Ampelopsin and basic amino acid solubilizing system

A technology of staphylococcus and amino acids, which is used in antitumor drugs, organic active ingredients, powder delivery, etc.

Inactive Publication Date: 2009-08-26
LANZHOU UNIVERSITY +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although it has been confirmed that staphylophyllin has a strong anti-tumor effect, it is very slightly soluble in water, which makes it difficult to use clinically

Method used

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  • Ampelopsin and basic amino acid solubilizing system
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  • Ampelopsin and basic amino acid solubilizing system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0115] Embodiment 1. The research of staphylophyllin basic amino acid solubilizing system

[0116] Test purposes

[0117] By comparing the solubilizing effect of L-lysine (L-Lys) and L-arginine (L-Arg) on ​​AMP and the solubility and dissolution stability of the resulting solution, to determine a method that can fully dissolve AMP and The preparation method of the AMP preparation which is stable in solubility and retains the original anti-tumor activity.

[0118] experiment method

[0119] The isoelectric point of AMP is close to pH 5.0, and its molecule contains 6 hydroxyl groups, which are weakly acidic; at the same time, L-Lys and L-Arg are basic amino acids, which can be used clinically in the human body, are safe and reliable, and are ampholytes. The points are 9.74 and 10.76 respectively, which can be combined with protons (H + ) combined into a positively charged cation (-NH3 + ). In order to make the H on the hydroxyl group in the AMP molecule combine with L-Lys o...

Embodiment 2

[0151] Example 2. The purpose of the dissolution stability test of the basic amino acid-solubilized staphylophyllin solution diluted with different pH buffers

[0152] The pH value of the injection should not exceed the range of human physiological tolerance, and the general pH can be between 4 and 9. For a small amount of intravenous injection, due to the buffering effect of blood, the pH can be appropriately relaxed, generally between 3 and 10. However, when a large amount is administered, such as overacid or overalkaline, it will cause acid-base poisoning, so it is advisable to close the blood pH (7.4).

[0153] AMP and L-Lys are formulated at a molar concentration ratio of 1:4, and L-Arg is formulated at a molar concentration ratio of 1:3. The concentration of AMP can reach 200 mg / ml, the pH value is around 9.0, and the alkalinity is relatively high. In order to be more in line with animal experiments And the concentration required for clinical application and the appropr...

Embodiment 3

[0173] Embodiment 3. Comparison of AMP-L-Arg and AMP-Na solubility, dissolution stability and chemical stability

[0174] Test purposes

[0175] By comparing the solubility, dissolution stability and chemical composition stability of the solution formed by the aid of L-arginine (AMP-L-Arg, AA) and staphylophyllin sodium (AMP-Na), in order to find out A preparation method of an AMP preparation with better solubility and better dissolution stability makes the AMP suitable for animal experiments and provides a basis for guiding clinical medication.

[0176] experiment method

[0177] 1. Comparison of solubility and stability of AMP-L-Arg and AMP-Na

[0178] AMP and L-Arg were weighed and mixed at a molar concentration ratio of 1:3, and dissolved in PBS with a pH value of 5.0 to obtain an AMP-L-Arg (AA) solution, and AMP-Na was dissolved in PBS with a pH value of 5.0, and compared Solubility and stability of both.

[0179] 2. Comparison of dissolution stability and pH value of...

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Abstract

The invention provides an ampelopsin composition and a method for preparing the same. The composition comprises: a) ampelopsin and b) a basic amino acid, wherein the weight ratio the component a) to the component b) is between 1:1 and 1:10. The composition can also comprise: c) a pH regulator and or d) a pharmaceutically acceptable carrier and / or a diluting agent. The invention also relates to a medicamnet box containing the ampelopsin composition and carboplatin. The ampelopsin composition can provide improved solubility, stability and a proper pH range and is suitable for clinic use.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations. More specifically, the present invention relates to steroid formulations with improved solubility and stability. Background technique [0002] Ampelopsin (AMP) is the extract of plants of the genus Snake Grapes, which belongs to polyphenolic hydroxyl dihydroflavonols, with a relative molecular weight of 356 and a molecular formula of C 15 h 12 o 8 2H 2 O, its pure product is light yellow granular. The AMP molecule contains 6 phenolic hydroxyl groups, is weakly acidic, and has an isoelectric point close to pH 5.0 (Edited by Sun Wenji et al., "Concise Handbook of Natural Active Ingredients", China Medical Science Press, 1993: 564). [0003] AMP has the advantages of low toxicity, wide range of sources and high extraction rate, but its stability is poor, it is prone to oxidation reaction, insoluble in chloroform and ether, and easily soluble in ethanol, methanol, methylene chloride an...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/352A61K47/16A61K9/14A61P35/00
Inventor 吴勇杰梁健仪李志成余剑桥刘达清范富林
Owner LANZHOU UNIVERSITY
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