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Preparation method for pH controlled releasedynamic polymer packaging system

A controlled release and polymer technology, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, drug combinations, etc., can solve the problem of abnormal rapidity, uncontrollable release, and difficulty in dissociation, etc. problems, to achieve the effect of broad application prospects

Inactive Publication Date: 2009-01-14
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, although the above-mentioned self-assembly system can change the assembly morphology under the regulation of solution pH value, salt and other factors (Jiang Ming, A. Eisenberg, Liu Guojun, Zhang Xi et al., Macromolecular Self-Assembly, 2006, Science Press), but because its polymer molecular chains are all strongly covalently linked, in an aqueous solution system, this type of encapsulation system is relatively stable, not easy to dissociate, and cannot effectively release the encapsulated small organic molecules; On the one hand, in the case of encountering a compatible solvent, the release of the encapsulated small molecule becomes extremely rapid, which fails to achieve the purpose of controlled release

Method used

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  • Preparation method for pH controlled releasedynamic polymer packaging system
  • Preparation method for pH controlled releasedynamic polymer packaging system
  • Preparation method for pH controlled releasedynamic polymer packaging system

Examples

Experimental program
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Effect test

Embodiment 1

[0033] Step 1: Add 7 grams of styrene monomer, 1.25 grams of benzyl bromide, 0.5 grams of cuprous bromide and 2 grams of bipyridyl into a 50-ml flask, bubbling nitrogen gas for 30 minutes, sealing it, and putting it in 110°C oil In the bath, react for 3 hours. Add a small amount of tetrahydrofuran to dissolve it, throw it into a large amount of methanol for precipitation twice, and dry it in a vacuum oven at 50°C for 1 day to obtain polystyrene with a molecular weight of 2,000.

[0034] Step 2: Add 2 grams of anhydrous potassium carbonate and 1 gram of p-hydroxybenzaldehyde to the acetone solution of 3 grams of polystyrene obtained above, and reflux at 60° C. for 1 day. By filtering, concentrating the solution, precipitating a large amount of methanol three times, and drying in vacuum at 50° C., polystyrene with an aldehyde group at the end can be obtained.

[0035] Step 3: Dissolve 20 mg of the above polystyrene and 10 mg of hydrazide-terminated monomethyl polyethylene glyco...

Embodiment 2

[0039] Step 1: Add 7 grams of styrene monomer, 1.25 grams of benzyl bromide, 0.5 grams of cuprous bromide and 2 grams of bipyridyl into a 50-ml flask, bubbling nitrogen gas for 30 minutes, sealing it, and putting it in 110°C oil In the bath, react for 3 hours. Add a small amount of tetrahydrofuran to dissolve it, throw it into a large amount of methanol for precipitation twice, and dry it in a vacuum oven at 50°C for 1 day to obtain polystyrene with a molecular weight of 2,000.

[0040] Step 2: Add 2 grams of anhydrous potassium carbonate and 1 gram of p-hydroxybenzaldehyde to the acetone solution of 3 grams of polystyrene obtained above, and reflux at 60° C. for 1 day. By filtering, concentrating the solution, precipitating a large amount of methanol, and drying in vacuum at 50°C, polystyrene with aldehyde groups at the end can be obtained.

[0041] The third step: 20 mg of the above-mentioned polystyrene and 5 mg of monomethyl polyethylene glycol (molecular weight: 550) wit...

Embodiment 3

[0045] Step 1: Add 7 grams of styrene monomer, 0.5 grams of benzyl bromide, 0.5 grams of cuprous bromide and 2 grams of bipyridyl into a 50-ml flask, bubbling nitrogen gas for 30 minutes, sealing it, and putting it in 110°C oil In the bath, react for 3 hours. Add a small amount of tetrahydrofuran to dissolve it, throw it into a large amount of methanol for precipitation twice, and dry it in a vacuum oven at 50°C for 1 day to obtain polystyrene with a molecular weight of 3000.

[0046] Step 2: Add 2 g of anhydrous potassium carbonate and 0.8 g of p-hydroxybenzaldehyde to the acetone solution of 3 g of polystyrene obtained above, and reflux at 60° C. for 1 day. By filtering, concentrating the solution, precipitating a large amount of methanol, and drying in vacuum at 50°C, polystyrene with aldehyde groups at the end can be obtained.

[0047] Step 3: Dissolve 15 mg of the above polystyrene and 10 mg of monomethyl polyethylene glycol (molecular weight 2000) with a hydrazide bond ...

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Abstract

The invention relates to a preparation method of a dynamic polymer packaging system of pH regulation and release, which belongs to the chemical industry field. The invention is characterized in that hydrophobic polymer and hydrophilic polymer are linked to form a block dynamic copolymer by adopting dynamic chemical bond, through dissolving the dynamic copolymer and hydrophobic dye or drug molecule in co-solvent, and in the case that precipitator is slowly added, the solution of the polymer assembled body packaged with the dye or the drug molecule is formed. The preparation method of the invention can realize the controllable release of dyes or drug molecules with the regulation and the control of pH value, thus the preparation method has broad application prospect in the aspects of drug delivery and dye release.

Description

technical field [0001] The invention relates to a preparation method in the technical field of chemical engineering, in particular to a preparation method of a pH-regulated release dynamic polymer encapsulation system. Background technique [0002] Dynamic polymers refer to polymers linked by dynamic chemical bonds. Dynamic chemical bond is a kind of chemical bond proposed in recent years, and its bond energy is between covalent bond and non-covalent bond. Compared with covalent bonds, such chemical bonds have the characteristics of reversible formation / breaking under mild conditions; compared with non-covalent bonds, such chemical bonds are more stable. Acylhydrazone bond (-CO-NH-N=CH-), imine bond (-N=CH-), ester bond (-CO-O-), disulfide bond (-S-S-), etc. belong to dynamic chemical bonds scope. The current research based on reversible covalent bonds is progressing rapidly. For example, the French Nobel laureate Lehn et al. prepared covalent dynamic polymers based on ac...

Claims

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Application Information

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IPC IPC(8): C09B67/00C09B67/14C08L87/00C08K5/3467C08G81/02A61K47/34A61K31/337A61K31/704A61P35/00
Inventor 蒋逸朱琦石云峰朱新远颜德岳
Owner SHANGHAI JIAO TONG UNIV
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