Ibrutinib preparation and application thereof

A technology of ibrutinib and its use, which is applied in the field of ibrutinib for the preparation of drugs, and can solve problems such as poor prognosis

Inactive Publication Date: 2016-08-31
FOSHAN TENGRUI MEDICINE TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Mantle cell lymphoma is derived from CD5-positive small B cells in the immature germinal center of the lymphoid follicle mantle area. It has all the malignant characteristics of indolent lymphoma and aggressive lymphoma. Extensive extranodal infiltration, insensitive to traditional chemotherapy and radiotherapy, poor prognosis

Method used

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  • Ibrutinib preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Prepare 50 mg ibrutinib capsules by the above method

[0022]

Embodiment 2

[0024] Prepare 100 mg ibrutinib capsules by the above method

[0025] Element

Embodiment 3

[0027] Prepare 140 mg ibrutinib capsules by the above method

[0028] Element

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PUM

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Abstract

The invention discloses an ibrutinib preparation and application thereof. The ibrutinib preparation is prepared from ibrutinib, lactose, microcrystalline cellulose and a pharmaceutically-acceptable carrier, and the ibrutinib preparation with the good flowability, stability and dissolution rate can be obtained, so that the ibrutinib preparation is suitable for large industrial production. The ibrutinib preparation is used for a medicine composition for treating patients suffering from MCL and CLL, the compatibility is reasonable, medicine can be rapidly released, and the good treatment effect on diseases can be generated.

Description

technical field [0001] The invention relates to the use of ibrutinib for preparing medicine, especially for preparing tablets and capsules suitable for oral administration. [0002] Ibrutinib, molecular formula: C25H24N6O2, molecular weight: 440.5 Chemical name: 1-[(3R)-3-[4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[ 3,4-d]pyrimidin-1-yl]-1-piperidinyl]-2-propen-1-one. [0003] It is a three-class new drug for the treatment of patients with mantle cell lymphoma (MCL) and chronic lymphocytic leukemia (CLL), and is currently undergoing preclinical research. Background technique [0004] Ibrutinib is a small molecule BTK inhibitor that can covalently bind to cysteine ​​residues in the active center of BTK, thereby inhibiting its activity. The full name of BTK is Bruton'styrosinekinase, which transmits signals in the BCR signaling pathway and cytokine receptor signaling pathway, and mediates the migration, chemotaxis and adhesion of B cells. Preclinical studies have shown that ib...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61K9/48A61K9/20A61K47/38A61P35/00A61P35/02
CPCA61K31/519A61K9/2054A61K9/4866
Inventor 王雪峰韩亮
Owner FOSHAN TENGRUI MEDICINE TECH CO LTD
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