Application of eutectic compound composed of proton pump inhibitor and hydroxymethylglutaryl coenzyme A reductase inhibitor in preparation of antitumor drug

A technology of hydroxymethylglutaryl coenzyme and proton pump inhibitor, which is applied in the field of preparation of antitumor drugs

Inactive Publication Date: 2019-10-15
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 anti-tumor effects in the prior art

Method used

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  • Application of eutectic compound composed of proton pump inhibitor and hydroxymethylglutaryl coenzyme A reductase inhibitor in preparation of antitumor drug
  • Application of eutectic compound composed of proton pump inhibitor and hydroxymethylglutaryl coenzyme A reductase inhibitor in preparation of antitumor drug
  • Application of eutectic compound composed of proton pump inhibitor and hydroxymethylglutaryl coenzyme A reductase inhibitor in preparation of antitumor drug

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Experimental program
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Effect test

preparation example Construction

[0143] 1 Preparation of eutectic composite

[0144] 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).

[0145] 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.

[0146] 2 Structure confirmation and characterization of the eutectic complex

[0147] 2.1 Determination of eutectic formation and preliminary detection of purity

[0148] A single eutectic complex was considered to have formed if the milled product had a melting range below 2°C.

[0149] 2.2 Determination of the molar ratio of proton pump inhibitor...

Embodiment 1

[0158] Example 1. Preparation of Omeprazole·atorvastatin co-crystal complex

[0159] 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

[0160] Example 2. Preparation of Omeprazole·atorvastatin co-crystal complex

[0161] 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 application of a eutectic compound composed of a proton pump inhibitor and a hydroxymethylglutaryl coenzyme A reductase inhibitor in preparation of an antitumor drug. The compound is characterized in that: the proton pump inhibitor is selected from one of omeprazole, esmeprazole, pantoprazole, rabeprazole and lansoprazole; and the hydroxymethylglutaryl coenzyme A reductase inhibitor is selected from one of atorvastatin, rosuvastatin, simvastatin, fluvastatin, pravastatin, lovastatin and pitavastatin or pharmaceutically acceptable salt of the atorvastatin, rosuvastatin, simvastatin, fluvastatin, pravastatin, lovastatin and pitavastatin. The antitumor drug can be used for treating one of liver cancer, lung cancer, stomach cancer, ovarian cancer, colon cancer, cervical cancer, oral squamous cell carcinoma and leukemia.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to the use of a co-crystal composed of a proton pump inhibitor and a hydroxymethylglutaryl-CoA reductase inhibitor in the preparation of antitumor drugs. Background technique [0002] Tumor is a major disease that seriously threatens human health, and the existing anti-tumor drugs have many shortcomings in terms of effectiveness and / or safety. [0003] Hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase inhibitors represented by atorvastatin are commonly used blood lipid regulating drugs in clinical practice. In recent years, the antitumor activity of these drugs has been frequently reported. For example, Ma Q et al. reported (Biomed Res Int.2019Mar 18; 2019:3235021.doi:10.1155 / 2019 / 3235021.eCollection2019.) Atorvastatin can down-regulate the PTEN / AKT pathway by promoting RhoB, and then inhibit the mammary gland Proliferation of cancer cells. Bai F et al. reported (Ag...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4439A61K31/40A61K31/505A61K31/366A61K31/405A61K31/22A61K31/47A61K31/4709A61P35/00
CPCA61K31/22A61K31/366A61K31/40A61K31/405A61K31/4439A61K31/47A61K31/4709A61K31/505A61P35/00A61K2300/00
Inventor 向飞曹新欣
Owner 黄泳华
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