Title:
METHOD FOR PREPARING HIGH-BULK-DENSITY IBUPROFEN SPHERICAL CRYSTAL AND PRODUCT THEREOF
Document Type and Number:
WIPO Patent Application WO/2022/222680
Kind Code:
A1
Abstract:
Disclosed in the present invention are a method for preparing a high-bulk-density ibuprofen spherical crystal and a product thereof. The preparation method comprises: (1) heating ibuprofen to a molten liquid state; and (2) pressurizing the ibuprofen in the molten liquid state, then adding same, via a liquid distributor, in a dropwise manner to a crystallizer containing water, carrying out crystallization while adding in a dropwise manner under stirring until the dropwise addition of the ibuprofen in the molten liquid state is completed, and reducing the rotation rate of stirring, carrying out crystal growing, and finally, carrying out a post-treatment on crystal slurry to obtain the ibuprofen spherical crystal with a bulk density of 0.50-0.70 g/mL, a tap density of 0.63-0.89 g/mL, a median particle size of 300-1000 μm, and a repose angle of 22-29°. The preparation method has a simple process, is free of additives and is suitable for industrial production. The prepared ibuprofen spherical crystal has a regular crystal habit, a smooth crystal face, a good fluidity, a high bulk density and a high product purity, and the product quality meets pharmacopoeia requirements CP2020, EP9.8, USP41, etc.
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Inventors:
LIU JINLONG (CN)
LV SHUMIN (CN)
HU RUIJUN (CN)
HE XUEZHONG (CN)
DU MENGLIANG (CN)
WANG XIAOCHUN (CN)
WANG ZIYU (CN)
LIANG LANYING (CN)
LV SHUMIN (CN)
HU RUIJUN (CN)
HE XUEZHONG (CN)
DU MENGLIANG (CN)
WANG XIAOCHUN (CN)
WANG ZIYU (CN)
LIANG LANYING (CN)
Application Number:
PCT/CN2022/082699
Publication Date:
October 27, 2022
Filing Date:
March 24, 2022
Export Citation:
Assignee:
ZHEJIANG NHU CO LTD (CN)
International Classes:
C07C51/43; C07C57/30
Foreign References:
| CN113200846A | 2021-08-03 | |||
| CN109956860A | 2019-07-02 | |||
| US4476248A | 1984-10-09 | |||
| US5191114A | 1993-03-02 | |||
| US20120004308A1 | 2012-01-05 | |||
| CN102311335A | 2012-01-11 | |||
| CN104193614A | 2014-12-10 | |||
| EP0362728A2 | 1990-04-11 |
Other References:
SUN MENGMENG, SHICHAO DU, TANG WEIWEI, JIA LINA, GONG JUNBO: "Design of Spherical Crystallization for Drugs Based on Thermal-Induced Liquid–Liquid Phase Separation: Case Studies of Water-Insoluble Drugs", INDUSTRIAL & ENGINEERING CHEMISTRY RESEARCH, AMERICAN CHEMICAL SOCIETY, vol. 58, no. 44, 6 November 2019 (2019-11-06), pages 20401 - 20411, XP055977944, ISSN: 0888-5885, DOI: 10.1021/acs.iecr.9b03795
TEYCHENE, S. ET AL.: "Is Spherical Crystallization without Additives Possible?", CHEMICAL ENGINEERING RESEARCH AND DESIGN, vol. 88, 31 December 2010 (2010-12-31), XP027544305, ISSN: 0263-8762
TEYCHENE, S. ET AL.: "Is Spherical Crystallization without Additives Possible?", CHEMICAL ENGINEERING RESEARCH AND DESIGN, vol. 88, 31 December 2010 (2010-12-31), XP027544305, ISSN: 0263-8762
Attorney, Agent or Firm:
HANGZHOU ZHIXIAN PATENT AGENCY (CN)
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