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Triptolide compound composition as well as preparation method and application thereof

A technology for triptolide and a composition is applied in the directions of drug combinations, pharmaceutical formulations, and non-active ingredients medical preparations, which can solve the problems of increasing curative effect, reducing the toxicity of triptolide, and achieving passive targeting. Strong, stable formulation and process parameters, the effect of reducing drug concentration

Inactive Publication Date: 2020-08-07
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it only reduced the toxic effect of triptolide, but did not increase the curative effect

Method used

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  • Triptolide compound composition as well as preparation method and application thereof
  • Triptolide compound composition as well as preparation method and application thereof
  • Triptolide compound composition as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Preparation of diammonium glycyrrhizinate phospholipid complex:

[0041] Weigh an appropriate amount of diammonium glycyrrhizinate and phospholipid (mass ratio: 1:1) and place in a 250mL round bottom flask, add an appropriate amount of reaction solvent absolute ethanol, and heat with magnetic stirring at a temperature of 60°C to make it fully react. The time was 30 min, and the reaction solvent was removed under reduced pressure. Vacuum dry at 50°C for 2 hours, add an appropriate amount of chloroform to the residue, fully dissolve, filter, wash the precipitate with chloroform several times, and recover the precipitate. The filtrate and washing liquid were combined, the chloroform was removed under reduced pressure, and the residue was vacuum-dried at 60° C. to obtain diammonium glycyrrhizinate phospholipid complex.

[0042]Weigh 10 mg of triptolide, 0.9 g of diammonium glycyrrhizinate phospholipid complex, and 1.5 g of egg yolk lecithin in ethanol, add the above drugs ...

Embodiment 2

[0051] Weigh an appropriate amount of diammonium glycyrrhizinate and phospholipid (mass ratio is 1:1) and place it in a 250mL round bottom flask, add an appropriate amount of reaction solvent absolute ethanol, and heat with magnetic stirring at a temperature of 50°C to make it fully react. The time was 30 min, and the reaction solvent was removed under reduced pressure. Vacuum-dry at 40°C for 2 hours, add an appropriate amount of chloroform to the residue, fully dissolve, filter, wash the precipitate with chloroform several times, and recover the precipitate. The filtrate and washing liquid were combined, the chloroform was removed under reduced pressure, and the residue was vacuum-dried at 60° C. to obtain diammonium glycyrrhizinate phospholipid complex. Weigh 10 mg of triptolide, 0.45 g of diammonium glycyrrhizinate phospholipid complex, and 2.7 g of egg yolk lecithin in ethanol, add the above drugs into 10 g of MCT and 0.6 g of oleic acid, and stir magnetically at 80 ° C fo...

Embodiment 3

[0060] Weigh an appropriate amount of diammonium glycyrrhizinate and phospholipid (mass ratio is 1:1.5) and place it in a 250mL round bottom flask, add an appropriate amount of reaction solvent absolute ethanol, and heat with magnetic stirring at a temperature of 60°C to make it fully react. The time was 30 min, and the reaction solvent was removed under reduced pressure. Vacuum-dry at 40°C for 2 hours, add an appropriate amount of chloroform to the residue, fully dissolve, filter, wash the precipitate with chloroform several times, and recover the precipitate. The filtrate and washing liquid were combined, the chloroform was removed under reduced pressure, and the residue was vacuum-dried at 60° C. to obtain diammonium glycyrrhizinate phospholipid complex. Weigh 10 mg of triptolide, 0.6 g of diammonium glycyrrhizinate phospholipid complex, and 1.5 g of egg yolk lecithin in ethanol, add the above drugs into 10 g of MCT and 0.6 g of oleic acid, and stir magnetically at 80 ° C f...

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Abstract

The invention relates to a triptolide compound composition as well as a preparation method and application thereof, and belongs to the technical field of medicines. The triptolide compound compositionhas an obvious effect-enhancing and toxicity-reducing effect. The triptolide compound composition is prepared from triptolide, an ammonium glycyrrhizinate phospholipid compound, an emulsifier, oil, awater-soluble stabilizer, a fat-soluble stabilizer, glycerol, a co-emulsifier and water according to the following ratio, by weight percentage, 0.01%-0.02% of triptolide, 0.1%-0.9% of the ammonium glycyrrhizinate phospholipid complex, 5%-15% of oil, 0.9%-2.7% of the emulsifier, 0.3%-0.9% of the fat-soluble stabilizer, 2.5% of glycerol, 0.05%-0.1% of the co-emulsifier, 0%-0.2% of the water-solublestabilizer and the balance of water. The triptolide and the ammonium glycyrrhizinate are matched for use, the ammonium glycyrrhizinate is used for protecting cells such as livers and kidneys of organisms from being damaged by the triptolide, and the phospholipid complex prepared from the special structure of the ammonium glycyrrhizinate is high in lipophilicity, high in bioavailability and high in preparation stability, so that the treatment effect is improved.

Description

technical field [0001] The invention relates to a triptolide compound composition, a preparation method and an application thereof, and belongs to the technical field of medicine. The triptolide compound composition has obvious synergistic and attenuating effects. Background technique [0002] Triptolide (TP) is an epoxy diterpene lactone compound, which is one of the main active ingredients of Tripterygium wilfordii Hook.F., a plant of the Euonymus family. Triptolide has a variety of pharmacological activities, and is widely used in the treatment of rheumatoid arthritis, rheumatoid arthritis, systemic lupus erythematosus, nephritis and other autoimmune and inflammatory diseases. At the same time, TP has obvious curative effects on ovarian cancer, liver cancer, breast cancer, melanoma, acute leukemia and so on. [0003] However, triptolide has poor water solubility and has severe irritation and adverse reactions to various tissues and organs. For example, triptolide can c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K47/10A61K47/24A61K47/44A61K31/585A61K31/704A61P35/00
CPCA61K9/107A61K47/10A61K47/24A61K47/44A61K31/585A61K31/704A61P35/00A61K2300/00
Inventor 王淑君叶田田牟良玉
Owner SHENYANG PHARMA UNIVERSITY
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