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

A technology of idarubicin and drugs, which is applied in the field of drugs containing idarubicin, can solve the limited clinical application of small molecule drug idarubicin delivery reliability, the contradiction between toxicity and transfection activity, and the difficulty of connection 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 idarubicin is one of the difficulties in solving the current limited clinical application of idarubicin.

Method used

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

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preparation example Construction

[0155]According to the second aspect of the present application, there is also provided a preparation method of the above-mentioned idarubicin-containing medicine, which comprises the following steps: providing any of the above-mentioned nucleic acid nanoparticles; by means of physical connection and / or covalent connection The idarubicin is mounted on the nucleic acid nanoparticles to obtain the idarubicin-containing medicine.

[0156] When physically linked, idarubicin is usually physically intercalated between GC base pairs. When the connection is made by covalent connection, idarubicin usually chemically reacts with the amino group outside the G ring to form a covalent connection. The idarubicin-containing medicine prepared by the above-mentioned method has good targeting ability after modification of the target head, can deliver idarubicin stably, and has high reliability.

[0157] In a preferred embodiment, the step of physically connecting idarubicin includes: mixing an...

Embodiment 1

[0180] 1. RNA and DNA nanoparticle carriers:

[0181] (1) The base sequences of the three polynucleotides constituting the RNA nanoparticles are shown in Table 1:

[0182] Table 1:

[0183]

[0184] (2) Three polynucleotide base sequences of DNA nanoparticles

[0185]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.

[0186] The a, b and c chains of the above RNA nanoparticles and DNA nanoparticles were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0187] Second, the self-assembly experimental steps:

[0188] (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;

[0189] (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 af...

Embodiment 2

[0200] 1. 7 groups of short-sequence RNA nanoparticle carriers:

[0201] (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:

[0202] Table 2: R-1

[0203]

[0204] Table 3: R-2

[0205]

[0206] Table 4: R-3

[0207]

[0208] Table 5: R-4

[0209]

[0210] Table 6: R-5

[0211]

[0212] Table 7: R-6

[0213]

[0214] Table 8: R-7

[0215]

[0216] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0217] Second, the self-assembly experimental steps:

[0218] (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;

[0219] (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;

[0220] (3) Load the product on...

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Abstract

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

Description

technical field [0001] The present application relates to the field of medicine, in particular, to a medicine containing idarubicin, its preparation method, pharmaceutical composition and application. Background technique [0002] Idarubicin (Molecular formula: C 26 H 27 NO 9 , molecular weight: 497.49) is an anthracycline cell cycle non-specific anticancer drug, which can inhibit DNA synthesis, interfere with RNA polymerase, and inhibit topoisomerase II. Its potency intensity is stronger than that of daunorubicin and doxorubicin. Mainly used for the treatment of acute non-lymphocytic leukemia, advanced breast cancer, but also for the treatment of myelodysplastic syndrome and non-Hodgkin's lymphoma. [0003] Currently, anti-tumor antibiotics, including idarubicin, must be administered in large doses of chemotherapeutic drugs in order to achieve effective therapeutic levels at the tumor site, but systemic administration of large doses may damage healthy normal cells and c...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/54A61K47/55A61K9/51A61K47/26A61K31/704A61P35/02A61P35/00
CPCA61K47/6929A61K47/549A61K47/55A61K9/5123A61K31/704A61P35/02A61P35/00
Inventor 王力源王萌
Owner BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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