Biodegradable unsaturated polyphosphate, preparation and use method thereof

A polyphosphate and biodegradation technology, which is applied to non-active ingredients in medical preparations, drug combinations, pharmaceutical formulations, etc., can solve problems such as difficulty in filling and repairing

Inactive Publication Date: 2009-04-08
HUAZHONG UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The purpose of the present invention is to overcome the disadvantage that the existing polyphosphate materials need to be formed in vitro, and at the same time solve the defect th

Method used

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  • Biodegradable unsaturated polyphosphate, preparation and use method thereof
  • Biodegradable unsaturated polyphosphate, preparation and use method thereof
  • Biodegradable unsaturated polyphosphate, preparation and use method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0078] Embodiment 1: the synthesis of unsaturated polyphosphate-P(BPGF-EDP)

[0079] Add 116.07 grams (1.0 mol) of fumaric acid, 63.89 grams (1.1 mol) of propylene oxide and 0.79 grams (0.01 mol) of pyridine in the reaction kettle, replace the air in the kettle with nitrogen, raise the temperature to 40 ° C and stir the reaction. React under these conditions for about 8 hours, the pressure in the reactor is reduced to 0.12MPa, the temperature is raised to 90°C, and the excess propylene oxide is evaporated after continuing the reaction for 1 hour to obtain light yellow oily fumaric acid bis(1,2- propylene glycol) esters.

[0080] 92.9g (0.4mol) bis(1,2-propanediol) fumarate (BPGF) was dissolved in 1500ml dry methylene chloride, added in the reaction flask, started stirring, added 89.0g (0.88mol) of triethylamine, Nitrogen protection. The reaction bottle was placed in an ice-water bath, and under rapid stirring, 65.2 g (0.40 mol) of ethyl dichlorophosphate (EDP) dissolved in 2...

Embodiment 2

[0083] Embodiment 2: the synthesis of unsaturated polyphosphate-P(BEGF-EDP)

[0084] Add 116.07 grams (1.0 mol) of fumaric acid and 0.79 grams (0.01 mol) of pyridine into the reaction kettle, replace the air in the kettle with nitrogen, add 48.4 grams (1.1 mol) of ethylene oxide, raise the temperature to 40 ° C and stir Reaction, react under this condition for about 8 hours, the pressure in the reactor is reduced to 0.28MPa, be warmed up to 90 ℃, continue to react after 1 hour and steam the excessive oxirane, obtain light yellow oily fumaric acid bis(1 , 2-ethylene glycol) ester.

[0085] 81.0g (0.4mol) of bis(1,2-ethylene glycol) fumarate (BPGF) was dissolved in 1500ml of dry dichloromethane, added to the reaction flask, started to stir, and 89.0g (0.88mol) of triethylamine was added ), nitrogen protection. The reaction bottle was placed in an ice-water bath, and under rapid stirring, 65.2 g (0.40 mol) of ethyl dichlorophosphate (EDP) dissolved in 200 ml of dichloromethane ...

Embodiment 3

[0086] Embodiment 3: two (1,2-propanediol) fumarates - the synthesis of phenyl dichlorophosphate polymer

[0087] Except that phenyl dichlorophosphate monomer is used to replace ethyl dichlorophosphate monomer, the synthesis and separation method described in Example 1 is used to prepare bis(1,2-propanediol) fumarate-phenyl dichlorophosphate polymer .

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Abstract

The invention relates to a biodegradable unsaturated polyphosphate ester containing phosphate ester and fumarate ester bonds and discloses a preparation method of the polyphosphate ester and a method for the application of the polyphosphate ester as a medical sustained release preparation for injecting into a treated part and as a hard tissue repair and filling material. The mixture composed of the polyphosphate ester, a cross-linking vinyl monomer, a free radical thermal initiator or photo initiator being capable of initiating or assist in initiating covalent cross-linking reaction and biologically active drugs has excellent medical sustained release effect and no toxic side effects. As a material for repairing the defects of osseous tissue, the biodegradable unsaturated polyphosphate ester can stimulate the formation of new bones; and the material can also be degraded gradually and finally be substituted by a new bone completely. The biodegradable unsaturated polyphosphate ester has outstanding biocompatibility and no obvious inflammation reactions and teratogenesis.

Description

technical field [0001] The present invention relates to a biodegradable unsaturated polyphosphate ester and its preparation and application method, in particular to an unsaturated polyester containing phosphate ester and fumarate bonds in the polymer skeleton and its preparation and application method. technical background [0002] The biomedical polymer materials used in the treatment of bone defects and drug release systems must have good biocompatibility, including the polymer itself and its degradation products, which should be non-toxic and non-teratogenic to the body. Degradable biomedical polymers are used in implanted medical devices and drug release systems. After the device completes the intended function, it can be decomposed into small molecules and fragments through hydrolysis or enzymolysis, and finally absorbed or excreted by the body, eliminating the need for The pain caused by the second surgery to remove it. [0003] Because of its structural similarity t...

Claims

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Application Information

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IPC IPC(8): C08G79/04A61K47/34A61P3/10A61P31/00A61P35/00A61L27/18
Inventor 邱进俊刘承美何钊煊
Owner HUAZHONG UNIV OF SCI & TECH
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