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Cytarabine-containing medicine, and preparation method, pharmaceutical composition and an application thereof

A cytarabine and drug technology, applied in the field of preparation of cytarabine-containing drugs, can solve the problems of difficult connection, non-toxic degradation, influence, toxicity and self-design contradiction of transfection activity, etc.

Active Publication Date: 2020-04-24
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 cytarabine is one of the difficulties in solving the current limited clinical application of cytarabine drugs.

Method used

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  • Cytarabine-containing medicine, and preparation method, pharmaceutical composition and an application thereof
  • Cytarabine-containing medicine, and preparation method, pharmaceutical composition and an application thereof
  • Cytarabine-containing medicine, and preparation method, pharmaceutical composition and an 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 cytarabine-containing drug, which includes the following steps: providing any one of the above-mentioned nucleic acid nanoparticles; by means of physical connection and / or covalent connection The cytarabine is mounted on the nucleic acid nanoparticles to obtain the cytarabine-containing drug.

[0155] When physically linked, cytarabine is usually intercalated between GC base pairs by physical intercalation. In the case of covalent linkage, cytarabine usually undergoes a chemical reaction with the amino group outside the G ring to form a covalent linkage. The drug containing cytarabine prepared by the above method can have better targeting after the target head is modified, and can stably deliver cytarabine with high reliability.

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

Embodiment 1

[0180] 1. RNA and DNA nanoparticle carriers:

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

[0182] Table 1:

[0183]

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

[0185] 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.

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

[0187] 2. Self-assembly experimental steps:

[0188] (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;

[0189] (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)...

Embodiment 2

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

[0201] (1) The base sequences of the three polynucleotides of the seven groups of RNA nanoparticles are shown in Table 2 to Table 8:

[0202] Table 2: R-1

[0203]

[0204]

[0205] Table 3: R-2

[0206]

[0207] Table 4: R-3

[0208]

[0209] Table 5: R-4

[0210]

[0211]

[0212] Table 6: R-5

[0213]

[0214] Table 7: R-6

[0215]

[0216] Table 8: R-7

[0217]

[0218] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0219] 2. Self-assembly experimental steps:

[0220] (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;

[0221] (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;

[0222] (3) Load the product onto an...

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Abstract

The invention provides a cytarabine-containing medicine, and a preparation method, a pharmaceutical composition and an application thereof. The medicine comprises a nucleic acid nanoparticle and cytarabine, and the cytarabine is loaded on the nucleic acid nanoparticle; and the nucleic acid nanoparticle comprises a nucleic acid structural domain, the nucleic acid structural domain comprises a sequence a, a sequence b and a sequence c, the sequence a comprises a sequence a1 or a sequence obtained by inserting, deleting or substituting at least one base in the sequence a1, the sequence b comprises a sequence b1 or a sequence obtained by inserting, deleting or substituting at least one base in the sequence b1, and the sequence c comprises a sequence c1 or a sequence obtained by inserting, deleting or substituting at least one base in the sequence c1. After the nucleic acid structural domain is modified with a target head, the cytarabine-containing medicine has a good targeting property, can stably deliver the cytarabine, and has a very high reliability.

Description

technical field [0001] The present application relates to the field of medicine, in particular, to a drug containing cytarabine, its preparation method, pharmaceutical composition and application. Background technique [0002] Cytarabine was first synthesized in 1959 by Richard Walwick, Walden Roberts and Charles Dekker at the University of California, Berkeley. The U.S. Food and Drug Administration approved cytarabine to enter the market in June 1969; it was originally sold by Upjohn under the trade name Cytosar-U. Hence the name "cytarabine". Normally, cytosine combines with another sugar (deoxyribose) to form deoxycytidine, one of the components of DNA. However, some polyporia organisms can combine arabinose and cytosine to form another compound (not a component of DNA), and this compound, cytarabine, has been found in these organisms. Cytarabine is so similar to deoxycytidine that it can be incorporated into human DNA instead of the latter, yet the structural differen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/54A61K47/69A61K9/51A61K47/26A61K31/7068A61P35/00A61P35/02
CPCA61K47/549A61K47/6929A61K9/5123A61K31/7068A61P35/00A61P35/02
Inventor 王力源王萌
Owner BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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