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A kind of small interfering nucleic acid pharmaceutical composition and use thereof

A small interfering nucleic acid and composition technology, applied in the field of biomedicine, can solve the problems of reducing the level of HBV DNA, reducing the effect of reducing surface antigens, etc.

Active Publication Date: 2021-04-27
SUZHOU RIBO LIFE SCIENCE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the other hand, for hepatitis B, traditional drugs only have a reducing effect on HBV DNA, and the reducing effect on surface antigen is extremely weak, while siRNA drugs can block HBV from the mRNA level based on the mechanism of RNA interference (RNA interference, RNAi). cut off, thereby reducing the levels of HBV DNA and HBsAg at the same time
However, since siRNA works in a sequence-specific manner, it is rare for a single siRNA drug to cover multiple genotypes

Method used

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  • A kind of small interfering nucleic acid pharmaceutical composition and use thereof
  • A kind of small interfering nucleic acid pharmaceutical composition and use thereof
  • A kind of small interfering nucleic acid pharmaceutical composition and use thereof

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Experimental program
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Effect test

Embodiment

[0100] The present invention is further described in detail by the following examples, but the present invention is not limited to these examples. It should be noted that, in the following examples, although only the modified siRNA X2M2 and siRNA X30M are used to illustrate the present invention, the pharmaceutical compositions containing unmodified siRNA X2M2 and siRNA X30M also have activity and certain stability sex.

[0101] Unless otherwise specified, the reagents and culture medium used in the following examples are all commercially available products, and operations such as nucleic acid electrophoresis and real-time PCR are performed according to conventional protocols. For example, it can be carried out as described in Molecular Cloning (Cold Spring Harbor Laboratory Press (1989)).

preparation Embodiment 1

[0103] The siRNAs listed in Table 1 were obtained by conventional solid phase synthesis methods. Equimolar mixtures of sense and antisense strands were dissolved in annealing salt solution, followed by conventional annealing to form siRNA duplexes. Among them, NC is an irrelevant sequence that has no targeting effect on HBV mRNA, and as a negative control, it is also referred to as a control siRNA hereinafter; the other siRNAs (siRNA X2M2 and siRNAX30M) are siRNAs that specifically target HBV, and are also referred to below as siRNAs. called the test siRNA.

[0104] Table 1 Sequences of siRNA

[0105]

[0106] Note: Capital letters C, G, U, A and T indicate the base composition of nucleotides; lowercase letter d indicates that a nucleotide to the right of the letter d is a deoxyribonucleotide; lowercase letter m indicates the letter m The ribosyl group of a nucleotide on the left is a 2'-methoxy ribosyl group formed by replacing a 2'-hydroxyl group with a methoxy group; t...

preparation Embodiment 2

[0108] Three dry powder lipid compounds (i.e., amine-containing compound, helper lipid, pegylated lipid) were suspended in ethanol at a molar ratio of 59:29:12 and mixed, the total mass concentration of the three lipid compounds About 8.85mg / ml. The synthesized siRNAs listed in Table 1 were dissolved in 200 mM sodium acetate (pH 5.2) solution so that the siRNA concentration was 0.2 mg / ml (for the case of using siRNA X2M2 and siRNA X30M alone, the siRNA concentration was 0.2 mg). / ml; in the case of combined application of siRNAX2M2 and siRNAX30M, the two siRNAs were mixed in equal proportions, that is, the concentration of each siRNA was 0.1 mg / ml). The resulting lipid ethanol solution and siRNA sodium acetate aqueous solution were mixed very rapidly in a 1:3 volume ratio. The specific composition of the liposome formulation obtained after mixing is described in Table 2.

[0109] Table 2 Composition of liposome preparations

[0110]

[0111] The resulting liposome formul...

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Abstract

The invention provides a small interfering nucleic acid pharmaceutical composition and its use in the preparation of medicines for preventing and / or treating hepatitis B. The small interfering nucleic acid pharmaceutical composition contains two small interfering nucleic acids targeting different genotypes of hepatitis B virus as active ingredients, which can achieve the effect of widely covering multiple genotypes of HBV, and has a synergistic effect on inhibiting multiple genotypes of HBV. And it can reduce the level of HBsAg at the same time, which has the potential of clinical application.

Description

technical field [0001] The present invention relates to the technical field of biomedicine, in particular to a small interference nucleic acid pharmaceutical composition and use thereof. Background technique [0002] Viral Hepatitis B (also known as Hepatitis B or Hepatitis B) is a type of infectious disease that seriously threatens the world, especially China. HBV can be divided into 8 types according to genotype: A, B, C, D, E, F, G, and H. These genotypes differ by at least 8% in sequence and have different geographical distribution characteristics. Among them, type A is distributed worldwide; type B and C are mainly distributed in Asia; type D is mainly distributed in America, southern Europe, and Australia and the Middle East; type E is mainly found in Africa; type F is found in Native Americans and Polynesia; type G is found in the Americas; type H is found in the United States. [0003] Currently, the two major classes of hepatitis B prevention and treatment drugs, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C12N15/113A61K31/713A61P31/20
CPCA61K31/713A61K2300/00
Inventor 张鸿雁高山
Owner SUZHOU RIBO LIFE SCIENCE CO LTD
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