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

A pentafluorouracil and drug technology, applied in the field of pentafluorouracil-containing drugs, can solve the problem of the small molecule drug pentafluorouracil delivery reliability, the limited clinical application of pentafluorouracil drugs, the self-design contradiction between toxicity and transfection activity, and the difficulty in ensuring targeting bases. Group and other problems, to achieve the effect of 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, but 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, it is difficult to achieve non-toxic degradation of its connection in vivo
[0006] Therefore, how to improve the delivery reliability of the existing small molecule drug pentafluorouracil is one of the difficulties in solving the current limited clinical application of pentafluorouracil drugs.

Method used

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  • Medicine containing pentafluorouracil, its preparation method, pharmaceutical composition and application
  • Medicine containing pentafluorouracil, its preparation method, pharmaceutical composition and application
  • Medicine containing pentafluorouracil, its preparation method, pharmaceutical composition and application

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preparation example Construction

[0154] According to the second aspect of the present application, there is also provided a method for preparing the above-mentioned pentafluorouracil-containing medicine, comprising the following steps: providing any of the above-mentioned nucleic acid nanoparticles; Fluorouracil is mounted on nucleic acid nanoparticles to obtain a medicine containing pentafluorouracil.

[0155] When physically linked, pentafluorouracil is usually physically intercalated between GC base pairs. When the covalent connection is used for connection, pentafluorouracil usually undergoes a chemical reaction with the amino group outside the G ring to form a covalent connection. The pentafluorouracil-containing medicine prepared by the above-mentioned method has good targeting ability after modification of the target head, can deliver pentafluorouracil stably, and has high reliability.

[0156] In a preferred embodiment, the step of mounting pentafluorouracil by physical connection includes: mixing an...

Embodiment 1

[0179] 1. RNA and DNA nanoparticle carriers:

[0180] (1) The three polynucleotide base sequences that make up the RNA nanoparticle are specifically shown in 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) Dissolve RNA or DNA single strands a, b, and 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 temperature is 95°C), and aft...

Embodiment 2

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

[0200] (1) 7 groups of three polynucleotide base sequences that make up RNA nanoparticles:

[0201] Table 2: R-1:

[0202]

[0203] Table 3: R-2:

[0204]

[0205] Table 4: R-3:

[0206]

[0207] Table 5: R-4:

[0208]

[0209] Table 6: R-5:

[0210]

[0211] Table 7: R-6:

[0212]

[0213] Table 8: R-7:

[0214]

[0215] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0216] Second, the self-assembly experimental steps:

[0217] (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;

[0218] (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;

[0219] (3) Load the product onto an 8% (m / v) native PAGE gel and purify the com...

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Abstract

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

Description

technical field [0001] The present application relates to the field of medicine, in particular, to a medicine containing pentafluorouracil, its preparation method, pharmaceutical composition and application. Background technique [0002] At present, cancer has become one of the major diseases that threaten human health and quality of life. The search for effective drugs and strategies for the treatment of cancer has become an urgent problem to be solved in the entire medical field around the world. [0003] Pentafluorouracil is commonly used in the treatment of liver cancer, colon cancer, rectal cancer, gastric cancer, breast cancer, ovarian cancer, chorioepithelial cancer, malignant mole, head and neck squamous cell carcinoma, skin cancer, lung cancer, cervical cancer, pancreatic cancer or bladder cancer. It can inhibit the synthesis of DNA by inhibiting thymidine nucleotide synthase, and also has a certain inhibitory effect on the synthesis of RNA, and plays an important r...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/513A61K47/54A61K47/69A61K9/51A61K47/26A61P35/00
CPCA61K31/513A61K47/549A61K47/6929A61K9/5123A61P35/00
Inventor 王力源王萌
Owner BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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