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Eutectic complex composed of resveratrol and protein kinase inhibitor, and composition comprising eutectic complex

A protein kinase inhibitor, resveratrol technology, applied in the field of medicine, can solve the problem of no resveratrol and protein kinase inhibitor.

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

[0009] At present, there is no technical teaching on the formation of co-crystals between resveratrol and protein kinase inhibitors to produce synergistic antihistamine effects in the prior art

Method used

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  • Eutectic complex composed of resveratrol and protein kinase inhibitor, and composition comprising eutectic complex
  • Eutectic complex composed of resveratrol and protein kinase inhibitor, and composition comprising eutectic complex
  • Eutectic complex composed of resveratrol and protein kinase inhibitor, and composition comprising eutectic complex

Examples

Experimental program
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[0096] 1 Preparation of eutectic composite

[0097] The invention adopts the hot-melt extrusion method to prepare the resveratrol-protein kinase inhibitor eutectic complex. Specifically, resveratrol and protein kinase inhibitors in a specific molar ratio are sieved and mixed to form a physical mixture. The screw of the hot-melt extruder (ZE-16 twin-screw hot-melt extruder, ATS Industrial Systems Co., Ltd.) is divided into modules 1~6 (Zone 1~6) from left (feed port) to right, representing 6 There are three temperature zones that can be set, and the process of feeding, conveying, melting and mixing, and output is performed in sequence. The temperature value of each module is set according to the process needs. After the temperature is stable for 10 minutes, the physical mixture is slowly added to the extruder, and the extruder is extruded. The material was ground and pulverized through an 80-mesh sieve, recrystallized, dried, and stored in the dark.

[0098] In the present in...

Embodiment 1

[0119] Example 1 Preparation of resveratrol imatinib co-crystal complex

[0120] Take resveratrol 493.6g and imatinib 100g, sieve and mix, as a physical mixture. The screw of the hot-melt extruder (ZE-16 twin-screw hot-melt extruder, ATS Industrial Systems Co., Ltd.) is divided into modules 1~6 from left (feeding port) to right, Zone 1~6) represents 6 There are three adjustable temperature zones, and the processes of feeding, conveying, melting and mixing, and output are performed in sequence. The temperature of modules 1-6 is 155°C, 175°C, 195°C, 225°C, 260°C, 165.8-167.6°C in sequence, and the rotation speed is 10r / min. After the temperature stabilizes for 10min, feed at a speed of 3g / min. The extrudate was collected, ground and passed through an 80-mesh sieve to obtain 999.175 g of an off-white solid with a melting point of 180.1-181.3°C. Recrystallize with ethanol, and dry to obtain 998.725 g of white solid, melting point is 211-211.1 °C, R value is 0.319, and its X-ray ...

Embodiment 2

[0121] Example 2 Preparation of resveratrol·erlotinib co-crystal complex

[0122] Take resveratrol 393.44g and erlotinib 100g, sieve and mix, as a physical mixture. The screw of the hot-melt extruder (ZE-16 twin-screw hot-melt extruder, ATS Industrial Systems Co., Ltd.) is divided into modules 1~6 from left (feeding port) to right, Zone 1~6) represents 6 There are three adjustable temperature zones, and the processes of feeding, conveying, melting and mixing, and output are performed in sequence. The temperature of modules 1 to 6 is 125°C, 180°C, 185°C, 235°C, 260°C, 180.4 to 181.6°C in sequence, and the rotation speed is 10r / min. After the temperature stabilizes for 10min, feed at a speed of 3g / min. The extrudate was collected, ground and passed through an 81-mesh sieve to obtain 999.369 g of an off-white solid with a melting point of 190.3-191.3°C. Recrystallize with isopropanol and dry to obtain 998.677g of white solid, melting point is 163.8~164.7°C, R value is 0.513, it...

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Abstract

The invention provides a eutectic complex composed of resveratrol and a protein kinase inhibitor, and a composition comprising the eutectic complex. The eutectic complex is characterized in that the protein kinase inhibitor is selected from one of imatinib, gefitinib, erlotinib, sunitinib, sorafenib, dasatinib, lapatinib, nilotinib, pazopanib, afatinib, crizotinib, axitinib, regorafenib, ibrutinib, lenvatinib, palbociclib, osimertinib and alectinib or pharmaceutically acceptable salt thereof. The eutectic complex provided by the invention can produce synergistic effects of inhibiting histamine release.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a co-crystal complex composed of resveratrol and protein kinase inhibitors and a composition containing the co-crystal 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. , such as 5-h...

Claims

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Application Information

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IPC IPC(8): C07C39/21C07D401/04C07D239/94C07D403/06C07D213/81C07D417/12C07D405/04C07D403/12C07D405/12C07D401/14C07D401/06C07D487/04C07D215/48C07D471/04C07D403/04A61K31/506A61K31/5377A61K31/517A61K31/404A61K31/44A61K31/4545A61K31/4439A61K31/519A61K31/47A61K31/05A61P37/08
CPCA61K31/05A61K31/404A61K31/44A61K31/4439A61K31/4545A61K31/47A61K31/506A61K31/517A61K31/519A61K31/5377A61P37/08C07B2200/13C07C39/21C07D213/81C07D215/48C07D239/94C07D401/04C07D401/06C07D401/14C07D403/04C07D403/06C07D403/12C07D405/04C07D405/12C07D417/12C07D471/04C07D487/04A61K2300/00
Inventor 向飞张守波
Owner 黄泳华
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