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Pharmaceutical composition for treating tumor diseases

A composition and drug technology, which can be used in drug combinations, antitumor drugs, pharmaceutical formulations, etc., and can solve problems such as poor selectivity, strong toxic and side effects, and easy generation of drug resistance.

Active Publication Date: 2011-05-11
JIANGSU HENGRUI MEDICINE CO LTD +1
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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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  • Pharmaceutical composition for treating tumor diseases
  • Pharmaceutical composition for treating tumor diseases
  • Pharmaceutical composition for treating tumor diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Embodiment 1, the preparation of compound A mesylate

[0048] 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%.

[0049] 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

[0050] Embodiment 2, compound A maleate and erlotinib hydrochloride compound tablet

[0051] Prescription Each tablet contains:

[0052]

[0053] 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

[0054] Embodiment 3, Compound A mesylate and erlotinib hydrochloride compound tablet

[0055] Prescription Each tablet contains:

[0056]

[0057] 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 pharmaceutical composition for treating tumor diseases, a preparation method of the pharmaceutical composition and application of the pharmaceutical composition in preparing the medicines for treating tumor diseases, wherein the pharmaceutical composition consists, in a fixed dosage, of N-[4-(1-cyan cyclopentyl)phenyl]-2-(4-picolyl) amidogen-3-pyridinecarboxamide or pharmaceutically acceptable salts thereof and angiostatin or pharmaceutically acceptable salts thereof, or N-[4-(1-cyan cyclopentyl)phenyl]-2-(4-picolyl) amidogen-3-pyridinecarboxamide or pharmaceutically acceptable salts thereof and gefitinib or pharmaceutically acceptable salts thereof.

Description

technical field [0001] 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. Background technique [0002] Cancer is a common and frequently-occurring disease that seriously endangers human health. For a long time, the commonly used cancer chemotherapy drugs in clinical practice are mainly cytotoxic drugs, which have disadvantages such...

Claims

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Application Information

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IPC IPC(8): A61K31/517A61K31/455A61K31/5377A61P35/00
CPCA61K9/2054A61K31/444A61K31/517A61K31/5377A61P35/00A61K2300/00
Inventor 孙飘扬袁开红
Owner JIANGSU HENGRUI MEDICINE CO LTD
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