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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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, wh...

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.

Application Domain

Organic chemistryViral antigen ingredients +6

Technology Topic

AntigenAntibody +11

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Examples

Experimental program(7)

Example Embodiment

[0042] Example 1: Synthesis of immunoagonist 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 the reaction was carried out at room temperature for 2h. The reaction was detected by LC-MS and the reaction was over. Afterwards, 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 white solid. Such as figure 2 As shown, ESI-MS: m/z=542.10[M+H]+.

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

Example Embodiment

[0045] Example 2:

[0046] Dissolve 1g of compound 1 (2.25mmol) in 13.4ml of anhydrous DMF, add EDC600mg and NHS400mg in batches, react at room temperature for 4h, and LC-MS to detect the reaction. After the reaction is over, pour the reaction solution into 100ml of ice water and filter with suction. Wash with water and dry to obtain 0.98 g of white solid. ESI-MS: m/z=542.10[M+H]+.

Example Embodiment

[0047] Example 3:

[0048] Dissolve 1g of compound 1 (2.25mmol) in 10ml of anhydrous DMF, add EDC450mg and NHS250mg in batches, react at room temperature for 1.5h, and detect the reaction by LC-MS. After the reaction is over, pour the reaction solution into 100ml of ice water and filter with suction. Wash with water and dry to obtain 0.86 g of white solid. ESI-MS: m/z=542.10[M+H]+.

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