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A kind of anti-drug abuse pva-g-mpeg graft polymer and preparation method thereof

A graft polymer and drug technology, applied in the field of PVA-g-mPEG graft polymer and its preparation, can solve the problems of high technical requirements required for process realization, complex, expensive, dangerous, and difficult catalytic system, and the like. The preparation method has the advantages of simple process, stable and reliable preparation process, and the effect of preventing the abuse of intravenous injection

Active Publication Date: 2022-05-24
安徽安生生物化工科技有限责任公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0006] Due to its unique performance, PEO has been widely used in the development of ADFs. However, the preparation conditions of high molecular weight PEO are relatively harsh, the catalytic system is complex, expensive or dangerous, and the technical requirements for process realization are high and difficult. Its market Basically monopolized by European, American and Japanese companies such as the Dow Chemical Company of the United States

Method used

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  • A kind of anti-drug abuse pva-g-mpeg graft polymer and preparation method thereof
  • A kind of anti-drug abuse pva-g-mpeg graft polymer and preparation method thereof
  • A kind of anti-drug abuse pva-g-mpeg graft polymer and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Pour 50g mPEG (Mw=4000) into a four-necked flask equipped with a mechanical stirrer, a thermometer and a reflux condenser, and add 0.4g BF to the flask at 55°C 3 -Et 2 O, 3.92mL ECH, react for 5h, then remove excess ECH by rotary evaporation to obtain mPEG-Cl.

[0032] 23.5g mPEG-Cl and 100g 8% (w / w) PVA-1788 aqueous solution were stirred evenly, then at 90°C, 12mL of 10% (w / w) NaOH aqueous solution was added, and the reaction was stirred for 5h. The solution was adjusted to neutrality with hydrochloric acid, and mPEG-Cl was eluted with ethanol precipitation to obtain a crude product of PVA-g-mPEG grafted polymer. The crude product was vacuum dried at 50°C to obtain the PVA-g-mPEG grafted polymer.

Embodiment 2

[0034] 10.93g mPEG-Cl and 100g 8% (w / w) PVA-1788 aqueous solution were stirred uniformly, then 12mL 10% (w / w) NaOH aqueous solution was added, and the reaction was continued at 70°C for 10h. After the reaction, the solution was adjusted to neutrality with hydrochloric acid, and the unreacted side chain mPEG-Cl was extracted with acetone soxhlet to obtain the crude product of PVA-g-mPEG grafted polymer. Then, it was thoroughly dialyzed with purified water (dialysis in a 2L container for 60h, water was changed every 12h) to remove small molecule NaCl, and vacuum dried at 50°C to obtain the purified PVA-g-mPEG grafted polymer.

Embodiment 3

[0036] Pour 50 g of mPEG (Mw=1000) into a four-necked flask equipped with a mechanical stirrer, thermometer and reflux condenser. Add 0.3 g BF to the flask at 70 °C 3 -Et 2 O, 5.88mL ECH, react for 3h. Excess ECH was then removed by rotary evaporation to give mPEG-Cl.

[0037]Take 55 mL of the 10% (w / v) aqueous solution of the above-prepared mPEG-Cl intermediate, add 50 g of 8% (w / w) PVA-1788 aqueous solution to the four-necked flask, stir evenly, and add 12 mL of 10% (w / w) NaOH aqueous solution, reacted at 70°C for 10h. After the reaction, the solution was adjusted to neutrality with hydrochloric acid, and the unreacted side chain mPEG-Cl was extracted with acetone soxhlet to obtain the crude product of PVA-g-mPEG grafted polymer. Then, it was thoroughly dialyzed with purified water (dialysis in a 2L container for 60 hours, and the water was changed every 12 hours) to remove small molecules of NaCl, and the purified PVA-g-mPEG graft polymer was obtained by vacuum drying a...

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Abstract

The invention discloses a drug abuse-resistant PVA-g-mPEG graft polymer and a preparation method thereof, and relates to the technical field of polymer materials. The invention successfully prepares a novel structure of PVA-g-mPEG through molecular design Graft polymer, the graft polymer is prepared by the etherification reaction between mPEG whose terminal hydroxyl group is epichlorohydrinated and PVA under alkaline conditions. The preparation method is simple, the preparation process is stable and reliable, and the raw materials used are also abundant. It is easy to get; and the grafted polymer can effectively prevent the extraction of drugs in water by forming a gel in contact with water, thereby preventing drug abuse through intravenous injection. It is an innovative potential excipient for developing anti-abuse preparations, and provides a new method for anti-abuse research. train of thought.

Description

Technical field: [0001] The invention relates to the technical field of polymer materials, in particular to a PVA-g-mPEG graft polymer for preventing drug abuse and a preparation method thereof. Background technique: [0002] Despite the widespread safety and addictive nature of opioid painkillers, the need for pain relief is growing. According to the survey, the global painkillers market size was US$71 billion in 2019 and is expected to grow to US$92 billion by 2027. The painkiller market in China is relatively small, about US$530 million in 2017, and is mostly used for surgical pain relief. [0003] Drug abusers produce euphoria by tampering with the drug product and changing the dosage form to make it suitable for abusive routes of administration, such as high-dose oral or chewing, nasal vaping or powder, intravenous injection, etc. Tablets and solvent extract active ingredients. [0004] Due to the growing problem of opioid abuse, abuse prevention formulations (ADFs) ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08G81/02A61K47/32
CPCC08G81/025A61K47/32
Inventor 李凤和杨璐姚日生李效文罗浩边侠玲
Owner 安徽安生生物化工科技有限责任公司
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