Composition containing tripterine, preparation method and use

A technology of tripterine and composition, which is applied in the field of medicine and can solve problems such as poor stability

Inactive Publication Date: 2009-08-05
SUZHOU LEINA PHARMA RES DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, tripteryne has a quinoid structure, and the carbonyl α-position has an active hydroxyl group, which has poor stability. Therefore, solving the stability problem of tripteryne is also a question of whether tripteryne can be used to prepare clinically acceptable drugs. a key question of

Method used

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  • Composition containing tripterine, preparation method and use
  • Composition containing tripterine, preparation method and use
  • Composition containing tripterine, preparation method and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Dissolve 2.25g of tripterine in 200ml of absolute ethanol, dissolve 1.74g of arginine in 10ml of water, add the aqueous solution to the ethanol solution, stir at room temperature for 2 hours until clear, and rotate the film under vacuum at 50°C The solvent was recovered by the evaporator to dryness, and the solid powder was 3.67 g in total.

Embodiment 2

[0020] Dissolve 2.25g of tripterine in 200ml of absolute ethanol, dissolve 2.61g of arginine in 20ml of water, add the aqueous solution to the ethanol solution, stir at room temperature for 1 hour until clear, and rotate the film in vacuum at 40°C The solvent was recovered by the evaporator to dryness, and the total solid powder was 4.57g.

[0021] Take 4.32 g of the solid powder obtained in this example, dissolve it in water for injection, add 2 g of mannitol as an excipient, add water for injection to 100 ml, filter and sterilize with a microporous membrane, and dispense 2 ml into 10 ml of cillin The bottle is freeze-dried to obtain the freeze-dried powder injection, and the specification is 40 mg / bottle in terms of tripterine.

Embodiment 3

[0023] Dissolve 2.25g of tripterine in 400ml of methanol, dissolve 0.73g of lysine in 10ml of water, add the aqueous solution to the methanol solution, stir at 30°C for 2 hours until clear, freeze-dry at -40°C for 24 hours, that is Obtained, a total of 2.84g of solid powder.

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Abstract

The invention discloses a composition of celastrol and arginine salts and a preparation method and application thereof. The medicine composition obtained by the method has better stability and water-solubility compared with the celastrol. The invention also provides the application of the medicine composition in preparing a medicine for treating tumor.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a pharmaceutical composition of tripterine and basic amino acids, a preparation method and its application in the preparation of antitumor drugs. Background technique [0002] Celastrol, tripterine, also known as celastrol, is a class of triterpenes in Tripterygium wilfordii of the Euonymus family. The structural formula is as follows: [0003] [0004] As early as the 1960s, it was found that tripterygne had a strong anti-tumor effect [KojiNaknishi, Yoshikazu Takahashi, et al.Pristimerin.Spectroscopic properties of thedienone-phenol-type rearrangement products and other derivatives.J.Org. Chem., 1965(30): 1729]. In 1998, Chinese scholars confirmed that Tripterygium wilfordii has the effect of inhibiting the formation of new blood vessels, and it is speculated that its anti-tumor activity is exerted through this mechanism [Gao Yong et al. Experimental research on red pigmen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/56A61K31/198A61K31/417A61P35/00C07J63/00
Inventor 刘军锋刘珂傅莹莹邵萌翟大伟柳全文陈猛
Owner SUZHOU LEINA PHARMA RES DEV
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