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siRNA composition for treating viral hepatitis B

A viral hepatitis and composition technology, applied in the field of medicine and biology, can solve the problems of packaging, poor protection effect, insufficient drug effect, large drug dosage, etc.

Active Publication Date: 2015-09-23
厦门成朴希晟股权投资合伙企业(有限合伙)
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The wrapping and protection effects of this invention are relatively poor, and the efficacy of the medicine cannot be fully exerted, and it is easily degraded, so a larger dose of medicine is required

Method used

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  • siRNA composition for treating viral hepatitis B
  • siRNA composition for treating viral hepatitis B
  • siRNA composition for treating viral hepatitis B

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] Put epoxyalkyl glycidyl ether (alkyl C12) and 1,4,7,10-tetraazacyclododecane in a molar ratio of 1:4 into a glass bottle with a stirring bar, and react at 90°C for 36 Hour. The reaction products were subjected to TLC analysis, and there was only one main product, which was purified and used to prepare the interfering composition.

[0055] (1) Dissolve 6.25 parts of ID No.267 in water or water containing 9% sucrose to obtain 1L of solution;

[0056] (2) Weigh 1 part of trimethyl [2,3-(dilinoleyloxy) propyl] ammonium chloride, 0.5 part of cylindrine, 1 part of phosphatidylethanolamine, 5 parts of T2C1 compound, cholesterol 1 part, 1 part of cholesterol polyethylene glycol and 3 parts of dimyristoyl glycerol polyethylene glycol, and dissolve these components in alcohol to obtain 0.25 L of solution 2;

[0057] (3) After the solution 1 and the solution 2 are mixed uniformly, vacuum filtration is carried out at room temperature, so that the alcohol therein is gradually evap...

Embodiment 2

[0061] (1) Dissolving 0.2 parts of the siRNA sequence in water or water containing 9% sucrose to obtain a solution of 1 L;

[0062] (2) Weigh 4 parts of T2C1 compound and dissolve it in alcohol to obtain 0.25L of solution 2;

[0063] (3) After the solution 1 and the solution 2 are mixed uniformly, vacuum filtration is carried out at room temperature, so that the alcohol therein is gradually evaporated;

[0064] (4) After most of the alcohol evaporates, homogeneously obtain the particles of the suspension to be 60nm;

[0065] (5) Perform high-pressure homogenization and freeze-drying on the suspension to form a dried product, and obtain the RNA interference composition for treating viral hepatitis B.

Embodiment 3

[0067] (1) Dissolving 0.5 parts of the siRNA sequence in water or water containing 9% sucrose to obtain a solution of 1 L;

[0068] (2) Weigh 6 parts of T2C1 compound and dissolve it in alcohol to obtain 0.5L of solution 2;

[0069] (3) After the solution 1 and the solution 2 are mixed uniformly, vacuum filtration is carried out at room temperature, so that the alcohol therein is gradually evaporated;

[0070] (4) After most of the alcohol is evaporated, homogenize, and the particles of the suspension are 120nm;

[0071] (5) Perform high-pressure homogenization and freeze-drying on the suspension to form a dried product, and obtain the RNA interference composition for treating viral hepatitis B.

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Abstract

The invention belongs to the field of hepatitis B medicine, and particularly relates to a siRNA composition for treating viral hepatitis B. The composition comprises a siRNA sequence and other components, wherein the siRNA sequence is ID No. 267; the other components include 0.5-3 parts by weight of cationic lipid, 2-8 parts by weight of T2C1 compound, 0.5-3 parts by weight of phospholipid, 0-2 parts by weight of cholesterol and 2-10 parts by weight of lipid-polyethylene glycol. Under the situation of achieving the same effect, the injection dosage of a siRNA preparation is much lower than the dosage of mouse medicine in the prior art.

Description

technical field [0001] The invention belongs to the field of medicine and biology, and in particular relates to an siRNA composition for treating viral hepatitis B. Background technique [0002] Hepatitis B (Hepatitis B), referred to as hepatitis B, also known as serotype hepatitis (Serum Hepatitis), is a disease caused by the hepatitis B virus. The hepatitis B virus can cause cirrhosis and liver cancer. Hepatitis B is mainly prevalent in China and some other Asian countries, and is also very prevalent in southern Africa in the Sahara Desert. In 2006, the carrier rate of HBsAg in the Chinese population was 7.18%. Hepatitis ranks with tuberculosis and AIDS as the most common infectious disease in the world. Hepatitis B is the 10th leading cause of death in the world. About 350 to 400 million people in the world are infected with hepatitis B virus, which is more than eight times the number of people infected with AIDS. [0003] Hepatitis B virus seriously plagues people's ...

Claims

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Application Information

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IPC IPC(8): A61K31/713A61P1/16A61P31/20A61K31/395
CPCA61K47/22A61K48/00
Inventor 崔坤元梁东
Owner 厦门成朴希晟股权投资合伙企业(有限合伙)
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