Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Medicine containing epirubicin, preparation method thereof, pharmaceutical composition and application thereof

A technology of epirubicin and drugs, which is applied in the field of medicine, can solve the problem of the small molecule drug epirubicin delivery reliability, the limited clinical application of epirubicin drugs, the contradiction between toxicity and transfection activity, and the difficulty of connection Poison 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
View PDF4 Cites 0 Cited by
  • 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 epirubicin is one of the difficulties in solving the current limited clinical application of epirubicin.

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Medicine containing epirubicin, preparation method thereof, pharmaceutical composition and application thereof
  • Medicine containing epirubicin, preparation method thereof, pharmaceutical composition and application thereof
  • Medicine containing epirubicin, preparation method thereof, pharmaceutical composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0160] According to the second aspect of the present application, there is also provided a method for preparing the above-mentioned epirubicin-containing medicine, comprising the following steps: providing any of the above-mentioned nucleic acid nanoparticles; by means of physical connection and / or covalent connection The epirubicin is mounted on the nucleic acid nanoparticles to obtain the epirubicin-containing medicine.

[0161] When physically linked, epirubicin is usually physically intercalated between GC base pairs. When the connection is made by covalent connection, epirubicin usually chemically reacts with the amino group outside the G ring to form a covalent connection. The epirubicin-containing medicine prepared by the above-mentioned method can have better targeting ability after being modified by the target head, can deliver epirubicin stably, and has high reliability.

[0162] In a preferred embodiment, the step of mounting epirubicin by physical connection inclu...

Embodiment 1

[0184] 1. RNA and DNA nanoparticle carriers:

[0185] (1) The base sequences of the three polynucleotides constituting the RNA nanoparticles are shown in Table 1:

[0186] Table 1:

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

[0188]

[0189] 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.

[0190] The a, b and c chains of the above RNA nanoparticles and DNA nanoparticles were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0191] Second, the self-assembly experimental steps:

[0192] (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;

[0193] (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 a...

Embodiment 2

[0204] 1. 7 groups of short-sequence RNA nanoparticle carriers:

[0205] (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:

[0206] Table 2: R-1

[0207]

[0208]

[0209] Table 3: R-2

[0210]

[0211] Table 4: R-3

[0212]

[0213] Table 5: R-4

[0214]

[0215]

[0216] Table 6: R-5

[0217]

[0218] Table 7: R-6

[0219]

[0220] Table 8: R-7

[0221]

[0222]

[0223] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0224] Second, the self-assembly experimental steps:

[0225] (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;

[0226] (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 / mi...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
Login to View More

Abstract

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

Description

technical field [0001] The present application relates to the field of medicine, in particular, to a medicine containing epirubicin, its preparation method, pharmaceutical composition and application. Background technique [0002] Epirubicin (Epirubicin, CSA: 56420-45-2, molecular formula: C 27 H 29 NO 11 .HCI, molecular weight: 580.0) is an anti-tumor antibiotic and an isomer of doxorubicin. Its mechanism of action is to directly intervene between DNA nucleic acid base pairs, interfere with the transcription process, prevent the formation of mRNA, and thereby inhibit DNA , RNA and protein synthesis. It is a cell cycle non-specific drug that is effective against a variety of transplanted tumors, including acute leukemia and malignant lymphoma, breast cancer, bronchial lung cancer, ovarian cancer, Wilms tumor, soft tissue sarcoma, liver cancer (including primary hepatic cell carcinoma and metastatic carcinoma) and a variety of solid tumors such as medullary thyroid carcin...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/69A61K47/54A61K31/704A61P35/02A61P35/00
CPCA61K47/6929A61K47/549A61K31/704A61P35/02A61P35/00
Inventor 王力源王萌
Owner BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com