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Eutectic compound with synergistic bacteriostatic effect

A complex, proton pump inhibitor technology, applied in the field of medicine

Inactive Publication Date: 2019-09-27
黄泳华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there is no technical teaching on the formation of co-crystals between proton pump inhibitors and hydroxymethylglutaryl-CoA reductase inhibitors to produce synergistic antibacterial effects in the prior art

Method used

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  • Eutectic compound with synergistic bacteriostatic effect
  • Eutectic compound with synergistic bacteriostatic effect
  • Eutectic compound with synergistic bacteriostatic effect

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0145] 1 Preparation of eutectic composite

[0146] The present invention prepares the eutectic composite described in the present invention with reference to the grinding method disclosed by Scott C. McKellar et al. (Crystal Growth & Design 2014, 14, 5, 2422-2430).

[0147] Specifically, a certain molar ratio of the proton pump inhibitor and the hydroxymethylglutaryl-CoA reductase inhibitor is placed in a ball mill, and ground at room temperature for 15-60 minutes at a frequency of 30-60 Hz. The frequency and grinding time of the ball mill were optimized and screened with the melting range of the product ≤ 2°C as the standard.

[0148] 2 Structure confirmation and characterization of the eutectic complex

[0149] 2.1 Determination of eutectic formation and preliminary detection of purity

[0150] A single eutectic complex was considered to have formed if the milled product had a melting range below 2°C.

[0151] 2.2 Determination of the molar ratio of proton pump inhibitor...

Embodiment 1

[0160] Example 1. Preparation of Omeprazole·atorvastatin co-crystal complex

[0161] Take 46.056g of omeprazole and 148.971g of atorvastatin, mix them thoroughly, place them in a planetary ball mill, grind them at a speed of 350r / min for 45min, and collect the product to obtain 183.363g of off-white powder with a melting point of 82.8-84.8°C . After recrystallization with ethanol, 182.740 g of white crystalline powder was obtained, with a melting point of 155.1-156.0° C. and an R value of 0.503.

Embodiment 2

[0162] Example 2. Preparation of Omeprazole·atorvastatin co-crystal complex

[0163] Take 92.112g of omeprazole and 74.485g of atorvastatin, mix them thoroughly, place them in a planetary ball mill, grind them for 30min at a speed of 300r / min, and collect the product to obtain 161.854g of off-white powder with a melting point of 109.2-111.1°C . After recrystallization with acetone, 161.362g of white crystalline powder was obtained, with a melting point of 110.6-111.5°C and an R value of 2.089.

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Abstract

The invention provides an eutectic compound comprising a proton pump inhibitor and a hydroxy-3-methylglutaryl coa reductase inhibitor. The eutectic compound is characterized in that the proton pump inhibitor is selected from one in omeprazole, esomeprazole, pantoprazole, rabeprazole and lansoprazole; the hydroxy-3-methylglutaryl coa reductase inhibitor is selected on or pharmacologically acceptable salt thereof in atorvastatin, rosuvastatin, simvastatin, fluvastatin, pravastatin, lovastatin and pitavastatin. The eutectic compound can produce a synergistic bacteriostatic effect.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a eutectic compound capable of producing synergistic antibacterial effects simultaneously. Background technique [0002] Bacterial infectious diseases are a class of diseases that seriously threaten human health and quality of life. With the increasing resistance to existing antimicrobial drugs, it is particularly urgent to develop new antibacterial drugs. [0003] Hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitors represented by atorvastatin are commonly used blood lipid regulating drugs in clinical practice, and the antibacterial activity of these drugs has been frequently reported in recent years. Studies by JerwoodS et al. (JAntimicrobChemother.2008Feb; 61(2):362-4) show that both simvastatin and fluvastatin have certain antibacterial effects, and the average MICs of the former for MSSA and MRSA are 29.2 and 74.9 respectively. mg / L, while the antib...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/06A61K31/4439A61K31/40A61K31/505A61K31/366A61K31/47A61K31/405A61K31/22A61P31/04A61P37/08C07D401/12C07D207/34C07D239/42C07D309/30C07D209/24C07D215/14C07C69/33
CPCA61K31/22A61K31/366A61K31/40A61K31/405A61K31/4439A61K31/47A61K31/505A61K45/06A61P31/04A61P37/08C07B2200/13C07D207/34C07D209/24C07D215/14C07D239/42C07D309/30C07D401/12A61K2300/00Y02A50/30
Inventor 向飞曹新欣
Owner 黄泳华
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