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Medicine containing aspirin, preparation method of medicine containing aspirin, medicine composition and application

A technology of aspirin and medicine, which is applied in the field of its preparation and aspirin-containing medicine, can solve the problems of limited clinical application of small molecule drug aspirin delivery reliability, difficult connection, non-toxic degradation, and influence

Active Publication Date: 2020-04-07
BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Cationic liposomes have high transfection activity in vivo and in vitro, however, because the positive charge on the surface affects their normal distribution in vivo, at the same time, cationic lipids can cause immunogenicity and inflammatory responses in animal experiments
The development of polycationic gene carriers has been relatively mature. However, it is difficult to ensure that the targeting group is on the surface of the structure in the structural design, and there is a self-design contradiction between toxicity and transfection activity. At the same time, its connection is difficult to achieve non-toxic degradation in vivo.
[0004] Therefore, how to improve the delivery reliability of the existing small molecule drug aspirin is one of the difficulties in solving the current limited clinical application of aspirin.

Method used

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  • Medicine containing aspirin, preparation method of medicine containing aspirin, medicine composition and application
  • Medicine containing aspirin, preparation method of medicine containing aspirin, medicine composition and application
  • Medicine containing aspirin, preparation method of medicine containing aspirin, medicine composition and application

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preparation example Construction

[0152] According to the second aspect of the present application, there is also provided a method for preparing the above-mentioned aspirin-containing drug, which includes the following steps: providing any one of the above-mentioned nucleic acid nanoparticles; Loaded on nucleic acid nanoparticles to obtain aspirin-containing medicines.

[0153] When physically linked, aspirin is usually intercalated between GC base pairs by physical intercalation. However, when a covalent link is used for linking, aspirin usually undergoes a chemical reaction with the amino group outside the G ring to form a covalent link. The aspirin-containing drug prepared by the above-mentioned method can have better targeting after the target head is modified, can deliver aspirin stably, and has high reliability.

[0154] In a preferred embodiment, the step of mounting aspirin through physical connection includes: mixing and stirring aspirin, nucleic acid nanoparticles and the first solvent to obtain a ...

Embodiment 1

[0178] 1. RNA and DNA nanoparticle carriers:

[0179] (1) The base sequences of the three polynucleotides that make up the RNA nanoparticles are shown in Table 1:

[0180] Table 1:

[0181]

[0182]

[0183] (2) Three polynucleotide base sequences of DNA nanoparticles

[0184] The DNA uses the same sequence as the above RNA, except that T is substituted for U. Among them, the molecular weight of chain a is 8802.66, the molecular weight of chain b is 8280.33, and the molecular weight of chain c is 9605.2.

[0185] The a, b, and c strands of the above-mentioned RNA nanoparticles and DNA nanoparticles were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0186] 2. Self-assembly experimental steps:

[0187](1) RNA or DNA single strands a, b, and c are simultaneously mixed and dissolved in DEPC water or TMS buffer at a molar ratio of 1:1:1;

[0188] (2) Heat the mixed solution to 80°C / 95°C (the RNA assembly temperature is 80°C, and the DNA assembly tempera...

Embodiment 2

[0199] 1. Seven groups of short-sequence RNA nanoparticle carriers:

[0200] (1) The base sequences of the three polynucleotides of the seven groups of RNA nanoparticles are shown in Table 2 to Table 8:

[0201] Table 2: R-1

[0202]

[0203] Table 3: R-2

[0204]

[0205]

[0206] Table 4: R-3

[0207]

[0208] Table 5: R-4

[0209]

[0210] Table 6: R-5

[0211]

[0212]

[0213] Table 7: R-6

[0214]

[0215] Table 8: R-7

[0216]

[0217] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0218] 2. Self-assembly experimental steps:

[0219] (1) RNA single strands a, b, and c are simultaneously mixed and dissolved in DEPC water or TMS buffer at a molar ratio of 1:1:1;

[0220] (2) Heat the mixed solution to 80°C, keep it for 5min and then cool down slowly to room temperature at a rate of 2°C / min;

[0221] (3) Load the product onto an...

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Abstract

The application provides medicine containing aspirin, a preparation method of the medicine containing aspirin, a medicine composition and application. The medicine comprises nucleic acid nanoparticlesand the aspirin, wherein the aspirin is hung and loaded on the nucleic acid nanoparticles; the nucleic acid nanoparticles comprise a nucleic acid structural domain; the nucleic acid structural domaincomprises a sequence a, a sequence b and a sequence c; the sequence a comprises a sequence a1 or a sequence obtained by performing insertion, deletion or substitution of at least one base on the sequence a1; the sequence b comprises a sequence b1 or a sequence obtained by performing insertion, deletion or substitution of at least one base on the sequence b1; and the sequence c comprises a sequence c1 or a sequence obtained by performing insertion, deletion or substitution of at least one base on the sequence c1. The medicine containing aspirin provided by the invention has the advantages thatafter the nucleic acid structural domain is modified by a target head, good targeting performance is realized; the aspirin can be stably delivered; and the reliability is very high.

Description

technical field [0001] The present application relates to the field of medicine, in particular to a medicine containing aspirin, its preparation method, pharmaceutical composition and application. Background technique [0002] Aspirin (Aspirin, acetylsalicylic acid) is a white crystal or crystalline powder, odorless or slightly smelly of acetic acid, slightly soluble in water, easily soluble in ethanol, soluble in ether and chloroform, and its aqueous solution is acidic. Aspirin is a derivative of salicylic acid. After nearly a hundred years of clinical application, it has been proved to be effective in relieving mild or moderate pain, such as toothache, headache, neuralgia, muscle pain and dysmenorrhea. It is also used for fever such as cold and flu. The fever of the disease, the treatment of rheumatic pain, etc. In recent years, it has been found that aspirin has an inhibitory effect on platelet aggregation and can prevent the formation of thrombus. It is clinically used ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/616A61K47/54A61K47/69A61K9/51A61K47/26A61P29/00A61P9/00A61P9/10A61P19/02A61P17/00A61P35/00
CPCA61K31/616A61K47/549A61K47/6929A61K9/5123A61P29/00A61P9/00A61P9/10A61P19/02A61P17/00A61P35/00
Inventor 王力源王萌
Owner BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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