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Regorafenib oral solid pharmaceutical composition preparation method

A solid composition, regorafenib technology, applied in the field of medicine and chemical industry, can solve the problems of low bioavailability, low solubility, slow dissolution rate, etc., and achieve the effect of improving bioavailability and enhancing stability

Inactive Publication Date: 2016-01-27
JIANGSU SINOBIOPHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the existing regorafenib has the problems of low solubility, slow dissolution rate, low bioavailability, and poor stability of the drug, which is not conducive to large-scale use in the market

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment １

[0018] A preparation method of regorafenib oral solid pharmaceutical composition, comprising the following steps:

[0019] (1) Dissolve 155g to 165g of the binder povidone K25 in a mixed solution of 470g to 490g of acetone and 115g to 125g of ethanol, stir well, add 40g of regorafenib raw material after stirring, and mix evenly to obtain granulation liquid;

[0020] (2) Mix 197g-105g diluent microcrystalline cellulose PH10 and 153g-158g disintegrant sodium carboxymethyl cellulose to obtain mixed auxiliary materials;

[0021] (3) Add the granulation liquid to the mixed excipients of the pharmaceutical composition by spraying, granulate and dry through a dry granulator, and prepare a solid dispersion of regorafenib;

[0022] (4) The regorafenib solid dispersion is made into the smallest pharmaceutical dosage unit of regorafenib, that is, the preparation of the regorafenib oral solid pharmaceutical composition is completed.

[0023] The minimum medicinal dose of regorafenib in ...

Embodiment ２

[0025] A preparation method of regorafenib oral solid pharmaceutical composition, comprising the following steps:

[0026] (1) Dissolve 155g to 165g of the binder povidone K25 in a mixed solution of 470g to 490g of acetone and 115g to 125g of ethanol, stir well, add 40g of regorafenib raw material after stirring, and mix evenly to obtain granulation liquid;

[0027] (2) Mix 197g-105g diluent microcrystalline cellulose PH10 and 153g-158g disintegrant sodium carboxymethyl cellulose to obtain mixed auxiliary materials;

[0028] (3) Add the granulation liquid to the mixed excipients of the pharmaceutical composition by spraying, granulate and dry through a dry granulator, and prepare a solid dispersion of regorafenib;

[0029] (4) The regorafenib solid dispersion is made into the smallest pharmaceutical dosage unit of regorafenib, that is, the preparation of the regorafenib oral solid pharmaceutical composition is completed.

Embodiment 2

[0030] The minimum medicinal dose of regorafenib in Example 2 is a tablet, each containing 40 mg of regorafenib; the oral solid composition of regorafenib is made of the following raw materials: regorafenib, microcrystalline cellulose ph101 , povidone k25, croscarmellose sodium, colloidal silicon dioxide and magnesium stearate, regorafenib, microcrystalline cellulose ph101, povidone k25, croscarmellose sodium , The mass ratio of colloidal silicon dioxide and magnesium stearate is: 40:100:160:155:3.5:2.5.

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PUM

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Abstract

The present invention discloses a regorafenib oral solid pharmaceutical composition preparation method, a binder solution is first prepared by solvent method, then regorafenib is added into the binder solution, and sufficiently stirred to obtain a clear granulating liquid; the clear granulating liquid is then sprayed into other auxiliary material to prepare into a suitable solid dispersion; further the suitable solid dispersion is compressed into the smallest pharmaceutical dosage unit, the tablet may further be coated; the composition contains a binder, a disintegrating agent, a lubricant and a wetting agent. Advantages of the method are that: the method mainly solves the problems of small regorafenib solubility andslow dissolution rate to further improve the bioavailability and enhance the stability of the drug.

Description

technical field [0001] The invention belongs to the field of medicine and chemical industry, and in particular relates to a preparation method of regorafenib oral solid pharmaceutical composition. Background technique [0002] Regorafenib's Chinese name: N-(4-chloro-3-(trifluoromethyl)phenyl)-N'-2-fluoro-(4-(2-(N-methylcarbamoyl) -4-pyridyloxy)phenyl)urea, regorafenib is a novel multi-kinase inhibitor that can block tumor-promoting [0003] A variety of enzymes, discovered and developed by Bayer; in September 2012, the US FDA approved it for the treatment of metastatic colorectal cancer; in February 2013, its new indication (advanced gastrointestinal stromal tumor) passed FDA priority review The evaluation process is approved. The drug is also granted orphan drug status for the treatment of rare diseases. [0004] However, the existing regorafenib has the problems of low solubility, slow dissolution rate, low bioavailability, and poor drug stability, which is not conduciv...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/44A61K47/32A61K47/38A61P35/04
Inventor 黄乐群夏孝天
Owner JIANGSU SINOBIOPHARMA
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