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A method for improving the water solubility of 7,8-dihydroxyflavone based on raft polymerization

A dihydroxyflavone and water-soluble technology, which is applied in the field of improving the water solubility of 7,8-dihydroxyflavone based on RAFT polymerization method, can solve the complex and changeable reaction mechanism of anti-Parkinson (PD) drugs, fluctuating symptoms, and aggravation Symptoms and other problems of patients, to achieve the effect of easy molecular weight, obvious effect, and improved water solubility

Inactive Publication Date: 2017-07-04
江苏世丰企业管理咨询有限公司
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  • Summary
  • Abstract
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  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the understanding of Parkinson's disease (PD) is gradually deepening with the continuous research of researchers, the mystery of Parkinson's pathology has not yet been solved, and the response mechanism of anti-Parkinson's (PD) drugs is even more important. Complex and changeable, so even though the current methods and paths to treat Parkinson's (PD) disease are springing up like mushrooms after a spring rain, the treatment of PD is still based on drug therapy
At present, the principle of drug treatment is mainly to replenish the missing dopamine in the human body in time. The drugs on the market mainly include anticholinergics, dopas (levodopa), dopamine receptor agonists and agonists, etc. These drugs Although some nerves can be protected and repaired for a certain period of time, Parkinson's symptoms can be alleviated and their quality of life can be improved, but if these drugs are taken for a long time, most patients may experience weakened therapeutic effects, fluctuating symptoms, Side effects such as mental abnormalities and body movement disorders, and even the metabolites produced by some drugs will have toxic reactions with certain substances in cells, which aggravates the patient's symptoms

Method used

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  • A method for improving the water solubility of 7,8-dihydroxyflavone based on raft polymerization
  • A method for improving the water solubility of 7,8-dihydroxyflavone based on raft polymerization
  • A method for improving the water solubility of 7,8-dihydroxyflavone based on raft polymerization

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Experimental program
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Effect test

Embodiment 1

[0033] Embodiment 1: The mensuration of 7,8-DHF solubility

[0034] In this embodiment, 7 after modification, 8-DHF (7 samples are obtained by controlling the ratio of RAFT reagent and monomer respectively, sample 1 is pure 7, 8-DHF; sample 2 ratio is 1:10; sample 3 ratio is 1:20; the ratio of sample 4 is 1:30; the ratio of sample 5 is 1:40; the ratio of sample 6 is 1:50; the ratio of sample 7 is 1:60). figure 2 shown, from figure 2 It can be seen that the solubility of 7,8-DHF is about 10044 μmol / L. Compared with the 7,8-DHF with a solubility of 126.8 μmol / L before modification, the modified 7,8-DHF (when the degree of polymerization is 60 ) Solubility increased by 78 times.

Embodiment 2

[0035] Embodiment 2: the mensuration of drug efficacy after modification

[0036] In this embodiment, the modified 7,8-DHF drug efficacy is measured, and the results are as follows: image 3 shown, from image 3 (a) It can be seen that the vasodilation of the samples of these 7 degrees of polymerization are 88.6±6.2%, 84.3±4.3%, 80.2±6.2%, 79.6±3.3%, 77.2±4.9%, 75.9±3.8% and 70.2±1.8%; image 3 (b) shows that the drug effect of modified 7,8-DHF decreases with the increase of degree of polymerization. When the degree of polymerization is 60, the drug effect of modified 7,8-DHF is the original drug level 79.2%.

Embodiment 3

[0037] Example 3: Determination of cytotoxicity after modification (DT is the cytotoxicity grade)

[0038] The present embodiment measures the toxicity of 7,8-DHF drug to cells after the modification, and the results are shown in Table 1. From Table 1, it can be obtained that the drug after modification has a toxicity level of one to cells, which is equal to the toxicity of the original drug. At the same level, the drug efficacy is only slightly reduced, and the toxicity of the drug is at the same level as before.

[0039] Table 1:

[0040]

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Abstract

The invention belongs to the technical fields of RAFT polymerization, PEG-A monomer grafting and drug toxicity testing, and relates to a method for improving the water solubility of 7,8-dihydroxyflavanone based on a RAFT polymerization method. The method comprises the following steps: first performing chlorination reaction on a RAFT reagent, then grafting the RFAT reagent to the 7,8-dihydroxyflavanone, and finally performing RAFT polymerization reaction to graft PEG-A to the 7,8-dihydroxyflavanone. A process is simple and convenient to operate, the improvement effect on the water solubility of the 7,8-dihydroxyflavanone is obvious, the molecular weight is easy to control, the cost and the toxicity are low, and the polymerization degree can be accurately controlled by RAFT polymerization so as to synthesize 7,8-dihydroxyflavanone with different molecular weights and different polymerization degrees.

Description

[0001] Technical field: [0002] The invention belongs to the technical fields of RAFT polymerization, PEG-A monomer grafting and drug toxicity testing, and relates to a method for improving the water solubility of 7,8-dihydroxyflavone based on a RAFT polymerization method, in which PEG-A is grafted to A method to increase the water solubility of the drug on the drug. [0003] Background technique: [0004] 7,8-dihydroxyflavone (7,8-DHF) is a drug that can imitate the effect of brain-derived neurotrophic factor (BDNF). It can enter the brain cell tissue through the blood-brain barrier and protect the nervous system. Therefore, it can be used to improve a variety of diseases with abnormal brain function, such as Parkinson's disease. However, due to the poor water solubility of 7,8-dihydroxyflavone, which affects its drug action time and effect, it is considered to increase its water solubility by modifying 7,8-dihydroxyflavone, because PEG- The hydrophilic group hydroxyl on th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08F2/38C08F120/28A61K31/78A61P25/00C07D311/30
CPCA61K31/78C07D311/30C08F2/38C08F120/28
Inventor 刘敬权陈涛许元红
Owner 江苏世丰企业管理咨询有限公司
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