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Drug composition for curing tumour diseases

A composition and drug technology, applied in the direction of drug combination, antineoplastic drugs, pharmaceutical formulations, etc., can solve the problems of poor selectivity, strong toxic and side effects, and easy drug resistance

Active Publication Date: 2013-06-05
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For a long time, the commonly used cancer chemotherapy drugs in clinical practice are mainly cytotoxic drugs, which have disadvantages such as poor selectivity, strong toxic and side effects, and easy drug resistance.

Method used

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  • Drug composition for curing tumour diseases
  • Drug composition for curing tumour diseases
  • Drug composition for curing tumour diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Embodiment 1, the preparation of compound A mesylate

[0049] In a 5L reaction flask, put 170g (0.428mol) of compound A, 42.5g (0.442mol) of methanesulfonic acid, and 2.55L of 95% isopropanol aqueous solution, stir and heat under nitrogen protection and light-shielding conditions until completely dissolved, to obtain light The yellow transparent solution was filtered while it was hot, cooled and crystallized to room temperature, then filtered, washed with isopropanol, and dried in vacuum to obtain 180.2 g (0.365 mol) of white needle-like crystals, with a yield of 85.4%.

[0050] In a 5L reaction flask, put 180.2g of compound A, 2.52L of 95% isopropanol aqueous solution, stir and heat until completely dissolved under nitrogen protection and dark conditions, filter while hot, and cool the filtrate to room temperature for crystallization, filter, isopropanol Wash and dry in vacuo to obtain 161.5 g of white needle-like crystals, with a yield of 89.6%. Melting range: 193.5~...

Embodiment 2

[0051] Embodiment 2, compound A maleate and erlotinib hydrochloride compound tablet

[0052] Prescription Each tablet contains:

[0053]

[0054] Preparation method: Mix compound A maleate, erlotinib hydrochloride and microcrystalline cellulose, and wet granulate with 2% starch slurry. Dry, add magnesium stearate, mix well and press into tablets.

Embodiment 3

[0055] Embodiment 3, Compound A mesylate and erlotinib hydrochloride compound tablet

[0056] Prescription Each tablet contains:

[0057]

[0058] Preparation method: Mix compound A mesylate, erlotinib hydrochloride and microcrystalline cellulose, and wet granulate with 2% starch slurry. Dry, add magnesium stearate, mix well and press into tablets.

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PUM

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Abstract

The invention discloses a drug composition for curing tumour diseases, which comprises fixed dose of N-(4-(1-cyanocyclopentyl) phenyl)-2-(4-picolyl) amino-3-pyridinecarboxamide or pharmaceutically acceptable salt of the N-(4-(1-cyanocyclopentyl) phenyl)-2-(4-picolyl) amino-3-pyridinecarboxamide and erlotinib or pharmaceutically acceptable salt of the erlotinib or comprises fixed dose of N-(4-(1-cyanocyclopentyl) phenyl)-2-(4-picolyl) amino-3-pyridinecarboxamide or pharmaceutically acceptable salt of the N-(4-(1-cyanocyclopentyl) phenyl)-2-(4-picolyl) amino-3-pyridinecarboxamide and gefitinib or pharmaceutically acceptable salt of the gefitinib. A method for preparing the drug composition and an application of the drug composition in preparing drugs for curing tumour diseases are further provided.

Description

[0001] This application is a divisional application of the Chinese patent application with the application number 200910209164.4, the application date is October 28, 2009, and the invention title is "a pharmaceutical composition for treating tumor diseases". technical field [0002] The invention relates to a pharmaceutical composition for treating tumor diseases, especially containing N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl)amino-3-pyridinecarboxamide or its Pharmaceutically acceptable salts and erlotinib or pharmaceutically acceptable salts thereof or containing N-[4-(1-cyanocyclopentyl)phenyl]-2-(4-pyridylmethyl)amino- A pharmaceutical composition of a fixed dose combination of 3-pyridinecarboxamide or a pharmaceutically acceptable salt thereof and gefitinib or a pharmaceutically acceptable salt thereof, a method for preparing the pharmaceutical composition and the pharmaceutical composition in Use in the preparation of medicines for treating tumor diseases. B...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/5377A61P35/00A61K31/444
Inventor 孙飘扬袁开红
Owner JIANGSU HENGRUI MEDICINE CO LTD
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