Application of triptolide and triptolide derivative to preparation of medicine for treating and/or preventing lung injury diseases

A technology for triptolide and lung injury, which is applied to the application field of triptolide and its derivatives in the preparation of medicines for treating and/or preventing lung injury diseases, and can solve the problem that triptolide and triptolide have not yet been seen. Problems such as terpenoids

Inactive Publication Date: 2017-08-01
王晓辉
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there are no reports of triptolide a

Method used

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  • Application of triptolide and triptolide derivative to preparation of medicine for treating and/or preventing lung injury diseases
  • Application of triptolide and triptolide derivative to preparation of medicine for treating and/or preventing lung injury diseases
  • Application of triptolide and triptolide derivative to preparation of medicine for treating and/or preventing lung injury diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0125] Preparation of Triptolide Oral Tablets: Triptolide Oral Tablets use β-cyclodextrin as an auxiliary material, which can reduce the stimulating effect of Triptolide on the gastrointestinal tract. The specific preparation method is: firstly, triptolide Dissolve the powder in ethanol to form a 100μM (36000μg / L) solution, mix β-cyclodextrin and triptolide at a mass ratio of 10:1-1000:1, stir thoroughly and then treat with ultrasonic waves (ultrasonic frequency 40000Hz) for 10 -30 minutes to prepare the triptolide β-cyclodextrin inclusion compound, dry it and make it into a tablet coated with sugar coating to make a finished medicine. Each tablet contains 40 μg of triptolide, which is divided into three doses at a dose of 0.5-10 μg / kg / day.

Embodiment 2

[0127] Inhalants through the respiratory tract (through the oral intake tube) inhalation route: triptolide is insoluble in water, in order to improve water solubility, try to disperse triptolide molecules, first dissolve triptolide powder in DMSO to 100μM (36mg / L) solution, add chitosan by weight / volume ratio and make concentration 0.6% (w / v) solution, after this solution is filtered through 0.8 μm microporous membrane, spray drier prepares microparticle, parameter setting is as follows: Nozzle diameter 0.5mm, inlet temperature 110°C, air velocity 0.7m 3 min -1 , atomization pressure 200kpa. When using nebulization or powder spray, daily inhalation of 0.01-2ug / kg body weight / day triptolide equivalent medicine, three times a day.

Embodiment 3

[0129] Oral solution: first dissolve triptolide powder in ethanol to form a 100μM (36000μg / L) solution, heat and mix until completely dissolved, slowly add 5 times the volume of water, keep the water temperature at 80°C, add appropriate amount of cyclamate and antiseptic After mixing, let it cool and stand for 24 hours, then remove the ethanol by suction filtration until the concentration is less than 0.5% (v / v). During this process, gradually add warm water at 80°C to supplement the lost volume, and pack it into 10ml graduated glass bottles , each bottle contains triptolide 60ug, 0.22um membrane filter sterilization, sterile seal. Take it three times according to the amount of 0.5-10μg / kg / day.

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Abstract

The invention provides a novel purpose of triptolide and a triptolide derivative. The triptolide can obviously inhibit the GFP fluorescent protein and P24 antigen rise effect in a phorbol ester activated lymphocyte model. When the concentration of the lymphocyte concentration is higher, the GFP positive cell percentage and the P24 antigen concentration are lower; the negative dosage-effect relationship exists. Even when the concentration of the methylprednisolone is as high as 400 uM, the inhibition effect cannot reach the inhibition effect of the triptolide with the concentration being 0.02 uM; the cell apoptosis proportion obviously exceeds the triptolide with the concentration being 0.02 uM. According to the principle, the triptolide inhibits the G0/G1 period cell proportion rise and S period cell proportion descending due to PMA; the cell period is promoted to be stopped in the unactivated state; the triptolide achieves the effect of inhibiting the lymphocyte cell proliferation and activation through regulating the cell period; meanwhile, the effect of inhibiting the virus replication is also achieved. The triptolide and the triptolide derivative can replace glucocorticoid analogues or can be combined with the glucocorticoid analogues to be used, and are used for treating and/or preventing lung injury diseases.

Description

technical field [0001] The present invention relates to a new application of triptolide and its derivatives, in particular to the application of triptolide and its derivatives in the preparation of medicines for treating and / or preventing lung injury diseases. Background technique [0002] Acute respiratory distress syndrome (ARDS) is a clinically severe disease. The etiology of ARDS is diverse, including direct causes such as aspiration and severe lung infection, and indirect causes such as severe trauma, disseminated intravascular coagulation, and shock. The specific pathogenesis of ARDS is not yet fully understood. It is generally accepted that pathogenic microorganisms and other damage factors destroy the tissues and cells of the respiratory system, and the excessive activation of lymphocytes leads to the imbalance of pro-inflammatory / anti-inflammatory responses. The excessive release of inflammatory factors leads to pulmonary capillary damage. cause oxygenation dysfunct...

Claims

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Application Information

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IPC IPC(8): A61K31/585A61K31/573A61P11/00A61P31/12
CPCA61K31/573A61K31/585A61K2300/00
Inventor 王晓辉
Owner 王晓辉
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