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Application of 6-hydroxy-1-hydro-indazole in preparation of medicine for preventing and treating neurodegenerative disease

A neurodegenerative, hydroxyl-based technology that can be used in the medical field to solve problems such as uncontrollable disease progression and unstoppable neuron loss

Inactive Publication Date: 2015-04-22
王文雅
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But, likewise, since the loss of neurons cannot be prevented, the progression of the disease cannot be controlled

Method used

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  • Application of 6-hydroxy-1-hydro-indazole in preparation of medicine for preventing and treating neurodegenerative disease
  • Application of 6-hydroxy-1-hydro-indazole in preparation of medicine for preventing and treating neurodegenerative disease
  • Application of 6-hydroxy-1-hydro-indazole in preparation of medicine for preventing and treating neurodegenerative disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0098] The preparation of embodiment one injection

[0099] Take by weighing 10 grams of 6-hydroxyl-1-hydrogen-indazole, be dissolved in 1000 milliliters of water for injection, dissolve, filter with ultra-microfiltration membrane, promptly make the injection solution that concentration is 1 gram / 100 milliliters (1%), kill Bacteria, subpackage.

[0100] For patients with Parkinson's disease and senile dementia: the dosages for subcutaneous injection, intramuscular injection, and slow intravenous injection are all the same, 50-100 mg each time, 2-3 times a day.

Embodiment 2

[0101] The preparation of embodiment two tablet

[0102]

[0103]

[0104] 0.2 g of citrate was dissolved in 20 ml of 10% starch slurry. Take the proportioning amount of 6-hydroxy-1-hydro-indazole and starch, mix evenly, add an appropriate amount of 10% starch slurry containing citric acid to make a soft material, pass through a 16-mesh sieve to granulate, and dry the wet granules at 40-60°C 16-mesh sieve for granulation, adding an appropriate amount of 1% magnesium stearate and compressing to form tablets each containing 100 mg of 6-hydroxyl-1-hydrogen-indazole.

[0105] For patients with Parkinson's disease and Alzheimer's disease: take 0.5-1.0 g orally once a day, and give it in 2-4 times.

Embodiment 3

[0106] The preparation of embodiment three sustained-release capsules

[0107]

[0108] The composition and weight percentage contained in the capsule are: 6-hydroxy-1-hydro-indazole 40%, calcium hydrogen phosphate 40%, HPMC4000cp 8%, HPMC 100cp 8%, EC 100cp 2%, magnesium stearate 1%, talc Powder 1%. Its preparation method is: pass the ratio of 6-hydroxyl-1-hydrogen-indazole, calcium hydrogen phosphate, HPMC4000cp, HPMC 100cp and EC 100cp through a 60-mesh to 100-mesh sieve respectively, put it in a mixer to mix, and add a concentration of 50 %~75% ethanol is used as a wetting agent and stirred to make a soft material, passed through a 14 mesh to 20 mesh sieve to granulate, the granules are dried at 50°C to 60°C, granulated with a 14 mesh to 20 mesh sieve, and then magnesium stearate and Talc powder, mixed evenly, packed into capsules, and divided into capsules each containing 100 mg of AR-A014418.

[0109] For patients with Parkinson's disease and Alzheimer's disease: ta...

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Abstract

The invention provides an application of 6-hydroxy-1-hydro-indazole in preparation of medicine for preventing and treating neurodegenerative disease. An action mechanism of the medicine for preventing and treating neurodegenerative disease is characterized in that 6-hydroxy-1-hydro-indazole can inhibit a phosphorylation process of Tau protein, a hyperphosphorylation state of Tau can be alleviated, neuronal apoptosis can be prevented, so that a purpose for preventing and treating neurodegenerative disease can be reached. The application of 6-hydroxy-1-hydro-indazole in preparation of medicine for preventing and treating neurodegenerative disease can effectively inhibit the phosphorylation level of Tau protein and prevent neuronal apoptosis, the action target is clear, so that the therapeutic effect is definite and obvious.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to the application of 6-hydroxy-1-hydro-indazole in the preparation of drugs for preventing and treating neurodegenerative diseases. Background technique [0002] Neurodegenerative diseases refer to a series of diseases caused by the degenerative changes of neurons in the human body. They mainly occur in the elderly and greatly affect people's quality of life. Among them, Parkinson's disease (PD) and Alzheimer's disease (AD) are the two most common neurodegenerative diseases. Neuron loss due to neuron apoptosis is the main pathological feature of neurodegenerative diseases, but for a long time, due to the lack of clear drug targets, people can only use "palliative" methods to treat such diseases. Specific chemicals are taken or injected intravenously to replenish the depleted neurons in the patient's brain. For example, the signs and symptoms of PD can be relieved by drugs that i...

Claims

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Application Information

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IPC IPC(8): A61K31/416A61P25/28A61P25/16
CPCA61K31/416
Inventor 王文雅梁小凤朱雯婷
Owner 王文雅
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