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Composition containing protein kinase inhibitor and metformin

A protein kinase inhibitor, metformin technology, applied in the field of compositions containing protein kinase inhibitor and metformin

Inactive Publication Date: 2019-01-04
黄泳华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In recent years, the antibacterial activity of metformin has attracted more and more attention. However, there is no technical inspiration for the combination of protein kinase inhibitors and metformin to produce synergistic antibacterial effects.

Method used

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  • Composition containing protein kinase inhibitor and metformin
  • Composition containing protein kinase inhibitor and metformin
  • Composition containing protein kinase inhibitor and metformin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Embodiment 1 comprises the preparation of the capsule of metformin hydrochloride and nilotinib hydrochloride monohydrate (molar ratio is 0.01:1)

[0054] prescription

[0055]

[0056] Preparation

[0057] Take the prescribed amount of metformin hydrochloride, nilotinib hydrochloride monohydrate, sorbitol and sodium stearyl fumarate, fully mix, fill in capsules, and subpackage.

Embodiment 2

[0058] Embodiment 2 comprises the preparation of the tablet of metformin hydrochloride and pazopanib hydrochloride (molar ratio is 0.5:1)

[0059] prescription

[0060]

[0061]

[0062] Preparation

[0063] Get the prescribed amount of metformin hydrochloride, pazopanib hydrochloride, microcrystalline cellulose, magnesium stearate, fully mix, and compress into tablets.

Embodiment 3

[0064] Example 3 Preparation of granules comprising metformin hydrochloride and afatinib dimaleate (molar ratio of 1:1)

[0065] prescription

[0066]

[0067] Preparation

[0068] Take the prescribed amount of metformin hydrochloride, afatinib dimaleate, microcrystalline cellulose, and sodium stearyl fumarate, mix them thoroughly, and pack them separately.

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Abstract

The invention firstly provides a composition containing a protein kinase inhibitor and metformin or pharmaceutically acceptable salts thereof. The composition is characterized in that the protein kinase inhibitor is one selected from nilotinib, pazopanib, afatinib, bosutinib, crizotinib, axitinib and regorafenib or pharmaceutically acceptable salts or solvates thereof or solvates of the pharmaceutically acceptable salts thereof, and the molar ratio of the metformin to the protein kinase inhibitor is (0.01-100):1. In-vitro bacteriostatic tests find that the composition containing the metforminand the protein kinase inhibitor can achieve a synergistic bacteriostatic effect on various bacteria such as staphylococcus aureus in the molar ratio of (0.01-100):1 (at an inhibition rate of 30%, thecombined medication index CI is smaller than 1).

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a composition containing protein kinase inhibitors and metformin. Background technique [0002] Infectious diseases are a large class of diseases caused by microbial infections such as bacteria, parasites, fungi, or viruses, and can be transmitted directly or indirectly between humans through various channels. Although a variety of anti-infective drugs, including antibiotics, antivirals, antifungals, and antiparasitics, are currently available for the treatment of infectious diseases, this disease remains one of the leading causes of illness or death worldwide. In 2010, approximately 15 million people worldwide died from infectious diseases. [0003] In 2001, the first protein kinase inhibitor imatinib was launched for the treatment of leukemia, which opened the prelude to the targeted therapy of tumors. As of October 2018, the FDA has approved more than ten protei...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/155A61P31/04
CPCA61K31/155A61K45/06A61P31/04
Inventor 向飞曾佑梅张花黄泳华
Owner 黄泳华
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