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Preparation method of cabozantinib s-malate tablets

A technology of cabozantinib malate tablets and cabozantinib malate, which is applied in the field of medicine, can solve problems such as poor fluidity, and achieve the effect of less process steps, suitable for industrial production, and easy operation

Inactive Publication Date: 2018-04-24
深圳万乐药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] In order to solve the existing problems in the preparation of Cabozantinib Malate Tablets, the invention provides a method for preparing Cabozantinib Malate Tablets. The poor fluidity of the raw drug of tini after crushing is not suitable for direct tableting. The preparation process is simpler than wet granulation, and the hardness, friability and content uniformity of the obtained cabozantinib malate tablets are qualified, and the active drug is dissolved degree is improved

Method used

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  • Preparation method of cabozantinib s-malate tablets
  • Preparation method of cabozantinib s-malate tablets
  • Preparation method of cabozantinib s-malate tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Embodiment 1 powder direct compression method prepares cabozantinib malate tablet

[0047] Take the raw and auxiliary materials (5000 tablets) according to the following prescription:

[0048] prescription

Content per piece

Cabozantinib Malate

76.03mg

Microcrystalline Cellulose (PH102)

332.7mg

Lactose (F100)

300mg

Carboxymethyl Starch Sodium

30mg

Colloidal silica (A200P)

3.75mg

Magnesium stearate

7.5mg

Core weight

750mg

Film coating premix (Opadry 03K92254) weight gain

4.0％

[0049] Preparation:

[0050] 1. Grind cabozantinib malate until D90≦25μm, set aside;

[0051] 2. Put cabozantinib malate, microcrystalline cellulose, lactose, carboxymethyl starch sodium, and colloidal silicon dioxide in a 10L hopper mixer machine. The materials account for 50% of the total volume of the hopper mixer. Turn on the equipment and mix After 150 revolutions, pass through a 60-mesh ...

Embodiment 2

[0056] Example 2 Preparation of cabozantinib malate tablets by wet granulation and tabletting

[0057] Take the raw and auxiliary materials (5000 tablets) according to the following prescription:

[0058] prescription

Content per piece

Cabozantinib Malate

76.03mg

Microcrystalline Cellulose (PH102)

93.24mg

Anhydrous Lactose (60M)

46.61mg

Hydroxypropyl Cellulose (EXF)

7.2mg

Colloidal silica (A200P)

0.72mg

Croscarmellose Sodium

14.4mg

Magnesium stearate

1.8mg

Core weight

210mg

Film coating premix (Opadry 03K92254) weight gain

4.0％

[0059] Preparation:

[0060] 1. Grind cabozantinib malate until D90≦25μm, set aside;

[0061] 2. Put cabozantinib malate, microcrystalline cellulose, lactose, and croscarmellose sodium (internal addition) into the wet granulator, turn on the equipment, and pre-mix for 20 minutes;

[0062] 3. Add an appropriate amount of water and stir ...

Embodiment 3

[0071] Example 3 Cabozantinib Malate Tablets (prepared in Examples 1 and 2) Take 0.01N HCl (0.5% Triton) as the Dissolution Profile Determination of Dissolution Medium

[0072] Determination of the dissolution curve of cabozantinib malate tablets in pH4.5 acetic acid-sodium acetate buffer solution (0.5% Triton) dissolution medium as follows:

[0073] Get respectively the cabozantinib malate sheet prepared by embodiment 1 and 2 according to the dissolution assay method (the second method of the second appendix XC of the Chinese Pharmacopoeia version in 2010), with water pH4.5 acetic acid-sodium acetate buffer solution (0.5% Triton) is the dissolution medium, and the rotating speed is 75 revolutions per minute, and it is operated according to the law. At 5, 10, 15, 30, 45, and 60 minutes, take 3.0ml of the dissolution solution, filter it through a 0.45μm filter membrane, and add the same amount of dissolution medium at the same temperature at the same time. The dissolution resu...

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Abstract

The invention provides a preparation method of cabozantinib s-malate tablets. The preparation method has the advantages that the tablets are prepared by directly subjecting powder to tableting, the technical problem that crushed cabozantinib s-malate raw material drugs are poor in flowability and not suitable for being subjected to direct tableting is solved, the preparation process is simpler than wet-method granulation and tableting, the hardness, rigidity and content of the obtained cabozantinib s-malate tablets are up to standards, and active drug dissolution rate is increased.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of cabozantinib malate tablets. Background technique [0002] Cabozantinib is a tyrosine kinase inhibitor. In vitro biochemical and / or cellular assays show that Cabozantinib inhibits RET, MET, VEGFR-1, -2 and -3, KIT, TRKB, FLT -3. Tyrosine kinase activity of AXL and TIE-2 receptors. [0003] In November 2012, the US FDA approved Cabozantinib Malate Capsules developed by Exelixis for the treatment of patients with advanced and metastatic medullary thyroid carcinoma (MTC), with the trade name COMETRIQTM. The active ingredient of COMETRIQ is the L-malate form of cabozantinib, whose chemical structure is shown in the diagram below. [0004] [0005] In 2016, the US FDA approved Exelixis' cabozantinib malate tablets (trade name CABOMETYX, three specifications of 20mg / 40mg / 60mg) for the treatment of patients with advanced renal cell carcinoma who had previou...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/36A61K31/47A61P35/00A61P35/04
CPCA61K31/47A61K9/2059A61K9/2095A61K9/2866
Inventor 杨流宽朱勇于玉根刘文皓卢政辉
Owner 深圳万乐药业有限公司
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