Intestine targeted formulation of PEGylated rotavirus and its synthesizing method

A technology of PEGylation and rotavirus, applied in the direction of antiviral agents, antiviral immunoglobulins, antibodies, etc., can solve the problems of low bioavailability, immune response, short half-life, etc., to reduce immunogenicity, Effect of reducing toxicity and increasing stability

Inactive Publication Date: 2005-06-01
付经国
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although anti-rotavirus-specific polyclonal antibody (RV-IgY) is used for the treatment of rotavirus diarrhea at present, unmodified naked antibody (RV-IgY) is the same as other antibodies or protein drugs, and is used in drug application. There are many shortcomings and limitations in the dosage form: 1) It is easy to cause the body's immune response; 2) It is easily degraded by various hydrolytic enzymes in the gastrointestinal tract; 3) The half-life is short and the bioavailability is low; 4) It is not easy to store, etc., so its curative effect greatly affected
[0005] At present, there are no relevant research reports on PEG-modified rotavirus antibody drugs at home and abroad The application and promotion in our country will drive the development of related industries

Method used

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  • Intestine targeted formulation of PEGylated rotavirus and its synthesizing method
  • Intestine targeted formulation of PEGylated rotavirus and its synthesizing method
  • Intestine targeted formulation of PEGylated rotavirus and its synthesizing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] (1) Synthesis of Polyethylene Glycol PEG Activated Intermediate

[0036] Step 1: Synthesis of omega-methoxypolyethylene glycol

[0037]

[0038] Under the condition of 0--100°C, add methyl bromide into the organic solvent of polyethylene glycol (molar ratio 1:1), stir, react for 2-10 hours, remove the organic solvent in vacuum, and separate the residue by column chromatography , TLC (iodine color) detection, the product was obtained.

[0039] The second step: the synthesis of omega-methoxy polyethylene glycol monoester

[0040]

[0041] name

molecular weight

The molar ratio of

Feeding amount

moles

MePEG2000

2000

1

100g

0.05

Succinic anhydride

100

3

15g

0.15

Triethylamine

101

2

14ml

0.1

DMAP

122

1.1

6.8g

0.055

Dichloromethane

500ml

[0042] Polyethylene glycol MePEG 2000 , succinic anhydride, DMAP, dichl...

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PUM

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Abstract

The present invention discloses polyglycol treated rotavirus antibody intestine targeting preparation as one kind of antibody medicine and its synthesis process. The novel medicine preparation is prepared through the following steps: first synthesizing the polyglycol activated intermediate MePEG-S-NHS and MePEG-S-EDC; then purifying specific anti-rotavirus antibody RV-IgY; and final performing structural modification of the specific anti-rotavirus antibody with the polyglycol activated intermediate MePEG-S-NHS and MePEG-S-EDC to prepare the polyglycol treated rotavirus antibody intestine targeting preparation. The medicine has certain intestine targeting and positioning effect, raised bioavailability, reduced toxic side effect of original medicine, certain delayed function and enhanced clinical treating effect. The medicine has obvious effect on infantile diarrhea caused by rotavirus.

Description

technical field [0001] The invention relates to a novel antibody drug and a preparation method thereof, in particular to a pegylated rotavirus antibody intestinal targeting preparation and a synthesis method thereof. Background technique [0002] In my country, there are 250 million children with diarrhea under the age of 5 every year, of which 120 million are autumn and winter diarrhea caused by rotavirus. Currently, there is no special treatment for this disease except oral or intravenous rehydration to correct dehydration. therapy. Rotavirus is highly contagious, and is often firstly infected by infants with weak resistance, and then spread to other children. Kindergartens are prone to spread infection and have a higher probability of nosocomial infection. After children are infected with rotavirus, due to frequent diarrhea and vomiting, loss of appetite, they are prone to dehydration in varying degrees, and electrolyte imbalance. What's more, encephalitis, intestinal ble...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K39/395A61K47/60A61P1/12A61P31/12C07K16/08C08G65/00
Inventor 付经国陈涛韩法元王昭王金良李继赵永德侯益民
Owner 付经国
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