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Application of tribaquidone sulfonate and its geniposide composition in the preparation of medicines

A technology of sulfonate and sodium sulfonate, which is applied in drug combinations, active ingredients of heterocyclic compounds, and pharmaceutical formulations, can solve the problems of rapid elimination, low bioavailability, and poor curative effect. To achieve the effect of exact curative effect and less side effects

Active Publication Date: 2019-10-15
张忠立
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The components of tribaturon lignans have the pharmacological activity of protecting the liver or treating senile dementia or Alzheimer's disease, but pharmacokinetic experimental studies have found that they are poorly absorbed in the body and eliminated quickly, mainly Because the water-solubility and fat-solubility of tribaurone are very poor
[0003] Geniposide (or geniposide) iridoids have the pharmacological activity of protecting or protecting the liver or treating senile dementia or Alzheimer's disease, but studies have reported that it can cause severe liver damage when applied in large doses , poor efficacy when applied in small doses
The main reason is that geniposide (also known as geniposide) has high polarity, good water solubility, and poor fat solubility. Oral administration has enterohepatic circulation, and its bioavailability is extremely low, less than 10%.
The above-mentioned studies have not been reported yet. We have firstly found that tribacuadone sodium sulfonate or the composition of tribacudenone and geniposide have effects on alcoholic hepatitis or liver injury, non-alcoholic hepatitis or liver damage by overall pharmacological experimental research. Injury, alcoholic fatty liver or liver damage, non-alcoholic fatty liver or liver damage, liver damage liver fibrosis, hepatitis in cirrhosis or liver damage has a significant therapeutic effect

Method used

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  • Application of tribaquidone sulfonate and its geniposide composition in the preparation of medicines
  • Application of tribaquidone sulfonate and its geniposide composition in the preparation of medicines
  • Application of tribaquidone sulfonate and its geniposide composition in the preparation of medicines

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Experimental program
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Effect test

Embodiment 1

[0036] Tribaumyrone lignans have hepatoprotective or hepatoprotective pharmacological activities, but pharmacokinetic experimental studies have found that they are poorly absorbed in vivo and eliminated quickly, mainly due to the water solubility and lipid Solubility is very poor. The inventors of the present invention modified its structure to prepare tribacudone sulfonate, especially sodium tribacudone sulfonate, which has increased water solubility. The above studies have not been reported yet. Through the overall pharmacological experimental research, we first found that tribagudone sodium has the therapeutic effect of protecting the liver or protecting the liver, and the curative effect is better than that of tribagudone.

[0037] Geniposide (or geniposide) iridoids have hepatoprotective or hepatoprotective pharmacological activities, but studies have reported that large doses of it can cause severe liver damage, and low doses have poor efficacy. The main reason is that ...

Embodiment 2

[0075] Tribaquidone lignans have pharmacological activity in the treatment of senile dementia drugs or Alzheimer's disease, but pharmacokinetic experimental studies have found that they are poorly absorbed in the body and eliminated quickly, mainly because of tribaquidone. The water solubility and fat solubility are very poor. The inventors of the present invention modified its structure to prepare tribacudone sulfonate, especially sodium tribacudone sulfonate, which has increased water solubility. The above-mentioned studies have not been reported yet. Through the overall pharmacological experimental research, we first found that tribacudone sodium has anti-senile dementia therapeutic effect, and the curative effect is better than that of tribacudone.

[0076] The pharmacological activity of geniposide (or geniposide) iridoids in the treatment of senile dementia drugs or Alzheimer's disease, but studies have reported that it can cause severe liver damage when applied in large...

Embodiment 3

[0103] The mensuration of the tribauminone lignans composition in the Rhizoma Rhizoma Rhizoma: The present inventor has set up the method for HPLC method to measure the tribaumerone content, adopts chloroform ultrasonic extraction, Eclipse XDB-C18 chromatographic column (4.6mm * 250mm, 5 μm ), mobile phase: methanol-water (75:25), the flow rate is 1.0mL min -1 , the detection wavelength is 240nm, and the column temperature is 25°C. Under this chromatographic condition, the retention time of tribaquidone is 10.2min, there is no impurity interference, and the separation degree from other peaks is good, and the regression equation is obtained: Y=4373376X+4304802, r=0.9997 (n=5), and the linear range is 0.232 Between μg and 4.640μg, the recoveries were 98.6%. The average content of tribaquidone in the medicinal material of Sanbai grass was found to be 0.7831 mg·g in the experiment. -1 . The results showed that the aerial part of Sanbai herb had a high content of flavonoids, whi...

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Abstract

The invention relates to sauchinone sulfonate or sauchinone and geniposide (or jasminoidin) composition and application thereof in preparing liver protection medicine or senile dementia medicine. The sauchinone or geniposide has the problems of poor absorption, quick elimination, low enterohepatic circulation and bioavailability and the like when being independently applied to pharmacological activity of protecting liver or treating senile dementia; thus, sauchinone sulfonate or sauchinone and geniposide are pharmacologically combined and applied; the problems that the sauchinone and the geniposide have poor curative effects when being independently applied are solved; the sauchinone sulfonate or sauchinone and geniposide composition has an accurate curative effect and a small side effect, especially sodium sauchinone sulfonate and geniposide injection has a very accurate curative effect for treating hepatitis or liver damage or senile dementia, and the sodium sauchinone sulfonate or sauchinone and geniposide composition can be applied to intravenous administration.

Description

technical field [0001] The present invention relates to tribacuadone sulfonate, tribacuadone sodium or a composition of tribacuadone and geniposide and its use in the preparation of liver-protecting medicine or senile dementia medicine or Alzheimer's disease medicine The application of the invention belongs to the technical field of traditional Chinese medicine preparation. Background technique [0002] The components of tribaturon lignans have the pharmacological activity of protecting the liver or treating senile dementia or Alzheimer's disease, but pharmacokinetic experimental studies have found that they are poorly absorbed in the body and eliminated quickly, mainly Because of the water-solubility and fat-solubility of tribagudone are very poor. The inventors of the present invention modified its structure to prepare tribacudone sulfonate, especially sodium tribacudone sulfonate, which has increased water solubility. The above studies have not been reported yet. Throug...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D493/20A61K31/36A61K31/7048A61P1/16A61P25/28
Inventor 张忠立左月明
Owner 张忠立
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