Ginsenoside-human serum albumin complex injection, preparation method therefor and application of ginsenoside-human serum albumin complex injection

A technology of human serum albumin and ginsenosides, which can be used in pharmaceutical formulations, drug combinations, drug delivery and other directions, can solve problems such as poor water solubility, affecting product yield, denaturation and inactivation, etc., to protect natural conformation and improve killing. effect, effect of strong killing effect

Inactive Publication Date: 2020-12-18
JILIN UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The problems with this technique are: 1. The chemical crosslinking using glutaraldehyde as a crosslinking agent will not specifically occur between proteins and small molecules, and a large amount of by-products will inevitably be produced in the reaction process. Take the cross-linking of small molecules of drugs as an example, such as HSA polymers, small molecule polymers, and the hydroxyl and amino groups inside the HSA molecule are cross-linked together, which greatly affects the yield of the product; 2. Through The chemically cross-linked HSA and the small molecular compound are combined in a covalent way, so the structure will also be destroyed, which will affect its function (structure determines function)
Taking ginsenosides as an example, the changes in the position of the hydroxyl group and the sugar ring in the saponin molecule, and the difference in the chirality of the 20-position carbon atom lead to a series of facts that the structure of ginsenosides is similar but the functions are very different.

Method used

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  • Ginsenoside-human serum albumin complex injection, preparation method therefor and application of ginsenoside-human serum albumin complex injection
  • Ginsenoside-human serum albumin complex injection, preparation method therefor and application of ginsenoside-human serum albumin complex injection
  • Ginsenoside-human serum albumin complex injection, preparation method therefor and application of ginsenoside-human serum albumin complex injection

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preparation example Construction

[0041] The invention provides a preparation method of ginsenoside-human serum albumin complex injection, comprising the following steps:

[0042] 1) mixing human serum albumin with physiological saline to obtain a human serum albumin solution;

[0043] 2) mixing ginsenosides with ethanol-containing physiological saline to obtain a ginsenoside suspension;

[0044] 3) Add the ginsenoside suspension obtained in step 2) dropwise into the human serum albumin solution obtained in step 1), stir, centrifuge to take the supernatant, filter, and take the filtrate;

[0045] The steps 1) and 2) are not limited in chronological order;

[0046] The ginsenosides include ginsenoside Rg5 and / or ginsenoside Rk1.

[0047] In the present invention, the molar ratio of the ginsenoside to human serum albumin is preferably (1:1) to (1:10), more preferably (1:3) to (1:7), most preferably ( 1:4) ~ (1:5). Within the molar ratio range of the present invention, the ginsenoside-human serum albumin comple...

Embodiment 1

[0059] Types and sources of raw materials: ginsenoside Rg5 and ginsenoside Rk1 were purchased from Shanghai Yuanye; human serum albumin was purchased from SigmaAldrich.

[0060] Process flow:

[0061] 1. Weigh 20g of HSA, add it to 100mL of normal saline, stir at 4°C for 3 hours to fully dissolve it (hereinafter referred to as solution A)

[0062] 2. Weigh 100 mg of the mixture of ginsenoside Rg5 and ginsenoside Rk1, add it to 50 mL of physiological saline containing 6% ethanol at room temperature, and stir at room temperature to form a suspension (hereinafter referred to as suspension B).

[0063] 3. At room temperature, add solution A drop by drop to suspension B while stirring, and the dropping speed is controlled at 1mL / min until solution A is completely added to suspension B.

[0064] 4. Move the mixed solution to an environment at 4°C, continue to stir for 3 hours, centrifuge at 20,000×g for 30 minutes, then filter with a 0.22 micron filter membrane, collect the filtere...

Embodiment 2

[0066] Determination of Interaction Between Human Serum Albumin and Ginsenosides Rg5 and Rk1 by Isothermal Calorimetric Titration

[0067] Use a Malvern MicroCal ITC200 isothermal calorimeter for measurement, add 200 μL of 20 μM ginsenoside solution (containing 5% ethanol) into the sample pool, draw 40 μL of 400 μM human serum albumin solution (containing 5% ethanol) into the sample needle, and start titration. The result is as figure 1 and figure 2 As shown, among them, figure 1 It is the result of the isothermal calorimetric titration experiment of ginsenoside Rg5 and HSA; figure 2 It is the result of isothermal calorimetric titration experiment of ginsenoside Rk1 and HSA. The abscissa in the figure represents time, the molar ratio of HSA and saponin, and the ordinate represents the heat change during the titration reaction. The results showed that ginsenoside Rg5 and ginsenoside Rk1 could bind to HSA, and the single binding site model was used for fitting, and the bin...

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Abstract

The invention relates to a ginsenoside-human serum albumin complex injection, a preparation method therefor and application of the ginsenoside-human serum albumin complex injection and belongs to thetechnical field of medicine preparation. The preparation method disclosed by the invention comprises the following steps: 1) mixing human serum albumin with physiological saline, so as to obtain a human serum albumin solution; 2) mixing ginsenoside with ethanol-containing physiological saline, so as to obtain a ginsenoside suspension; 3) dropwise adding the ginsenoside suspension obtained in the step 2) into the human serum albumin solution obtained in the step 1), carrying out stirring, carrying out centrifugation to obtain supernatant, and carrying out filtering, so as to obtain filter liquor. The ginsenoside comprises ginsenoside Rg5and/or ginsenoside Rk1. According to the preparation method disclosed by the invention, a natural structure of the ginsenoside can be protected from being damaged, and the activity of the ginsenoside is guaranteed; the water solubility of the ginsenoside is improved greatly, and the ginsenoside-human serum albumin complex injection is safe and effective;and the prepared injection can also be used for effectively improving a tumor cell killing effect of cisplatin, adriamycin and paclitaxel.

Description

technical field [0001] The invention relates to the technical field of medicine preparation, in particular to a ginsenoside-human serum albumin complex injection and a preparation method and application thereof. Background technique [0002] Human serum albumin (HSA) is widely distributed in various tissues and organs of the human body. It is used as a drug carrier because of its molecular surface has multiple binding sites that can interact with small molecules. Through intravenous injection, the small molecule drug can be delivered to various parts of the body through the blood circulation. In the relevant patents that have been consulted, in order to improve the binding strength of drug molecules and HSA, people have adopted the method of chemical cross-linking of small molecules and HSA. After cross-linking, HSA and drug small molecules are covalently bonded connect. The problems with this technique are: 1. The chemical crosslinking using glutaraldehyde as a crosslinki...

Claims

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Application Information

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IPC IPC(8): A61K9/08A61K47/64A61K31/704A61K33/243A61K31/337A61P35/00
CPCA61K9/0019A61K9/08A61K31/337A61K31/704A61K47/643A61P35/00A61K33/243A61K2300/00
Inventor 金英花李赫李杨
Owner JILIN UNIV
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