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Eutectic compound formed by lipase inhibitor and hydroxy methylglutaryl coenzyme A reductase inhibitor

A technology of hydroxymethylglutaryl coenzyme and lipase inhibitor, which is applied in the field of co-crystal complexes

Inactive Publication Date: 2019-10-22
黄泳华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] At present, there is no technical teaching on lipase inhibitors and hydroxymethylglutaryl-CoA reductase inhibitors forming co-crystals to produce synergistic antibacterial and antihistamine effects in the prior art

Method used

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  • Eutectic compound formed by lipase inhibitor and hydroxy methylglutaryl coenzyme A reductase inhibitor
  • Eutectic compound formed by lipase inhibitor and hydroxy methylglutaryl coenzyme A reductase inhibitor
  • Eutectic compound formed by lipase inhibitor and hydroxy methylglutaryl coenzyme A reductase inhibitor

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preparation example Construction

[0056] 1 Preparation of eutectic composite

[0057] 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).

[0058] Specifically, a certain molar ratio of the lipase inhibitor and the hydroxymethylglutaryl-CoA reductase inhibitor is placed in a ball mill, and ground at a frequency of 30-60 Hz for 15-60 minutes at room temperature. The frequency and grinding time of the ball mill were optimized and screened with the product melting distance ≤ 2°C as the standard.

[0059] 2 Structure confirmation and characterization of the eutectic complex

[0060] 2.1 Determination of eutectic formation and preliminary detection of purity

[0061] A single eutectic complex was considered to have formed if the milled product had a melting range below 2°C.

[0062] 2.2 Determination of the molar ratio of lipase inhibitor to hydroxymet...

Embodiment 1

[0070] Example 1. Preparation of orlistat·atorvastatin co-crystal complex

[0071] Take 148.719g of orlistat and 55.864g of atorvastatin, mix them thoroughly, place them in a planetary ball mill, grind them for 55min at a speed of 350r / min, and collect the product to obtain 192.915g of off-white powder with a melting point of 73.3-75.3°C . After recrystallization with ethanol, 192.306g of white crystalline powder was obtained, the melting point was 73.4-74.3°C, the R value was 2.858, and its X-ray powder diffraction pattern was as follows figure 1 shown.

Embodiment 2

[0072] Example 2. Preparation of orlistat-rosuvastatin co-crystal complex

[0073] Take 132.195g of orlistat and 64.205g of rosuvastatin, mix them thoroughly, place them in a planetary ball mill, grind them for 35min at a speed of 350r / min, and collect the product to obtain 178.411g of off-white powder with a melting point of 160.0-162.0°C . Obtain 177.975g of white crystalline powder after recrystallization with acetone, melting point is 162.9~163.9 ℃, R value is 1.932, and its X-ray powder diffraction figure is as follows figure 2 shown.

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Abstract

The invention provides a eutectic compound formed by a lipase inhibitor and a hydroxy methylglutaryl coenzyme A reductase inhibitor and composition containing the eutectic compound. The eutectic compound is characterized in that the lipase inhibitor is selected from one of orlistat and cetilistat; the hydroxy methylglutaryl coenzyme A reductase inhibitor is selected from one of atorvastatin, rosuvastatin, simvastatin, fluvastatin, pravastatin, lovastatin and pitavastatin or pharmacologically acceptable salts thereof. The eutectic compound can simultaneously have synergistic antibacterial action and synergistic histamine release inhibition function, so that the treatment effect on patients with allergic diseases caused by bacterial infection and the economic characteristics can be improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a eutectic complex composed of a lipase inhibitor and a hydroxymethylglutaryl-CoA reductase inhibitor and a composition containing the complex. Background technique [0002] An allergic reaction is also known as anaphylaxis. It is tissue damage or physiological dysfunction caused by stimulation of the body by antigenic substances (such as bacteria, viruses, parasites, pollen, etc.). An abnormal or focal immune response. The so-called hypersensitivity reaction usually refers to type I hypersensitivity reaction, that is, immediate hypersensitivity reaction. The mechanism is that after the allergen enters the allergic person's body, specific antibodies are produced, and the latter binds to the surface of mast cells, making the body in an sensitized state. When exposed to the allergen for the first time, the mast cells degranulate and release various chemical mediators...

Claims

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Application Information

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IPC IPC(8): C07D215/14C07D309/30C07C69/33C07D209/24C07D239/42C07D207/34C07D265/26C07D305/12A61K31/365A61K31/536A61K31/40A61K31/506A61K31/366A61K31/405A61K31/22A61K31/47A61K45/06A61P31/04A61P37/08
CPCA61K31/22A61K31/365A61K31/366A61K31/40A61K31/405A61K31/47A61K31/506A61K31/536A61K45/06A61P31/04A61P37/08C07B2200/13C07C69/33C07D207/34C07D209/24C07D215/14C07D239/42C07D265/26C07D305/12C07D309/30A61K2300/00Y02A50/30
Inventor 向飞张守波
Owner 黄泳华
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