of dronedarone hydrochloride and its cyclodextrin-based inclusion complexes", PHOTOCHEMICAL & PHOTOBIOLOGICAL SCIENCES, ROYAL SOCIETY OF CHEMISTRY , CAMBRIDGE, GB, vol. 18, no. 6, 12 June 2019 (2019-06-12), GB , pages 1565 - 1575, XP055922935, ISSN: 1474-905X, DOI: 10.1039/C8PP00559A
Attorney, Agent or Firm:
BEIJING ORIGINTELLIGENCE IP LAW FIRM (CN)
Download PDF: