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Anti-tumour medicine composition

A composition and drug technology, applied in the field of new anti-tumor drug composition, can solve problems such as blindness, excessive blood vessel proliferation, etc., and achieve the effect of excellent pharmaceutical properties

Active Publication Date: 2015-05-06
北京元延医药科技股份有限公司
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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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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0134] Example 1: Preparation of pharmaceutical composition in tablet form

[0135] Plain Tablet Prescription (per tablet):

[0136] The monohydrate of the compound of formula I: 40 mg (calculated as anhydrous substance),

[0137] Polyvinylpyrrolidone (k25): 160 mg,

[0138] Croscarmellose sodium (adding part of disintegrant): 100mg,

[0139] Microcrystalline cellulose: 100mg;

[0140] Croscarmellose sodium (additional part of disintegrant): 54mg,

[0141] Colloidal silicon dioxide (anhydrous grade, that is, colloidal silicon dioxide, also known as colloidal anhydrous silica): 2.4mg,

[0142] Magnesium stearate: 3.6 mg.

[0143] Preparation method:

[0144] (1) (a) dissolving two solid materials of active drug and polyvinylpyrrolidone in a prescription amount in a solvent ethanol-acetone mixture (ethanol: acetone=1:4, the weight ratio of solid material to solvent is 1:3), Prepare a drug-containing solution; (b) at a temperature of 60-70°C, use a fluidized bed vacu...

Embodiment 2

[0148] Embodiment 2: 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 (k30): 100 mg,

[0152] Croscarmellose sodium (adding part of disintegrant): 150mg,

[0153] Microcrystalline cellulose: 50mg;

[0154] Croscarmellose sodium (additional part of disintegrant): 50mg,

[0155] Colloidal silicon dioxide: 2mg,

[0156] Magnesium stearate: 3 mg.

[0157] Preparation method:

[0158] (1) (a) dissolving two solid materials of active drug and polyvinylpyrrolidone in a prescription amount in a solvent ethanol-acetone mixture (ethanol: acetone=1:2, the weight ratio of solid material to solvent is 1:2), Prepare 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 a part of the disintegratin...

Embodiment 3

[0162] Embodiment 3: 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 (k15): 200 mg,

[0166] Croscarmellose sodium (adding part of disintegrant): 40mg,

[0167] Microcrystalline cellulose: 200mg;

[0168] Croscarmellose sodium (additional part of disintegrant): 10mg,

[0169] Colloidal silicon dioxide: 2mg,

[0170] Magnesium stearate: 3 mg.

[0171] Preparation method:

[0172] (1) (a) dissolving two solid materials of active drug and polyvinylpyrrolidone in a prescription amount in a solvent ethanol-acetone mixture (ethanol: acetone=1:6, the weight ratio of solid material to solvent is 1:4), Prepare 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 a part of the disintegratin...

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Abstract

The invention relates to an anti-tumour medicine composition, and specifically relates to a medicine composition. The anti-tumour medicine composition comprises an active pharmaceutical compound, a diluent, a disintegrant, an adhesive and a lubricant. The compound is a compound shown in a formula I specified in the description or a pharmaceutically acceptable salt, a solvate, a polycrystalline type compound and the like. The invention further relates to coated tablets prepared by the medicine composition. The composition disclosed by the invention is excellent in pharmaceutical properties.

Description

technical field [0001] The present invention relates to novel antineoplastic pharmaceutical compositions useful for the treatment of diseases and disease symptoms mediated by abnormal VEGFR, PDGFR, raf, p38, and / or flt-3 kinase signaling. 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 cells Return to normal growth phenotype. Kolch et al. further demonstrated that inhibition of raf expression by antisense RNA blocks cell proliferation induced by a m...

Claims

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Application Information

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IPC IPC(8): A61K9/28A61K9/30A61K9/36A61K31/44A61P35/00
Inventor 王立强郑金琪黄丽华
Owner 北京元延医药科技股份有限公司
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