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Medicine containing aspirin, its preparation method, pharmaceutical composition and application

A technology of aspirin and drugs, applied in the field of aspirin-containing drugs, and its preparation field, can solve the problems of limited clinical application of small molecule drug aspirin delivery reliability, contradiction between toxicity and transfection activity design itself, difficult connection and non-toxic degradation, etc. Achieve high reliability, improve stability, and reduce the chance of contact

Active Publication Date: 2022-07-26
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, its preparation method, pharmaceutical composition and application
  • Medicine containing aspirin, its preparation method, pharmaceutical composition and application
  • Medicine containing aspirin, its preparation method, pharmaceutical composition and application

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Experimental program
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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 medicine, which comprises the following steps: providing any of the above-mentioned nucleic acid nanoparticles; Loaded on nucleic acid nanoparticles to obtain aspirin-containing medicines.

[0153] When physically linked, aspirin is usually physically intercalated between the GC base pairs. When the connection is made by covalent connection, aspirin usually chemically reacts with the amino group outside the G ring to form a covalent connection. The aspirin-containing medicine prepared by the above-mentioned method can have better targeting ability after being modified by the target head, can deliver aspirin stably, and has high reliability.

[0154] In a preferred embodiment, the step of physically connecting aspirin includes: mixing and stirring aspirin, nucleic acid nanoparticles and a first solvent to obtain a premixed syste...

Embodiment 1

[0178] 1. RNA and DNA nanoparticle carriers:

[0179] (1) The base sequences of the three polynucleotides constituting 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 adopts the same sequence as the RNA described above, except that T replaces U. Among them, the molecular weight of the a chain is 8802.66, the molecular weight of the b chain is 8280.33, and the molecular weight of the c chain is 9605.2.

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

[0186] Second, the self-assembly experimental steps:

[0187](1) Mix and dissolve RNA or DNA single-stranded a, b, c in DEPC water or TMS buffer at a molar ratio of 1:1:1;

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

Embodiment 2

[0199] 1. 7 groups of short-sequence RNA nanoparticle carriers:

[0200] (1) The base sequences of the three polynucleotides that make up the 7 groups of RNA nanoparticles are shown in Tables 2 to 8 respectively:

[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] Second, the self-assembly experimental steps:

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

[0220] (2) heating the mixed solution to 80°C, keeping the temperature for 5min and then slowly cooling to room temperature at a rate of 2°C / min;

[0221]...

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Abstract

The application provides an aspirin-containing medicine, its preparation method, pharmaceutical composition and application. The drug includes nucleic acid nanoparticles and aspirin, and aspirin is mounted on the nucleic acid nanoparticles; the nucleic acid nanoparticles include a nucleic acid domain, the nucleic acid domain includes a sequence, b sequence and c sequence, and the a sequence includes a1 sequence or a1 sequence occurs at least A sequence of base insertion, deletion or substitution, b sequence contains b1 sequence or b1 sequence has at least one base insertion, deletion or substitution, c sequence contains c1 sequence or c1 sequence has at least one base insertion, deletion or substitution the sequence of. The aspirin-containing medicine provided by the present application, after the nucleic acid domain is modified by the target head, can have better targeting, can deliver aspirin stably, and has high reliability.

Description

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

Claims

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Application Information

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Patent Type & Authority Patents(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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