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

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...

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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. Therefore, ginsenosides, etc. A natural compound is equivalent to a new chemical modification on the basis of the original compound. The product is no longer the original compound, but its derivative. It may produce unpredictable results if used

3. The existing chemical cross-linking technology using glutaraldehyde is toxic due to the residue of the cross-linking agent glutaraldehyde in the product

4. During the cross-linking reaction, due to the presence of high concentration of ethanol in the reaction system, the structure of HSA will also be destroyed, resulting in its denaturation and inactivation

However, the water solubility of ginsenoside Rg5 and ginsenoside Rk1 is not good, and they can only be dissolved in aqueous solution at a very low concentration (about 11 μM) at room temperature, and cannot be administered in large quantities through intravenous injection. Those will be hydrolyzed in the human digestive tract and lead to inactivation, so they cannot be effectively used in clinical practice at present.

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