Oral solid tablet comprising bruton's tyrosine kinase inhibitor and preparation method therefor

Pending Publication Date: 2022-08-11
BEIGENE SWITZERLAND GMBH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The melting point of the active pharmaceutical ingredient is 145° C., which is lower than the ideal melting point of 150° C. for tablet development,

Method used

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  • Oral solid tablet comprising bruton's tyrosine kinase inhibitor and preparation method therefor
  • Oral solid tablet comprising bruton's tyrosine kinase inhibitor and preparation method therefor
  • Oral solid tablet comprising bruton's tyrosine kinase inhibitor and preparation method therefor

Examples

Experimental program
Comparison scheme
Effect test

Example

Example 1

[0048]Preparation of Solid Tablet for Oral Administrations of Zanubrutinib, Specification: 160 mg

[0049]Prescription (Per 100 g Plain Tablets):

Zanubrutinib (Crystal form A)34.8gLactose53.2gCroscarmellose sodium2gColloidal silica4.5gSodium lauryl sulfate1gMicrocrystalline cellulose4gMagnesium stearate0.5gOpadry2.4g

[0050]Preparation Process: 53.2 g of lactose, 2 g of croscarmellose sodium, 1 g of sodium lauryl sulfate and 34.8 g of Zanubrutinib are added into a high-shear granulator (MYCROMIX, manufactured by BOSCH) and mixed for 5 minutes, an appropriate amount of purified water is added for granulation, followed by dying and then sizing, 4.5 g of colloidal silica, 4 g of microcrystalline cellulose and 0.5 g of magnesium stearate are further added and mixed. After mixing, the above ingredients are pressed into tablets to obtain plain tablets. The above-mentioned plain tablets are coated with 2.4 g of Opadry to obtain solid tablet for oral administrations containing Zanubrutin...

Example

Example 2

[0053]Preparation of Solid Tablet for Oral Administrations of Zanubrutinib, Specification: 160 mg

[0054]Prescription (Per 100 g Plain Tablets):

Zanubrutinib (Crystal form A)36.2gLactose55.6gCroscarmellose sodium2.2gColloidal silica4.3gSodium lauryl sulfate1.1gMagnesium stearate0.5g

[0055]Preparation Process: 55.6 g of lactose, 2.2 g of croscarmellose sodium, 1.1 g of sodium lauryl sulfate, 4.3 g of colloidal silica and 36.2 g of Zanubrutinib are added into a high-shear granulator and mixed for 5 minutes, an appropriate amount of purified water is added for granulation, followed by dying and then sizing, and 0.5 g of magnesium stearate is further added and mixed. After mixing, the above ingredients are pressed into tablets to obtain plain tablets, that is, an solid tablet for oral administration containing Zanubrutinib.

[0056]Drug Cumulative Dissolution (In Vitro Dissolution) Test: About 90% of Zanubrutinib is dissolved at 30 minutes.

Example

Example 3

[0057]Preparation of Solid Tablet for Oral Administrations of Zanubrutinib, Specification: 160 mg

[0058]Prescription (Per 100 g Plain Tablets):

Zanubrutinib (Crystal form A)33.3gLactose49.2gHypromellose2gCroscarmellose sodium2gColloidal silica4gSodium lauryl sulfate1gMicrocrystalline cellulose8gMagnesium stearate0.5g

[0059]Preparation Process: 49.2 g of lactose, 2 g of croscarmellose sodium, 1 g of sodium lauryl sulfate and 33.3 g of Zanubrutinib are added into a high-shear granulator and mixed for 5 minutes, 2 g of hypromellose aqueous solution is added for granulation, followed by dying and then sizing, 4 g of colloidal silica, 8 g of microcrystalline cellulose and 0.5 g of magnesium stearate are further added and mixed. After mixing, the above ingredients are pressed into tablets to obtain plain tablets, that is, an solid tablet for oral administration containing Zanubrutinib.

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Abstract

Provided are an oral solid tablet comprising (S)-7-[4-(1-acryloylpiperidine)]-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and preparation method therefor. The oral solid tablet has good drug release characteristics, features easy administration, quick and high-efficient release, no particular requirements on equipment, and a simple formulation preparation process, can ensure formulation stability and facilitate transportation and storage, and is suitable for large-scale production.

Description

TECHNICAL FIELD[0001]The present invention relates to an solid tablet for oral administration containing a Bruton's Tyrosine Kinase (BTK) inhibitor, in particular (S)-7-[4-(1-acryloylpiperidine)]-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide and a preparation method thereof.BACKGROUND ART[0002]International application WO 2014173289 A disclosed a novel Bruton's Tyrosine Kinase (BTK), more particularly (S)-7-[4-(1-acryloylpiperidine)]-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a] pyrimidine-3-carboxamide (with a generic name of Zanubrutinib), which has a chemical structure as follows:[0003]Zanubrutinib belongs to the second-generation BTK inhibitor, which irreversibly inactivates the tyrosine kinase by covalently binding with the enzyme. It is used as a single agent or in combination with other drugs for the treatment of B lymphocyte tumors, including chronic lymphocytic leukemia / small lymphocytic lymphoma (CLL / SLL), mantle cell lymphoma (MCL),...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61K9/20A61K9/28
CPCA61K31/519A61K9/2018A61K9/2866A61K9/2009A61K9/2013A61K9/2054A61K9/2806
Inventor QIU, GANGSHEN, YIWEIFAN, WENYUANXU, SHUOLV, HUIRUBIAN, JIALINDU, ZHENGMING
Owner BEIGENE SWITZERLAND GMBH
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