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Regorafenib solid dispersion and preparation thereof

A technology of regorafenib solid and solid dispersion, applied in the field of regorafenib solid dispersion and its preparation, and pharmaceutical preparations containing the solid dispersion, can solve the problems of incomplete dissolution and slow dissolution speed, and achieve Improved solubility, low cost, and improved stability

Active Publication Date: 2017-09-29
广东安诺药业股份有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0010] The present invention aims to provide a stable solid dispersion of regorafenib with significantly improved dissolution rate and bioavailability, and pharmaceutical preparations containing the above solid dispersion of regorafenib and other pharmaceutically acceptable adjuvants to solve the problem of Problems such as incomplete dissolution and slow dissolution rate caused by low solubility of regorafenib

Method used

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  • Regorafenib solid dispersion and preparation thereof
  • Regorafenib solid dispersion and preparation thereof
  • Regorafenib solid dispersion and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-7 and comparative example 1-4

[0033] Preparation of Example 1-7 and Comparative Example 1-4 Regorafenib Solid Dispersion

Embodiment 1-7

[0034] Example 1-7 The composition of regorafenib solid dispersion is shown in the table below:

[0035]

Embodiment 1

[0038] Example 1 Preparation of regorafenib solid dispersion:

[0039](1) Dissolving regorafenib in absolute ethanol to make a solution with a concentration of 20% (m / v) for later use;

[0040] (2) get sorbitol to be dissolved in water, make the solution that concentration is 35% (m / v), for subsequent use;

[0041] (3) Under stirring conditions, add the sorbitol aqueous solution to the regorafenib ethanol solution, stir for 10 min, then add the pre-dissolved povidone ethanol solution with a concentration of 15% (m / v), and continue stirring for 3 min , Concentrate the solution to dryness under reduced pressure with a rotary evaporator, transfer the product to a vacuum drying oven, and continue drying at room temperature for 24 hours to obtain the product.

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Abstract

The invention discloses a regorafenib solid dispersion, which comprises regorafenib, a carrier material and a synergistic agent in the mass ratio of 1: (2-20): (0.2-5), the carrier material comprises povidone and sorbitol in the mass ratio of 1: (0.1-0.5), and the synergistic agent comprises silica and Docusate sodium in the mass ratio of 1: (0.5-1). Through a certain process, the regorafenib is prepared into the sorbitol-regorafenib-povidone sandwich structure solid dispersion, dissolution of the regorafenib from inside to outside is promoted, the solubility of the regorafenib is greatly improved, safe, non-toxic and volatile ethanol is used as a solvent in the preparation process, and no security risk is caused by residual solvent. At the same time, the aging phenomenon in the long time storage process of the regorafenib solid dispersion can be avoided, and stability is improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a regorafenib solid dispersion, a preparation method thereof, and a pharmaceutical preparation containing the solid dispersion. Background technique [0002] Regorafenib, chemical name: N-(4-chloro-3-(trifluoromethyl)phenyl)-N'-2-fluoro-(4-(2-(N-methylcarbamoyl) -4-pyridyloxy)phenyl)urea, the structural formula is: [0003] [0004] It is a new type of multikinase inhibitor, which can block various enzymes that promote tumor growth. It was discovered and developed by Bayer. It is an effective anticancer and antiangiogenic agent, which has various activities, including VEGFR , PDGFR, raf, p38 and / or flt-3 kinase signaling molecule inhibitory activity, and it can be used in the treatment of various diseases and conditions, such as hyperproliferative diseases, such as: cancer, tumor, lymphoma, sarcoma and leukemia, mainly with For the treatment o...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K47/26A61K47/32A61K47/04A61K47/20A61K31/44A61P35/00
CPCA61K9/2009A61K9/2013A61K9/2018A61K9/2027A61K31/44
Inventor 龙世松曹祺
Owner 广东安诺药业股份有限公司
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