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Anti-tumor targeted drug sustained-release carrier, preparation and preparation method thereof

A slow-release carrier and slow-release preparation technology, which can be used in anti-tumor drugs, drug combinations, drug delivery, etc., and can solve problems such as intolerance, patients with toxic side effects, and lack of targeting.

Inactive Publication Date: 2021-01-05
杭州鹿扬科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In clinical treatment, the low toxicity and high efficiency of drugs have always been the focus of people's research. Chemotherapy is the main means of clinical treatment of tumors, but the current common dosage forms of traditional chemotherapy drugs lack targeting. Normal cells produce toxicity, causing toxic side effects that patients cannot tolerate

Method used

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  • Anti-tumor targeted drug sustained-release carrier, preparation and preparation method thereof
  • Anti-tumor targeted drug sustained-release carrier, preparation and preparation method thereof
  • Anti-tumor targeted drug sustained-release carrier, preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0035] Embodiment 1 The preparation method of anti-tumor targeting drug sustained-release carrier

[0036] S1. Preparation of polyphosphate-amino acid copolymer: 1g of alanine, 0.5g of tyrosine, 0.1g of caprolactam, 20mL of deionized water and 0.01g of 1-(3-dimethylaminopropyl)-3-ethyl Add carbodiimide into the reactor, raise the temperature to 180°C under the protection of nitrogen, the reaction time is 0.5h, continue to heat up to 200°C, the reaction time is 1h, then add 0.5g adenosine cyclic phosphate to react for 0.5h, stop Reaction, to be cooled to room temperature to obtain polyphosphate-amino acid copolymer; figure 1 shown;

[0037] S2. Configuration of polylactic acid-glycolic acid copolymer solution: weigh 1g of polylactic acid-glycolic acid copolymer, dissolve it in 10mL carbon tetrachloride, and use it as the oil phase;

[0038] S3. Preparation of amphiphile compound: Dissolve 1g of polyphosphate-amino acid copolymer in 10mL of dichloromethane, react for 2h under ...

Embodiment 2

[0041] Example 2 The preparation method of anti-tumor targeted drug sustained-release carrier

[0042] S1. Preparation of polyphosphate-amino acid copolymer (PPE-AA): 1g alanine, 1.2g tyrosine, 0.5g caprolactam, 20mL deionized water and 0.05g dicyclohexylcarbodiimide were added to the reaction In the container, under the protection of nitrogen, the temperature was raised to 200°C, the reaction time was 2h, the temperature was continued to 220°C, the reaction time was 4h, then 0.7g adenosine cyclic phosphate was added to react for 1h, the reaction was stopped, and the polyphosphate was obtained after cooling to room temperature - amino acid copolymers;

[0043] S2. Configuration of polylactic-co-glycolic acid (PLGA) solution: take 1g of poly-lactic-co-glycolic acid, dissolve it in 10mL of dichloromethane, and use it as the oil phase;

[0044] S3. Preparation of amphiphile compound (PPE-AA-PLGA): 1g of polyphosphate-amino acid copolymer was dissolved in 10mL of dichloromethane,...

Embodiment 3

[0048] The difference between this example and Example 2 is that the volume of deionized water added in step S5 in Example 1 is 50 times that of ethyl acetate.

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Abstract

The invention provides an anti-tumor targeted drug sustained-release carrier, a preparation and a preparation method thereof. The preparation method comprises the following steps: S1, preparing a polyphosphoester and amino acid copolymer; S2, preparing a polylactic acid and glycolic acid copolymer solution; S3, preparing an amphiphilic compound; S4, preparing an amphiphilic compound connected witha targeting molecule; and S5, preparing the nano microspheres. The drug selectivity and positioning accuracy are greatly improved through the anti-tumor targeted drug sustained-release carrier, antitumor drugs are released after enzyme hydrolysis, cancer cells are efficiently killed, the drug effect is improved, the sustained release preparation can effectively avoid the blood concentration peakvalue after drug taking, the blood concentration is controlled to be in a stable curve, and the drug effect durability is improved.

Description

technical field [0001] The invention relates to the technical field of sustained-release drugs, in particular to a sustained-release carrier for anti-tumor targeted drugs, a preparation and a preparation method thereof. Background technique [0002] Antitumor drugs are highly toxic and are easily hydrolyzed in the body. After an effective dose of the drug is applied, the blood drug level of the patient rises, and then drops rapidly to zero after reaching the maximum value. As a result, the drug has not yet reached the tumor cell tissue, and the drug effect has already been reached. Not much left. The emergence of antineoplastic drug sustained and controlled release preparations has improved the above situation. Antineoplastic drug sustained and controlled release preparations have overcome the shortcomings of traditional antineoplastic drugs such as short half-life, difficulty in maintaining effective concentration for a long time, and lack of targeting. Gel, microspheres, ...

Claims

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Application Information

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IPC IPC(8): A61K47/59A61K47/60A61K47/54A61K47/24A61K47/69A61K31/704A61K31/7068A61P35/00C08G69/42C08G81/00
CPCA61K31/704A61K31/7068A61K47/24A61K47/545A61K47/593A61K47/605A61K47/6925A61P35/00C08G69/42C08G81/00
Inventor 不公告发明人
Owner 杭州鹿扬科技有限公司
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