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Biodegradability hydrogel controlled-release preparation and its preparation method and application

A technology of biodegradable and controlled-release preparations, which is applied in the field of biodegradable hydrogel controlled-release preparations and its preparation, can solve the problems of restricting widespread use, reduce the rate of inactivation, avoid related problems, and reduce operating temperature Effect

Inactive Publication Date: 2008-10-15
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the preparation of physical hydrogels containing polylactic acid, hydrophilic and hydrophobic interactions are often used, but organic solvents are required in the preparation process, and the residue of organic solvents limits the wide application of the hydrogel system

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Add 22g of dihydroxy polyethylene glycol with a molecular weight of 6000, 12g of L-lactide (or dextro-lactide) and 46mg of zinc lactate into a 100ml reaction flask, seal the tube after vacuuming, and put it in the reaction box. After reacting at ℃ for 3 days, take it out, dissolve in dichloromethane, precipitate with anhydrous ether, and dry to constant weight in vacuum. The obtained samples are tested by nuclear magnetic resonance method to determine the L-polylactic acid and polyethylene glycol, and the right-handed polylactic acid and polyethylene glycol. The molar ratios of the repeating units of the alcohol are 1 / 3.9 and 1 / 3.9, respectively. The melting points are 54.9℃ and 54.8℃, and the glass transition temperatures are -52.0℃ and -50.2℃, respectively, as measured by differential thermal scanning calorimetry. Cold crystallization The temperatures are -32.6°C and -32.6°C, respectively. Dissolve 0.15 g of each of the two polymers in 1 ml of deionized water and stir uni...

Embodiment 2

[0022] Add 33g of dihydroxy polyethylene glycol with a molecular weight of 12000, 12g of L-lactide (or D-lactide) and 12mg of zinc lactate into a 100ml reaction flask, seal the tube after vacuuming, and put it in the reaction box. After reacting at ℃ for 8 days, take it out, dissolve with dichloromethane, precipitate with anhydrous ether, and dry to constant weight in vacuum. The obtained samples are determined by nuclear magnetic resonance method to determine the L-polylactic acid and polyethylene glycol, and the dextro-polylactic acid and polyethylene glycol. The molar ratios of the repeating units of alcohol are 1 / 8.5 and 1 / 8.0, respectively. The melting points are 59.2℃ and 55.6℃, and the glass transition temperatures are -57.9℃ and -56.4℃, respectively. Cold crystallization The temperatures are -46.6°C and -45.6°C, respectively. Dissolve 0.40 g of each of the two polymers in 1 ml of deionized water and stir evenly to prepare a solution with a concentration of 0.4 / ml. After fu...

Embodiment 3

[0024]Add 44g of dihydroxy polyethylene glycol with a molecular weight of 20000, 12g of L-lactide (or D-lactide), and 12mg of zinc lactate into a 100ml reaction flask, seal the tube after vacuuming, and put it in the reaction box. After reacting at ℃ for 1 day, take it out, dissolve in dichloromethane, precipitate with anhydrous ether, and dry to constant weight in vacuum. The obtained samples are tested by nuclear magnetic resonance method to determine the L-polylactic acid and polyethylene glycol, and the right-handed polylactic acid and polyethylene glycol. The molar ratios of the repeating units of the alcohol are 1 / 11.0 and 1 / 10.0, respectively. The melting points are 60.7℃ and 59.9℃, and the glass transition temperatures are -61.4℃ and -62.2℃, respectively, as measured by differential thermal scanning calorimetry. Cold crystallization The temperatures are -50.6°C and -50.3°C, respectively. Dissolve 0.20 g of each polymer in 1 ml of deionized water and stir evenly to prepare ...

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Abstract

The invention relates to a biodegradable hydrogel controlled release preparation and a preparation and an application thereof, belonging to the technology field of medicines. The preparation method comprises the steps of: synthesizing poly(lactic acid)-polyethylene glycol-poly(lactic acid) (PLA-PEG-PLA) triblock copolymer by inducing L-lactide and D-lactide to respectively conduct ring-expansion polymerization by using zinc powder, zinc lactate or stannous octoate as catalyst and polyethylene glycol (PEG) 2,000-20,000; respectively dissolving poly-L-lactic acid-polyethylene glycol-poly-L-lactic acid and poly-D-lactic acid-polyethylene glycol-poly-D-lactic acid in water to obtain solutions with concentration of 0.05-0.5g / mL, swelling, mixing, and allowing gelatinization under constant temperature to obtain PLA-PEG-PLA triblock copolymer hydrogel for injection by complexing reaction. The hydrogel has good biological compatibility and biodegradability, can be used for embedding water-soluble drugs, and is an ideal drug controlled release carrier.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a biodegradable hydrogel controlled-release preparation and a preparation method and application thereof. Background technique [0002] In recent years, with the development of medicine and biotechnology, the pharmaceutical industry has developed more and more products. Biologically active drugs such as peptides and proteins are gradually being synthesized. These drugs need a controlled release system to perform or perform better. utility. At the same time, the drug controlled release system has great potential for applications in cardiovascular diseases, respiratory diseases, analgesia, malignancies, immune system diseases, contraception, etc. that require long-term medication, large amounts of medication, drug toxicity or addiction. Some common digestive system drugs and anti-infective drugs are also suitable for the use of sustained and controlled release preparations. ...

Claims

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Application Information

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IPC IPC(8): A61K9/00C08G63/78C08G63/08C08J3/075C08L67/04
Inventor 李速明韦嘉张彦
Owner FUDAN UNIV
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