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Combination containing M10C1 compound and active ingredient and preparation method of combination

A technology of M10C1 and active ingredients, applied in the field of compositions comprising M10C1 compounds and active ingredients and their preparation fields, can solve the problems of short half-life, difficult to pass through cell membranes, produce strong inflammatory response, etc., to achieve changes in biodistribution, improve Pharmacokinetic characteristics, effect of reducing adverse reactions

Inactive Publication Date: 2015-11-25
XIAMEN CHENGKUN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Naked siRNA itself is negatively charged, has a large molecular weight, and strong polarity. It is difficult to pass through the cell membrane and vascular endothelium, and it is easy to stay in the spleen. It is easily degraded by nucleases in vivo, with a short half-life, low transfection efficiency, and even strong inflammation. reaction etc.

Method used

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  • Combination containing M10C1 compound and active ingredient and preparation method of combination
  • Combination containing M10C1 compound and active ingredient and preparation method of combination
  • Combination containing M10C1 compound and active ingredient and preparation method of combination

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Embodiment 1 synthetic compound M10C1 compound

[0027] The M10C1 compound is obtained by reacting (1,4,7,10,13,16-hexaazacycloctadecane hexahydrochloride) and an epoxy compound at 90° C. without solvent in a glass bottle equipped with a stirring bar. The reaction time is 24-72 hours at 90°C. Its N, N-bis (3-aminopropyl) methylamine and epoxy alkyl compound (alkyl (C12-C14) glycidyl ether, C12-14 glycidyl ether ratio (molar ratio) in the reaction is 1: 4. Its result is known to obtain confirmation from thin-layer chromatography (TLC), and there is only a kind of main product in the reaction mixture.The product of reactant can be applied after being purified;

Embodiment 2

[0029] The synthetic method of cholesterol-polyethylene glycol compound is: place in 2000 milliliters of round bottom flasks, be (1S, 2R, 5S, 10S, 11S, 14R, 15R)-2,15-dimethyl-14-[(2R )-6-methylheptyl-2 base]tetracyclo[8.7.0.0^[2,7].O^[11,15]]heptadecan-7-en-5-ol (200 grams, 517.26mmol , 1.0 equivalents, pyridine (1000 milliliters). Add 4-toluenesulfonyl chloride (148 grams, 776.30 1.50 equivalents). Stir overnight in an oil bath at 50° C. The reaction mixture is cooled to a cryogenic room with water / ice bath. Add 2000 milliliters of ether to dilute .To the mixture was added water 1×1000 water and 5×1000 20% citric acid. The resulting mixture was washed with 1×1000 ml sat. , 11S, 14R, 15R)-2,15-dimethyl-14-[(2R)-6-methylheptyl-2-yl]tetracyclo[8.7.0.0^[2,7].0^[ 11,15]] Heptadecan-7-en-5-yl 4-methylphenyl-1-sulfonate was placed in a 3000 ml round bottom flask (1S, 2R, 5S, 10S, 11S, 14R, 15R )-2,15-dimethyl-14-[(2R)-6-methylheptyl-2-yl] tetracyclo [8.7.0.0^[2,7].0^[11,15]] ten ...

Embodiment 3

[0031] Carriers for siRNA drugs:

[0032] Justice chain: CCGUGUGCACUUCGCUUCA[dT][dT];

[0033] Antisense strand: UGAAGCGAAGUGCACACGGUC.

[0034] The RNA interference composition also includes components in the following weight ratios:

[0035] The M10C1 compound 1g that embodiment 1 makes

[0036] Cholesterol-polyethylene glycol 10002g;

[0037] The above-mentioned preparation method of the RNA interference composition for the treatment of hepatitis B comprises the following steps:

[0038] (1) dissolving one of the siRNA sequence groups in 0.9% water and 5% sucrose or pure water to obtain solution 1;

[0039] (2) Take the following components by weight, and dissolve these components in alcohol to obtain solution two:

[0040] M10C1 compound 1g

[0041] Cholesterol-polyethylene glycol 10002g;

[0042] The weight ratio of the weight sum of the components in step (2) to one group or mixture in the siRNA sequence group is 2-10:1; the volume ratio of solution one to solutio...

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Abstract

The invention belongs to the field of biological medicine, and particularly relates to a combination containing an M10C1 compound and an active ingredient and a preparation method of the combination. The active ingredient is siRNA, and the combination comprises, by mass, 1-5 parts of siRNA, 1-24 parts of M10C1 compound and 1-10 parts of cholesterol-polyethylene glycol. The combination can improve pharmacokinetic characteristics of siRNA treatment, change bio-distribution, intracellular intake, targeting ability and transfection efficiency and reduce adverse reaction.

Description

technical field [0001] The invention belongs to the field of medicine and biology, and specifically relates to a composition comprising an M10C1 compound and an active ingredient and a preparation method thereof. Background technique [0002] Double-stranded RNA (dsRNA) inhibits the expression of proteins and silences genes, and has a wide range of potential uses in the treatment of human diseases. There are three ways for dsRNA to induce gene silencing: 1. Inactivation of transcriptional function, which refers to DNA or histone methylation under the guidance of RNA; 2. Small interfering nucleic acid (small interfering RNA, siRNA)-induced messenger RNA (mRNA) 3. Attenuation of RNA-mediated transcription function. However, dsRNA-induced gene interference (suppression) is generally considered to refer to RNA degradation in animal cells. Chemically synthesized small molecule RNA, such as siRNA, can degrade more than 95% of mRNA in cells under submicromolar concentration under...

Claims

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Application Information

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IPC IPC(8): A61K31/7088A61K47/22A61P31/20
CPCA61K31/7088A61K47/22
Inventor 崔坤元梁东陈波
Owner XIAMEN CHENGKUN BIOTECH
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