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Preparation and application of flavonols as brain-targeted synergists

A flavonol and brain technology, applied in the field of new pharmaceutical compositions, to achieve the effects of low production cost, wide sources, and easy and wide use

Active Publication Date: 2019-06-11
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For example, ginsenoside extract and polygoni multiflorum stilbene glycoside extract are important natural medicines for the treatment of brain diseases, but their active ingredients ginsenoside Rb1, Rd, Re, Rg1, stilbene glycoside, resveratrol, and chemical Drugs such as levodopa, edaravone, vinpocetine, nicergoline, citicoline, oxiracetam and other ingredients are not easy to enter the brain tissue through the blood-brain barrier to play a role

Method used

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  • Preparation and application of flavonols as brain-targeted synergists
  • Preparation and application of flavonols as brain-targeted synergists
  • Preparation and application of flavonols as brain-targeted synergists

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Flavonol kaempferol (content ≥ 99.0%) 50, 100g.

[0043] Active ingredients of traditional Chinese medicine: ginsenoside Rb1 (referred to as Rb1, content ≥ 95%) 200g;

[0044] Weigh the above-mentioned various extracts in the prescribed amount, and mix them uniformly according to the method of equal increase, and the obtained mixtures are recorded as LXN1-1 and LXN1-2.

[0045] Drug efficacy experiment:

[0046] Treatment group: LXN1-1 and LXN1-2 were made into a suspension, administered to SD rats by intragastric administration, and administered to 5 rats at a dose of 125 / 150 mg / kg (equivalent to ginsenoside Rb1100 mg / kg) in a volume of 20 ml / kg;

[0047] Control group: another ginsenoside Rg1 extract was taken to make a suspension, administered to SD rats by intragastric administration, and administered to 5 rats according to the dose of ginsenoside Rb1100mg / kg, 20ml / kg volume;

[0048] After 0.5 hr of administration, the blood was taken, and the rats were sacrifice...

Embodiment 2

[0055] Rutin (content ≥ 99.0%) 80, 100g.

[0056] Active ingredients of traditional Chinese medicine: ginsenoside Rg1 (referred to as Rg1, content ≥ 95%) 200g;

[0057] Weigh the above-mentioned various extracts in the prescribed amount, and mix them uniformly according to the method of equal increase, and the obtained mixtures are recorded as LXN11-1 and LXN11-2.

[0058] Drug efficacy experiment:

[0059] Treatment group: LXN11-1 and LXN11-2 were made into suspension, and SD rats were given 140 / 150mg / kg dose (equivalent to ginsenoside Rg1100mg / kg) by intragastric administration of 20ml / kg volume, 5 mice in each group ;

[0060] Control group: another ginsenoside Rg1 extract was taken to make a suspension, and administered to SD rats by intragastric administration, at a dose of 100mg / kg, and a volume of 20ml / kg, for 5 rats;

[0061] After 0.5 hr of administration, the blood was taken, and the rats were sacrificed acutely, and the brain tissue was taken to make a brain homo...

Embodiment 3

[0068] Troxerutin (content ≥95.0%) 50 or 100g;

[0069] Active ingredient of traditional Chinese medicine: 200g of Hewu extract (stilbene glycoside, EB, content ≥ 50%).

[0070] Weigh the above-mentioned various extracts in the prescription amount, mix them uniformly according to the method of equal increase, and record the obtained mixtures as LXN2-1 and LXN2-2.

[0071] Drug efficacy experiment:

[0072] Treatment group: LXN2-1 and LXN2-2 were made into a suspension, administered to SD rats by intragastric administration, and administered to 5 rats at a dose of 100 mg / kg of stilbene glycosides in a volume of 20 ml / kg;

[0073] Control group: another stilbene glycoside extract was taken to make a suspension, administered to SD rats by intragastric administration, and dosed to 5 rats at a dose of 100 mg / kg stilbene glycoside and a volume of 20 ml / kg;

[0074] After administration for 0.5 hr, the blood was collected, the rats were sacrificed acutely, and the brain tissue was ...

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Abstract

The invention discloses the preparation and application of flavonol as a brain targeting synergist. The inventors have found in long-term experimental research that some flavonol compounds, especially kaempferol, rutin, troxerutin, myricetin, hesperidin, and their hydroxy derivatives, especially their glycosides, esters, ethers Derivatives, can be very good to promote the therapeutic drug molecules ginsenoside, stilbene glycoside, resveratrol, levodopa, edaravone, vinpocetine, nicergoline, cytosine When choline, oxiracetam, etc. enter the brain tissue, the concentration of the drug in the brain tissue is greatly increased without increasing its blood concentration, and the curative effect of the drug is effectively improved.

Description

technical field [0001] The present invention relates to a new application of a compound and a new pharmaceutical composition based on the application. Background technique [0002] The brain is the center of life, and its complex nervous system structure and function has become the most valuable research topic in the history of human science, and has attracted more and more attention from scientists around the world. [0003] Cerebral blood flow is the fastest, but many drugs enter the brain tissue much slower than other tissues after systemic administration, thus forming the concept of blood-brain barrier. The blood-brain barrier refers to the barrier between blood-brain interstitial fluid and blood-cerebrospinal fluid, which consists of blood-brain barrier (BBB), cerebro-spinal fluid-brain barrier and blood-cerebrospinal Barrier (blood-cerebro-spinal fluid barrier) consists of three barriers. The function of the blood-brain barrier is to selectively prevent certain subst...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/7048A61K31/352A61P9/10A61P25/28A61P25/16A61P25/00A61K31/4015A61K31/4152A61K31/7068A61K31/704A61K31/7034
CPCA61K31/05A61K31/198A61K31/352A61K31/4015A61K31/4152A61K31/4375A61K31/48A61K31/7028A61K31/7034A61K31/704A61K31/7048A61K31/7068A61K2300/00A61K45/06A61K31/475A61K36/258A61K36/704A61P25/00A61P25/16A61P25/28A61P9/10
Inventor 贝伟剑郭姣
Owner GUANGDONG PHARMA UNIV
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