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Drug containing tacrine, preparation method for drug, pharmaceutical composition and application of drug

A tacrine and drug technology, applied in the field of its preparation, tacrine-containing drugs, can solve the problems of self-design contradiction between toxicity and transfection activity, difficult connection, non-toxic degradation, difficult to ensure targeting groups, etc.

Active Publication Date: 2020-04-07
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 tacrine is one of the difficulties in solving the current limited clinical application of tacrine.

Method used

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  • Drug containing tacrine, preparation method for drug, pharmaceutical composition and application of drug
  • Drug containing tacrine, preparation method for drug, pharmaceutical composition and application of drug
  • Drug containing tacrine, preparation method for drug, pharmaceutical composition and application of drug

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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 tacrine-containing drug, which includes the following steps: providing any nucleic acid nanoparticle described above; Tacrine is mounted on nucleic acid nanoparticles to obtain tacrine-containing medicines.

[0155] When physically linked, tacrine is usually intercalated between GC base pairs by physical intercalation. When the covalent link is used for linking, tacrine usually reacts with the amino group outside the G ring to form a covalent link. The drug containing tacrine prepared by the above method can have better targeting after the target head is modified, and can stably deliver tacrine with high reliability.

[0156] In a preferred embodiment, the step of mounting tacrine through physical connection includes: mixing and stirring tacrine, nucleic acid nanoparticles and the first solvent to obtain a premixed system; precipitating the premixed system...

Embodiment 1

[0177] 1. RNA and DNA nanoparticle carriers:

[0178] (1) The base sequences of the three polynucleotides that make up the RNA nanoparticles are shown in Table 1:

[0179] Table 1:

[0180]

[0181] (2) Three polynucleotide base sequences of DNA nanoparticles

[0182] 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.

[0183] The a, b, and c strands of the above-mentioned RNA nanoparticles and DNA nanoparticles were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0184] 2. Self-assembly experimental steps:

[0185] (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;

[0186] (2) Heat the mixed solution to 80°C / 95°C (the RNA assembly temperature is 80°C, and the DNA assembly temperature is 95°...

Embodiment 2

[0197] 1. Seven groups of short-sequence RNA nanoparticle carriers:

[0198] (1) See Table 2 to Table 8 for the base sequences of the three polynucleotides that make up the RNA nanoparticles in seven groups:

[0199] Table 2: R-1

[0200]

[0201] Table 3: R-2

[0202]

[0203] Table 4: R-3

[0204]

[0205] Table 5: R-4

[0206]

[0207] Table 6: R-5

[0208]

[0209] Table 7: R-6

[0210]

[0211] Table 8: R-7

[0212]

[0213] The single strands of the above seven groups of short-sequence RNA nanoparticle carriers were all synthesized by Sangon Bioengineering (Shanghai) Co., Ltd.

[0214] 2. Self-assembly experimental steps:

[0215] (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;

[0216] (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;

[0217] (3) Load the product onto an 8% (m / v) non-denat...

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Abstract

The application provides a drug containing tacrine, a preparation method for the drug, a pharmaceutical composition and application of the drug. The drug comprises a nucleic acid nanoparticle and thetacrine, and the tacrine is deposited on the nucleic acid nanoparticle; the nucleic acid nanoparticle includes a nucleic acid domain; the nucleic acid domain includes an a sequence, a b sequence and ac sequence; the a sequence includes an a1 sequence or a sequence of insertion, deletion or substitution of at least one base of the a1 sequence; the b sequence includes a b1 sequence or a sequence ofinsertion, deletion or substitution of at least one base of the b1 sequence; and the c sequence includes a c1 sequence or a sequence of insertion, deletion or substitution of at least one base of thec1 sequence. After the nucleic acid domain is modified by a target head, the drug containing the tacrine has a relatively good targeting property, can stably deliver the tacrine, and has very high reliability.

Description

technical field [0001] The present application relates to the field of medicine, in particular to a drug containing tacrine, its preparation method, pharmaceutical composition and application. Background technique [0002] Alzheimer's disease (Alzheimer's disease) is a neurodegenerative disease, clinically manifested as degenerative loss of memory and cognitive function. At present, Alzheimer's disease has become one of the major diseases that threaten human health and quality of life. Finding effective drugs and treatment strategies for Alzheimer's disease has become an urgent problem to be solved in the entire medical field around the world. [0003] Tacrine is the world's first marketed drug for the treatment of Alzheimer's disease by inhibiting the activity of acetylcholinesterase. Acetylcholinesterase inhibition has the most treated cases and the most affirmed curative effect. Therefore, although its clinical application is limited due to hepatotoxicity, research on t...

Claims

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Application Information

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IPC IPC(8): A61K31/473A61K47/54A61K47/69A61K9/51A61K47/26A61P25/28
CPCA61K31/473A61K47/549A61K47/6929A61K9/5123A61P25/28
Inventor 王力源王萌
Owner BAI YAO ZHI DA BEIJING NANOBIO TECH CO LTD
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