Llex A-cyclodextrin polymer medicine composition for preventing and curing atherosclerosis and preparation method thereof

A technology of atherosclerosis and polycyclodextrin, which is applied in the direction of drug combination, non-active ingredients of polymer compounds, pharmaceutical formulations, etc., to achieve stable structure, easy control of conditions, and improvement of pathological changes

Inactive Publication Date: 2012-12-12
YANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the great difference in the structure of different drugs, can a specific drug be included, can the water solubility be improved after inclusion, and can the inclusion compound achieve the same drug effect as the main drug? None of these could be expected; pending further research to resolve

Method used

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  • Llex A-cyclodextrin polymer medicine composition for preventing and curing atherosclerosis and preparation method thereof
  • Llex A-cyclodextrin polymer medicine composition for preventing and curing atherosclerosis and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] The synthesis of embodiment 1 polycyclodextrin

[0017] Add sodium hydroxide (20 g), cyclodextrin (25 g) and water (40 mL) into a 250 mL three-necked flask. Stir at room temperature until all the solids are dissolved, then add epichlorohydrin (1 mL), and stir at room temperature for 24 h.

[0018] After the reaction was completed, the solution was dialyzed until the pH value of the solution was neutral. The solution was rotary evaporated to a viscous state, acetone was added to precipitate a white solid, filtered, and vacuum dried at 50°C for 24 hours. Finally polycyclodextrin (15 g) was obtained.

Embodiment 2

[0019] The synthesis of embodiment 2 water-soluble Ilexin A / polycyclodextrin inclusion compound

[0020] In a 250 mL round bottom flask was added polycyclodextrin (4 g), icolin A (1 g) and water (100 mL). Stir at room temperature for 24h and let stand for 12h.

[0021] After the reaction was completed, the clathrate solution was suction-filtered to obtain a milky yellow solution. Add 100mL of acetone to the solution to precipitate the solid, filter the solid with suction, wash the filter cake with absolute ethanol, and then dry the solid under vacuum at 50°C for 24h to obtain a solid (3g), which is the water-soluble phyllin A / polycyclodextrin package compound. Its infrared spectrum is shown in figure 1 .

Embodiment 3

[0022] Example 3 Ilexin A / polycyclodextrin inclusion complex regulates the biological activity of blood lipids (see Table 1).

[0023] Table 1. Effect of Ilex A-CDP on serum lipids in mice with hyperlipidemia (x±s, n=8)

[0024]

[0025] ①Effect of Ilex A-CDP on blood lipids in hyperlipidemia model Orally administered Ilex A-CDP and IlexA respectively to interfere with ApoE - / - In the mouse model of hyperlipidemia, after detecting serum lipids, it was found that Ilex A-CDP can significantly reduce TC, TG, LDL-C, increase HDL-C, apo A1, and down-regulate apo B in a dose-dependent manner, and The effect is better than the main drug Ilex A.

[0026] ②Effect of Ilex A-CDP on atherosclerosis coefficient and cardiovascular disease risk coefficient

[0027] Serum lipids were detected in hyperlipidemia model mice, and AS coefficient (AI) and cardiovascular disease risk factor (CRF) were calculated. It was found that IlexA-CDP could significantly reduce AI and increase CRF, and th...

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Abstract

The invention provides a novel llex A-cyclodextrin polymer (llex A-CDP) medicine composition for preventing and curing atherosclerosis (AS) and in particular relates to a preparation method of the novel water-soluble llex A-CDP medicine composition which takes CDP as the host molecule and llex A as the guest molecule. The invention obviously enhance the water-solubility of llex A and has regulating effect for dyslipidemia related to AS and inbibitional effect for inflammatory cell factor in vessel atheromatous plaque. The preparation method comprises the following steps: cyclodextrin polymer is taken as the raw material and is crosslinked with epoxy chloropropane under the condition of strong basicity to generate cyclodextrin polymer; the cyclodextrin polymer is taken as the host molecule, the llex A is taken as the guest molecule and water is taken as the reaction solvent to prepare the water-soluble llex A-CDP medicine composition by supermolecular reaction.

Description

technical field [0001] The invention belongs to the preparation of water-soluble organic materials in the field of supramolecular technology, and is specially designed to involve a new type of water-soluble hollylicin A / polycyclodextrin inclusion compound with polycyclodextrin inclusion compound as the main molecule and hollylicin A as the guest molecule (IlexA-CDP) preparation method and its anti-atherosclerosis application, the IlexA-CDP can prevent atherosclerosis (AS) by regulating blood lipids and inhibiting the production of inflammatory cytokines to prevent atherosclerotic plaque deposition. Background technique [0002] The mechanism of inflammatory immunity and oxidative damage in AS is considered to be a state of high oxidative stress, which is characterized by lipid deposition and lipoprotein oxidation in the vessel wall, and low-density lipoprotein (LDL) is oxidized to form oxidized low-density lipoprotein (ox- LDL), the phagocytosis of ox-LDL by macrophage scave...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/56A61P9/10A61K47/40
Inventor 孙云刁国旺王强刘畅张旺
Owner YANGZHOU UNIV
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