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Regorafenib tablet pharmaceutical composition and preparation method thereof

A composition and solvate technology, applied in the field of new anti-tumor drug compositions, can solve the problems of excessive blood vessel proliferation, blindness and the like

Active Publication Date: 2015-04-29
HANGZHOU ZHUYANGXIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Overexpression of VEGF (such as under extreme hypoxic conditions) can cause angiogenesis in the eyeball, resulting in excessive blood vessel proliferation and eventually blindness

Method used

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  • Regorafenib tablet pharmaceutical composition and preparation method thereof
  • Regorafenib tablet pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0148] Example 1: Preparation of pharmaceutical composition in tablet form

[0149] Plain Tablet Prescription (per tablet):

[0150] The monohydrate of the compound of formula I: 40 mg (calculated as anhydrous substance),

[0151] Polyvinylpyrrolidone (k25): 160 mg,

[0152] Croscarmellose sodium (adding part of disintegrant): 100mg,

[0153] Microcrystalline cellulose: 100mg;

[0154] Croscarmellose sodium (additional part of disintegrant): 54mg,

[0155] Colloidal silicon dioxide (anhydrous grade, that is, colloidal silicon dioxide, also known as colloidal anhydrous silica): 2.4mg,

[0156] Magnesium stearate: 3.6 mg.

[0157] Preparation method:

[0158] (1) (a) The active drug of prescription quantity and two kinds of solid materials of polyvinylpyrrolidone are dissolved in solvent ethyl acetate-ethanol mixed solution (ethyl acetate: ethanol=1:4, solid material and solvent weight ratio are 1: 3) to make a drug-containing solution; (b) at a temperature of 60-70...

Embodiment 2

[0162] Embodiment 2: Preparation of pharmaceutical composition in tablet form

[0163] Plain Tablet Prescription (per tablet):

[0164] The monohydrate of the compound of formula I: 40 mg (calculated as anhydrous substance),

[0165] Polyvinylpyrrolidone (k30): 100 mg,

[0166] Croscarmellose sodium (adding part of disintegrant): 150mg,

[0167] Microcrystalline cellulose: 50mg;

[0168] Croscarmellose sodium (additional part of disintegrant): 50mg,

[0169] Colloidal silicon dioxide: 2mg,

[0170] Magnesium stearate: 3 mg.

[0171] Preparation method:

[0172] (1) (a) The active drug of prescription quantity and two kinds of solid materials of polyvinylpyrrolidone are dissolved in solvent ethyl acetate-ethanol mixed solution (ethyl acetate: ethanol=1: 2, solid material and solvent weight ratio are 1: 2) to make a drug-containing solution; (b) at a temperature of 60-70 ° C, use a fluidized bed vacuum granulator to spray the solution into a powder bed of diluent an...

Embodiment 3

[0176] Embodiment 3: Preparation of pharmaceutical composition in tablet form

[0177] Plain Tablet Prescription (per tablet):

[0178] The monohydrate of the compound of formula I: 40 mg (calculated as anhydrous substance),

[0179] Polyvinylpyrrolidone (k15): 200 mg,

[0180] Croscarmellose sodium (adding part of disintegrant): 40mg,

[0181] Microcrystalline cellulose: 200mg;

[0182] Croscarmellose sodium (additional part of disintegrant): 10mg,

[0183] Colloidal silicon dioxide: 2mg,

[0184] Magnesium stearate: 3 mg.

[0185] Preparation method:

[0186] (1) (a) The active drug of prescription quantity and two kinds of solid materials of polyvinylpyrrolidone are dissolved in solvent ethyl acetate-ethanol mixed solution (ethyl acetate: ethanol=1: 6, solid material and solvent weight ratio are 1: 4) to make a drug-containing solution; (b) at a temperature of 60-70°C, use a fluidized bed vacuum granulator to spray the solution into a powder bed of a diluent and ...

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Abstract

The invention relates to a regorafenib tablet pharmaceutical composition and a preparation method thereof and in particular relates to a pharmaceutical composition. The pharmaceutical composition comprises an active pharmaceutical compound, a diluent, a disintegrating agent, an adhesive and a lubricating agent, wherein the active pharmaceutical compound refers to 4-[4-({4-chloro-3-(trifluoromethyl)phenyl]carbamyl}amino)-3-chlorophenoxy]-N-methylpyridine-2-formamide or pharmaceutically acceptable salts, solvates and polymorphism. The pharmaceutical composition has a contact angle of 40-100 degrees, particularly a contact angle of 40-90 degrees, preferably a contact angle of 40-80 degrees, and in particular a contact angle of 40-70 degrees. The pharmaceutical composition disclosed by the invention can be used for treating diseases and disease symptoms mediated by abnormal VEGFR, PDGFR, raf, p38 and / or flt-3 kinase signals. The invention also relates to a method for preparing an anti-tumor pharmaceutical composition. The pharmaceutical composition disclosed by the invention has excellent preparation performance.

Description

technical field [0001] The present invention relates to a new antitumor pharmaceutical composition, in particular to a regorafenib tablet pharmaceutical composition, which can be used for the treatment of abnormal VEGFR, PDGFR, raf, p38, and / or flt-3 kinase Signaling-mediated diseases and disease symptoms. The invention also relates to a preparation method of the antitumor pharmaceutical composition. Background technique [0002] Activation of the ras signaling pathway implies a cascade of events with profound effects on cell proliferation, differentiation and transformation. Raf kinase, a downstream effector of Ras, is a key transmitter of these signals from cell surface receptors to the nucleus. Inhibition of the effect of activated ras by inhibition of the raf kinase signaling pathway using an inactivating antibody to raf kinase or co-expression of dominant negative raf kinase or dominant negative MEK (a substrate of raf kinase) has been shown to result in transformed c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K31/44A61K9/30A61K9/36A61P35/00
Inventor 李阅东唐建飞沈如杰何海珍马雯霞姚成娥张群赵福斌张婧
Owner HANGZHOU ZHUYANGXIN PHARMA
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