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Composition for preparing hepatitis B vaccine and preparation method and application of composition

A hepatitis B vaccine and composition technology, which is applied in the directions of drug combinations, active ingredients of heterocyclic compounds, and medical preparations containing active ingredients, etc., can solve the problem that hepatitis B vaccine cannot prevent and clear chronic infection of hepatitis B virus at the same time, and achieves enhanced immunity. Effects of cytokine induction, strong immune activation effect, high antibody production effect

Inactive Publication Date: 2017-10-24
SHENZHEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The object of the present invention is to provide a composition for preparing hepatitis B vaccine and its preparation method and application, which solves the problem that the hepatitis B vaccine in the prior art cannot simultaneously prevent and eliminate chronic infection of hepatitis B virus

Method used

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  • Composition for preparing hepatitis B vaccine and preparation method and application of composition
  • Composition for preparing hepatitis B vaccine and preparation method and application of composition
  • Composition for preparing hepatitis B vaccine and preparation method and application of composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1: the synthesis of immunostimulant activated ester (T7)

[0043] Such as figure 1 As shown, 1g of compound 1 (2.25mmol) was dissolved in 12ml of anhydrous DMF, EDC (518mg, 2.7mmol) and NHS (337mg, 2.93mmol) were added in batches, and reacted at room temperature for 2h, LC-MS detected the reaction, and the reaction was completed Finally, the reaction solution was poured into 100 ml of ice water, filtered with suction, washed with water, and dried to obtain 0.9 g of a white solid. Such as figure 2 Shown, ESI-MS: m / z=542.10[M+H]+.

[0044] It should be noted that EDC is a water-soluble carbodiimide with the chemical formula C 8 h 17 N 3 .HCl, specifically 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride; NHS is N-hydroxysuccinimide; DMF dimethylformamide.

Embodiment 2

[0046] Dissolve 1 g of compound 1 (2.25 mmol) in 13.4 ml of anhydrous DMF, add 600 mg of EDC and 400 mg of NHS in batches, react at room temperature for 4 hours, and detect the reaction by LC-MS. After the reaction, pour the reaction solution into 100 ml of ice water, and filter with suction. Washed with water and dried to obtain 0.98g of white solid. ESI-MS: m / z=542.10[M+H]+.

Embodiment 3

[0048] Dissolve 1 g of compound 1 (2.25 mmol) in 10 ml of anhydrous DMF, add 450 mg of EDC and 250 mg of NHS in batches, react at room temperature for 1.5 h, and detect the reaction by LC-MS. After the reaction, pour the reaction solution into 100 ml of ice water, and filter with suction. Washed with water and dried to obtain 0.86g of white solid. ESI-MS: m / z=542.10[M+H]+.

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Abstract

The invention relates to a composition for preparing a hepatitis B vaccine and a preparation method and application of the composition. Cells infected by a hepatitis B virus can be inactivated and removed in an animal and a human body on the basis of keeping a hepatitis b virus specificity antibody of an original preventive vaccine, so that the composition has double effects of prevention and treatment. A novel high-activity antigen is formed by combining an immunostimulant activated ester and an original antigen HBsAg, and an immunoactivation effect higher than that of the original antigen HBsAg is achieved under the collaboration with an aluminum adjuvant. The composition has the beneficial effects of enhanced immunocytokine induction and higher antibody generation effect, especially high-level mark Th1 immunity generation of a gamma-interferon and an IgG2a antibody has significant innovativeness and practicability in removal of the hepatitis B virus.

Description

technical field [0001] The invention relates to the technical field of hepatitis B vaccine prevention and treatment, more specifically, relates to a composition for preparing hepatitis B vaccine, its preparation method and application. Background technique [0002] Hepatitis B vaccine is a medicine used to prevent hepatitis B. After vaccination, the immune system can be stimulated to produce protective antibodies, so that the human body has the immunity to prevent hepatitis B and achieve the purpose of preventing hepatitis B infection. However, there are 90 million people infected with hepatitis B virus (HBV) in my country, of which 20 million are chronic hepatitis B patients. For chronic hepatitis B infection patients and patients, preventive hepatitis B vaccine is basically ineffective. Therefore, there is a great need for a "therapeutic hepatitis B vaccine" that can both prevent and eliminate the chronic infection of hepatitis B virus. Contents of the invention [00...

Claims

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Application Information

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IPC IPC(8): A61K39/39A61K39/29A61K39/385A61P1/16A61P31/20A61P37/02C07D473/18A61K31/52
CPCA61K31/52A61K39/12A61K39/385A61K39/39A61K2039/55505A61K2039/575A61K2039/60C07D473/18
Inventor 靳广毅王竹林唐黎胡云龙
Owner SHENZHEN UNIV
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