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5-fluorouracil-containing medicine and preparation method thereof, and pharmaceutical composition and application thereof

A pentafluorouracil and drug technology, applied in the field of pentafluorouracil-containing drugs, can solve problems such as difficulty in ensuring targeting groups, influence, and delivery reliability of small-molecule drug pentafluorouracil, and limited clinical application of pentafluorouracil drugs.

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, 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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  • 5-fluorouracil-containing medicine and preparation method thereof, and pharmaceutical composition and application thereof
  • 5-fluorouracil-containing medicine and preparation method thereof, and pharmaceutical composition and application thereof
  • 5-fluorouracil-containing medicine and preparation method thereof, and pharmaceutical composition and application thereof

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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 drug, which includes the following steps: providing any one of the above-mentioned nucleic acid nanoparticles; Fluorouracil is mounted on nucleic acid nanoparticles to obtain a drug containing pentafluorouracil.

[0155] When a physical connection is used, 5-fluorouracil will usually be intercalated between GC base pairs by physical intercalation. In the case of covalent linkage, pentafluorouracil usually reacts with the amino group outside the G ring to form a covalent linkage. The pentafluorouracil-containing drug prepared by the above method can have better targeting after the target head is modified, can stably deliver the pentafluorouracil, and has high reliability.

[0156] In a preferred embodiment, the step of mounting pentafluorouracil through physical connection includes: mixing and stirring pentafluorouraci...

Embodiment 1

[0179] 1. RNA and DNA nanoparticle carriers:

[0180] (1) The three polynucleotide base sequences that make up the RNA nanoparticles, see Table 1 for details:

[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 temperature is 95°C), keep i...

Embodiment 2

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

[0200] (1) Seven 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] 2. Self-assembly experimental steps:

[0217] (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;

[0218] (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;

[0219] (3) Load the product onto an 8% (m / v) non-denaturing PAGE gel and purify the comple...

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Abstract

The application provides a 5-fluorouracil-containing medicine and a preparation method thereof, and a pharmaceutical composition and an application thereof. The medicine comprises nucleic acid nanoparticles and 5-fluorouracil, and besides, the 5-fluorouracil is carried on the nucleic acid nanoparticles; and the nucleic acid nanoparticles comprise a nucleic acid domain, the nucleic acid domain comprises a sequence a, a sequence b and a sequence c, the sequence a comprises a sequence a1 or a sequence of the sequence a1 with at least one base insertion, deletion or substitution, the sequence b comprises a sequence b1 or a sequence of the sequence b1 with at least one base insertion, deletion or substitution, and the sequence c comprises a sequence c1 or a sequence of the sequence c1 with at least one base insertion, deletion or substitution. After the nucleic acid structural domain is modified by a target head, the provided 5-fluorouracil-containing medicine has relatively good targetingproperty, can stably deliver the 5-fluorouracil and is very high in reliability.

Description

technical field [0001] The 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. Finding effective drugs and treatment strategies for cancer treatment 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, choriocarcinoma, 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 synthetase, and also has a certain inhibitory effect on the synthesis of RNA, which plays an important role in the medic...

Claims

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Application Information

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Patent Type & Authority Applications(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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