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Ethanesulfonic acid nintedanib preparation and application thereof

A technology of nintedanib ethanesulfonate and its application, which is applied in the directions of pill delivery, medical preparations without active ingredients, and medical preparations containing active ingredients, etc.

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

There is currently no preventive method or internationally recognized curative treatment other than lung transplantation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] 50 mg of nintedanib ethanesulfonate capsules were prepared by the above method

[0019] Element

Embodiment 2

[0021] 100 mg of nintedanib ethanesulfonate capsules were prepared by the above method

[0022] Element

Embodiment 3

[0024] 150 mg of nintedanib ethanesulfonate capsules were prepared by the above method

[0025] Element

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PUM

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Abstract

The invention discloses an ethanesulfonic acid nintedanib preparation and application thereof. The ethanesulfonic acid nintedanib preparation is prepared from ethanesulfonic acid nintedanib, lactose, microcrystalline cellulose and a pharmaceutically-acceptable carrier, and the ethanesulfonic acid nintedanib preparation with the good flowability, stability and dissolution rate can be obtained, so that the ethanesulfonic acid nintedanib preparation is suitable for large industrial production. The ethanesulfonic acid nintedanib preparation is the pharmaceutical composition for treating IPF, the compatibility is reasonable, medicine can be rapidly released, and the good treatment effect on the disease can be generated.

Description

technical field [0001] The present invention relates to the use of nintedanib ethanesulfonate for preparing medicines, especially for preparing tablets and capsules suitable for oral administration. [0002] Nintedanib esylate, molecular formula: C31H33N5O4·C2H6O3S, molecular weight: 649.76 [0003] It is a third class of new drugs for the treatment of idiopathic pulmonary fibrosis (IPF) and is currently undergoing preclinical research. Background technique [0004] Nintedanib is an oral triple angiokinase inhibitor developed by Boehringer Ingelheim. In October 2014, the FDA approved OFEV® (nintedanib) for the treatment of idiopathic pulmonary fibrosis (IPF). , the first tyrosine kinase inhibitor (TKI) approved for the treatment of IPF. Nintedanib acts on growth factor receptors that have been shown to have potential effects in the pathological mechanism of pulmonary fibrosis, the most important of which are platelet-derived growth factor receptor (PDGFR), fibroblast growt...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K9/48A61K31/496A61K45/06A61K47/26A61K47/38A61K47/36A61K47/10A61K47/02A61P11/00
CPCA61K31/496A61K9/0056A61K9/2054A61K9/4866A61K45/06
Inventor 王雪峰韩亮
Owner FOSHAN TENGRUI MEDICINE TECH CO LTD
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