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Axitinib tablet and preparation method thereof

An axitinib tablet and axitinib technology, which are applied in the field of medicine, can solve the problems of unqualified, low bioavailability, low solubility of insoluble drugs, etc., and achieve the effects of rapid drug dissolution and simple preparation process

Active Publication Date: 2017-07-04
SHANDONG NEWTIME PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because axitinib is a poorly soluble drug and is almost insoluble in water, the actual production of axitinib oral solid preparations often encounters the problem of low dissolution rate or even unqualified
When there is an urgent need for quick-acting and high-efficiency preparations in clinical practice, solving the problem of low bioavailability of insoluble drugs due to low solubility and slow dissolution has always been a major problem in the pharmaceutical industry
This technology has problems such as easy re-aggregation of drugs, poor mixing uniformity of raw materials and excipients, and insignificant effect of improving dissolution.
[0009] In the prior art, there is not yet an effective method for improving the dissolution rate of axitinib tablets

Method used

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  • Axitinib tablet and preparation method thereof
  • Axitinib tablet and preparation method thereof
  • Axitinib tablet and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027]

[0028] Preparation Process:

[0029] Dissolve axitinib in glacial acetic acid, add mesoporous silica, stir evenly, add sodium hydroxide aqueous solution to this solution under stirring conditions, axitinib and mesoporous silica complexes are precipitated, Filter, dry at 60°C, then mix with microcrystalline cellulose and sodium carboxymethyl starch, mix evenly, add magnesium stearate, mix, and compress into tablets.

Embodiment 2

[0031] Axitinib 5g

[0032] Glacial acetic acid 25g

[0033] Mesoporous silica gel 2.5g

[0034] 5mol / L sodium hydroxide aqueous solution 83.4ml

[0035] Microcrystalline Cellulose 150g

[0036] Crospovidone 5g

[0037] Magnesium Stearate 1g

[0038] Preparation Process:

[0039] Dissolve axitinib in glacial acetic acid, add mesoporous silica, stir evenly, add sodium hydroxide aqueous solution to this solution under stirring conditions, axitinib and mesoporous silica complexes are precipitated, Filtrate, dry at 65°C, then mix evenly with the mixed powder of microcrystalline cellulose and crospovidone, add magnesium stearate, mix, and compress into tablets.

Embodiment 3

[0041]

[0042] Preparation Process:

[0043] Dissolve axitinib in glacial acetic acid, add mesoporous silica, stir evenly, add sodium hydroxide aqueous solution to this solution under stirring conditions, axitinib and mesoporous silica complexes are precipitated, Filter, dry at 60°C, then mix with microcrystalline cellulose and sodium carboxymethyl starch, mix evenly, add magnesium stearate, mix, and compress into tablets.

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PUM

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Abstract

The invention discloses an axitinib tablet and a preparation method thereof. The preparation method comprises the following steps: controlling crystallization process so as to obtain an axitinib-mesoporous silica compound, then mixing the axitinib-mesoporous silica compound with a filler and a disintegrating agent, carrying out granulation and drying, adding a lubricant into dry particles and then carrying out tableting. Compared with the prior art, the axitinib tablet prepared in the invention can be rapidly dissolved out in water, and the preparation method is simple in process and suitable for industrial production.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an axitinib tablet and a preparation method thereof. Background technique [0002] Axitinib was approved by the FDA on January 27, 2012, for the treatment of advanced renal cell carcinoma (Renal Cell Carcinoma, RCC) ineffective by other systemic treatments. Axitinib was developed by Pfizer with the trade name Inlyta. Similar to Sunitinib, another anticancer drug of Pfizer, axitinib is also a multi-target tyrosine kinase inhibitor, which can inhibit the vascular endothelial cell growth factor receptors VEGFR1, VEGFR2, VEGFR3, platelet-derived growth Factor receptors and c-KIT. [0003] The chemical name of axitinib is N-methyl-2-[[3-[(1E)-2-(2-pyridyl)vinyl]-1H-indazol-6-yl]thio]-benzo Amide, the structural formula is as follows: [0004] [0005] Molecular formula: C 22 h 18 N 4 OS, molecular weight: 386.47 [0006] Axitinib is a white to slightly yellow p...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/4439A61K47/04A61P35/00
CPCA61K9/2009A61K9/2054A61K9/2059A61K31/4439
Inventor 张贵民陈小伟郑华李姝影
Owner SHANDONG NEWTIME PHARMA
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