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

A gemcitabine and drug technology, which is applied in drug combination, medical preparations containing active ingredients, drug delivery, etc., can solve the limitation of gemcitabine drug delivery reliability in small molecule drug gemcitabine, the contradiction between toxicity and transfection activity in its own design , difficult to connect, non-toxic degradation and other issues, to achieve high reliability, improve stability, and reduce the chance of contact

Active Publication Date: 2022-07-22
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.
[0006] Therefore, how to improve the delivery reliability of the existing small molecule drug gemcitabine is one of the difficulties in solving the current limited clinical application of gemcitabine.

Method used

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

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preparation example Construction

[0156] According to the second aspect of the present application, there is also provided a method for preparing the above-mentioned gemcitabine-containing medicine, comprising the following steps: providing any of the above-mentioned nucleic acid nanoparticles; Loaded on nucleic acid nanoparticles to obtain a drug containing gemcitabine.

[0157] When physically linked, gemcitabine usually forms a physical intercalation between the GC base pairs. When the connection is made by covalent connection, gemcitabine usually chemically reacts with the amino group outside the G ring to form a covalent connection. The gemcitabine-containing medicament prepared by the above-mentioned method can have good targeting ability after being modified by the target head, can deliver gemcitabine stably, and has high reliability.

[0158] In a preferred embodiment, the step of mounting gemcitabine by physical connection includes: mixing and stirring gemcitabine, nucleic acid nanoparticles and a fi...

Embodiment 1

[0182] 1. RNA and DNA nanoparticle carriers:

[0183] (1) The base sequences of the three polynucleotides constituting the RNA nanoparticles are shown in Table 1:

[0184] Table 1:

[0185]

[0186]

[0187] (2) Three polynucleotide base sequences of DNA nanoparticles

[0188] 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.

[0189] The a, b and c chains of the above RNA nanoparticles and DNA nanoparticles were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0190] Second, the self-assembly experimental steps:

[0191] (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;

[0192](2) Heating the mixed solution to 80°C / 95°C (wherein the RNA assembly temperature is 80°C and the DNA assembly temperature is 9...

Embodiment 2

[0203] 1. 7 groups of short-sequence RNA nanoparticle carriers:

[0204] (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:

[0205] Table 2: R-1

[0206]

[0207] Table 3: R-2

[0208]

[0209]

[0210] Table 4: R-3

[0211]

[0212] Table 5: R-4

[0213]

[0214] Table 6: R-5

[0215]

[0216]

[0217] Table 7: R-6

[0218]

[0219] Table 8: R-7

[0220]

[0221] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0222] Second, the self-assembly experimental steps:

[0223] (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;

[0224] (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;

[0225]...

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Abstract

The application provides a medicine containing gemcitabine, its preparation method, pharmaceutical composition and application. The drug includes nucleic acid nanoparticles and gemcitabine, and gemcitabine 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 gemcitabine-containing medicine provided by the present application, after the nucleic acid domain is modified by the target head, can have better targeting, can deliver gemcitabine stably, and has high reliability.

Description

technical field [0001] The present application relates to the field of medicine, in particular, to a medicine containing gemcitabine, its preparation method, pharmaceutical composition and application. Background technique [0002] Gemcitabine is a new cytosine nucleoside derivative. Like cytarabine, it is activated by deoxycytosine kinase and metabolized by cytosine deaminase after entering the human body. This product is a pyrimidine antitumor drug with the same mechanism of action as cytarabine. Its main metabolite is incorporated into DNA in cells and mainly acts on the G1 / S phase. But the difference is that in addition to being incorporated into DNA, difluorodeoxycytidine can also inhibit nucleotide reductase, resulting in a decrease in intracellular deoxynucleoside triphosphate; another difference from cytarabine is that it can inhibit deoxycytidine Pyrimidine deaminase reduces the degradation of intracellular metabolites and has a self-potentiating effect. Clinical...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/54A61K31/7068A61P35/00
CPCA61K47/6929A61K47/549A61K31/7068A61P35/00
Inventor 王力源王萌
Owner BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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