Dihydroartemisinin-containing medicament, preparation method thereof, pharmaceutical composition and application of pharmaceutical composition

A technology of dihydroartemisinin and drug, applied in the field of medicine, can solve the problems of difficult to ensure targeting group, influence, difficult connection, non-toxicity and degradation, etc.

Active Publication Date: 2020-05-05
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 dihydroartemisinin is one of the difficulties in solving the current limited clinical application of dihydroartemisinin drugs

Method used

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  • Dihydroartemisinin-containing medicament, preparation method thereof, pharmaceutical composition and application of pharmaceutical composition
  • Dihydroartemisinin-containing medicament, preparation method thereof, pharmaceutical composition and application of pharmaceutical composition
  • Dihydroartemisinin-containing medicament, preparation method thereof, pharmaceutical composition and application of pharmaceutical composition

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Experimental program
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preparation example Construction

[0155] According to the second aspect of the present application, there is also provided a method for preparing the above-mentioned dihydroartemisinin-containing drug, which includes the following steps: providing any one of the above-mentioned nucleic acid nanoparticles; The method mounts dihydroartemisinin on nucleic acid nanoparticles to obtain dihydroartemisinin-containing drugs.

[0156] When physical linking is used, dihydroartemisinin is usually intercalated between GC base pairs by physical intercalation. In the case of covalent linkage, dihydroartemisinin usually undergoes a chemical reaction with the amino group outside the G ring to form a covalent linkage. The dihydroartemisinin-containing drug prepared by the above method can have better targeting after the target head is modified, can stably deliver dihydroartemisinin, and has high reliability.

[0157] In a preferred embodiment, the step of mounting dihydroartemisinin through physical connection includes: mixin...

Embodiment 1

[0180] 1. RNA and DNA nanoparticle carriers:

[0181] (1) The three polynucleotide base sequences that make up the RNA nanoparticles, see Table 1 for details:

[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) Seven groups of three polynucleotide base sequences that make up RNA nanoparticles:

[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] 2. Self-assembly experimental steps:

[0218] (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;

[0219] (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;

[0220] (3) Load the product onto an 8% (m / v) non-denaturing PAGE gel and purify the comple...

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Abstract

The invention provides a dihydroartemisinin-containing medicament, a preparation method thereof, a pharmaceutical composition and an application of the pharmaceutical composition. The medicament comprises nucleic acid nanoparticles and dihydroartemisinin, wherein the dihydroartemisinin is carried on the nucleic acid nanoparticles; the nucleic acid nanoparticles comprise a nucleic acid structural domain, wherein the nucleic acid structural domain comprises a sequence a, a sequence b and a sequence c; the sequence a comprises an a1 sequence or a sequence obtained by insertion, deletion or substitution of at least one base in the a1 sequence; the sequence b comprises a b1 sequence or a sequence obtained by insertion, deletion or substitution of at least one base in the b1 sequence; and the sequence c comprises a c1 sequence or a sequence obtained by insertion, deletion or substitution of at least one base in the c1 sequence. After the nucleic acid structural domain of the dihydroartemisinin-containing medicament provided by the invention is modified by a target head, the medicament can have better targeting property, can stably deliver dihydroartemisinin, and has high reliability.

Description

technical field [0001] The present application relates to the field of medicine, in particular, to a medicine containing dihydroartemisinin, its preparation method, pharmaceutical composition and application. Background technique [0002] Dihydroartemisinin (Dihydroartemisinin, referred to as DHA) is a derivative of artemisinin, which has significant anti-tumor activity. The balance state of intracellular iron element can kill tumor cells. Dihydroartemisinin is mainly used in the treatment of cancers such as liver cancer, ovarian cancer, lung cancer, pancreatic cancer, osteosarcoma and brain medulloblastoma. [0003] At present, antitumor antibiotics including dihydroartemisinin must be administered with large doses of chemotherapy drugs in order to achieve effective therapeutic levels at the tumor site, but large doses of systemic administration may damage healthy normal cells, in a series of Adverse reactions in tissues and organs. These adverse reactions include suppre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/357A61K47/54A61K47/69A61K9/51A61K47/26A61P35/00
CPCA61K31/357A61K47/549A61K47/6929A61K9/5123A61P35/00
Inventor 王力源王萌
Owner BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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