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PVA-g-mPEG graft polymer for preventing drug abuse and preparation method thereof

A technique of grafting polymers and drugs, which is applied in the field of PVA-g-mPEG grafting polymers and its preparation, can solve the problems of high technical requirements for process realization, complex, expensive, dangerous, and difficult catalytic systems, and achieve The preparation method has the advantages of simple process, stable and reliable preparation process, and the effect of preventing intravenous abuse

Active Publication Date: 2021-07-16
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

AI Technical Summary

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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  • PVA-g-mPEG graft polymer for preventing drug abuse and preparation method thereof
  • PVA-g-mPEG graft polymer for preventing drug abuse and preparation method thereof
  • PVA-g-mPEG graft polymer for preventing drug abuse and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

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

Embodiment 2

[0034] Stir 10.93g of mPEG-Cl and 100g of 8% (w / w) PVA-1788 aqueous solution evenly, then add 12mL of 10% (w / w) NaOH aqueous solution, and continue the reaction 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 thoroughly dialyzed with purified water (dialysis in a 2L container for 60 h, changing water every 12 h) to remove small molecule NaCl, and vacuum-dried at 50° C. to obtain 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, a thermometer and a reflux condenser. Add 0.3 g of BF to the flask at 70 °C 3 -Et 2 O, 5.88mL ECH, reacted for 3h. Excess ECH was then removed by rotary evaporation to obtain mPEG-Cl.

[0037]Take 55 mL of the 10% (w / v) aqueous solution of the mPEG-Cl intermediate prepared above, add it to a four-necked flask with 50 g of 8% (w / w) PVA-1788 aqueous solution, stir well and add 12 mL of 10% (w / w) NaOH aqueous solution, react 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 thoroughly dialyzed with purified water (dialysis in a 2L container for 60 h, changing the water every 12 h) to remove small molecule NaCl, and vacuum-dried at 50°C to obtain a purified PVA-g-mPEG grafted polymer.

[0038] Depe...

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Abstract

The invention discloses a PVA-g-mPEG graft polymer for preventing drug abuse and a preparation method thereof, and relates to the technical field of high polymer materials. The PVA-g-mPEG graft polymer with a novel structure is successfully prepared through molecular design. The graft polymer is prepared by carrying out etherification reaction on mPEG of which the terminal hydroxyl is epichlorohydrin and PVA under an alkaline condition, the preparation method is simple in process, the preparation process is stable and reliable, and the adopted raw materials are rich and easy to obtain. Moreover, the graft polymer can form gel when encountering water to effectively prevent extraction of drugs in water, so that the drugs are prevented from being abused through intravenous injection, and the graft polymer is an innovative potential auxiliary material for developing abuse prevention preparations and provides a new thought for research on abuse prevention.

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 widespread safety and addiction concerns with opioid painkillers, there is a growing need for pain relief. According to the survey, the global pain medication market size was US$71 billion in 2019 and is expected to grow to US$92 billion by 2027. China's painkiller market is relatively small, about US$530 million in 2017, and most of it is used for surgical pain relief. [0003] Drug abusers tamper with drug products and change dosage forms to make them suitable for abused administration routes, such as large doses of oral or chewing, sniffing smoke or powder, intravenous injection, etc., resulting in euphoria. The common operation methods mainly include crushing and grinding Tablets and solvent extracted active ingredients. [0004] Due to t...

Claims

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Application Information

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Patent Type & Authority Applications(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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