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Tetrandrine organic acid salt as well as preparation method and application

A technology of tetrandrine and organic acid salts, applied in organic chemistry, organic active ingredients, medical preparations containing active ingredients, etc., can solve problems affecting anti-tumor effects, etc., and achieve improved bioavailability and strong anti-tumor activity , the effect of high success rate

Inactive Publication Date: 2009-05-06
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Alkaloids often combine with organic acids (citric acid, fruit acid, oxalic acid, succinic acid, acetic acid, propionic acid, etc.) alkaloid, the hydrophobicity of this tetrandrine will undoubtedly affect its anti-tumor effect in vivo

Method used

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  • Tetrandrine organic acid salt as well as preparation method and application
  • Tetrandrine organic acid salt as well as preparation method and application
  • Tetrandrine organic acid salt as well as preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Example 1 Preparation of tetrandrine salt of citric acid monohydrate powder

[0031] At room temperature, weigh 10 grams of tetrandrine, put it into a glass beaker, then add 100 milliliters of 2.5% citric acid monohydrate (C 6 h 5 o 7· h 2 (0) solution, stirring, until the tetrandrine powder is completely dissolved, the solution is completely transparent, then the citric acid powder tetrandrine salt solution is dried to obtain white citric acid powder tetrandrine salt powder.

[0032]

[0033] Tetrandrine (I)

[0034] The experimental results show that the citric acid monohydrate tetrandrine salt prepared by this method not only has a high success rate (100%); moreover, the required reagents are few, only citric acid and water are required, and the operation steps are few and simple. It can be operated immediately, and the success rate is 100%.

Embodiment 2

[0035] Example 2 Preparation of anhydrous citric acid powder tetrandrine salt

[0036] At room temperature, weigh 10 grams of tetrandrine, put it into a glass beaker, then add 100 milliliters of 2.5% anhydrous citric acid (C 6 h 5 o 7 ) solution, stirring, until the tetrandrine powder is completely dissolved and the solution is completely transparent, then the citric acid powder tetrandrine salt solution is dried to obtain white tetrandrine citrate powder. Reaction formula:

[0037]

[0038] Experimental results show that: the anhydrous citric acid powder tetrandrine salt prepared by this method not only has a high success rate (100%); moreover, it requires few reagents, only citric acid and water, and the operation steps are few and simple, which is easy to use in ordinary laboratories. to operate.

Embodiment 3

[0039] Example 3 Solubility determination of citric acid powder tetrandrine salt

[0040] Weigh 0.1 g of citric acid powder tetrandrine at room temperature, put it into a 10ml test tube, then slowly add deionized water or distilled water, shake well while adding, until the added citric acid powder tetrandrine salt is fully dissolved, and the solution appears completely until transparent. Then, measure the water required for completely dissolving citric acid powder tetrandrine salt, and calculate the solubility of citric acid powder tetrandrine salt in water-soluble.

[0041] The experimental results show that the solubility of citric acid powder tetrandrine salt in water is greater than 200mg / ml.

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PUM

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Abstract

The invention provides tetrandrine organic acid salts. White citric acid tetrandrine salt crystal is prepared through adding tetrandrine to citric acid solution to carry out salt-forming reaction, and drying the obtained tetrandrin citric acid salt solvent. The invention is proved through pharmacological test to have wider and stronger antineoplastic activity, and is proved through in-vitro cell culture system and animal test to have no obvious toxic or side effects on cell growth of a normal person and a tested animal with effective antineoplastic dosage, and have good safety, good water solubility and pH value approximate to the physiological status of human blood, thereby facilitating the improvement on bioavailability and drug action. The tetrandrine organic acid salts can be applied to preparing medicine for treating neopastic diseases. The preparation method has the advantages of simple and feasible process, high success ratio and low cost, and is applicable to scale production. The structural general formula of the tetrandrine organic acid salts is shown as the above.

Description

technical field [0001] The invention relates to citrate powder Tetrandrine citrate and its preparation, as well as the application of the drug combination containing them in the preparation of drugs for treating tumor diseases. Background technique [0002] According to the report of the World Health Organization: in 2007, about 25 million people in the world suffered from various cancers, and 7.9 million people died of these cancers (accounting for about 13% of all deaths). Cancer deaths are projected to continue to increase worldwide, with an estimated 12 million deaths from cancer in 2030. Cancer claimed nearly 1.8 million lives in China in 2006, about 300,000 more than in 2005. Cancer has become the number one killer of human health. Unfortunately, the currently commonly used drugs cannot effectively control and treat these cancers, so it is of great significance to study new and better drugs to prevent and treat these cancers. [0003] Tetrandrine, also known as Tetr...

Claims

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Application Information

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IPC IPC(8): C07D491/18A61K31/4748A61P35/00
Inventor 徐荣臻古莹张旭照干小仙
Owner ZHEJIANG UNIV
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