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Phytoagglutinin modified lactic acid-hydroxacetic acid copolymer and its preparing method

A technology of glycolic acid copolymer and plant lectin, which is applied in the field of medicine to achieve the effects of improving oral bioavailability, prolonging residence time, and simple reaction process

Inactive Publication Date: 2010-12-29
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

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Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Synthesis of Lactic Acid-Glycolic Acid Copolymer Modified by Wheat Germ Agglutinin

[0013] Dissolve 20 mg of PLGA, 5 mg of EDC, and 5 mg of NHS with a molecular weight of 10,000 and a molar ratio of 50:50 in 1 ml of dimethyl sulfoxide, stir and react at room temperature for 2 hours, add a large amount of water, precipitate appears, filter, collect the precipitate, and obtain PLGA-NHS; WGA 10mg and PLGA-NHS 10mg were dissolved in a mixed solvent of 3ml water and acetone (volume ratio 5:1), reacted at 4°C for 24h, the reaction mixture was filtered to remove the precipitate, the filtrate was placed in a dialysis bag for dialysis, and the dialysis solution, freeze-dried to obtain the product wheat germ agglutinin modified lactic acid-glycolic acid copolymer (PLGA-WGA).

Embodiment 2

[0015] Synthesis of Lactic Acid-Glycolic Acid Copolymer Modified by Wheat Germ Agglutinin

[0016] Dissolve 50 mg of PLGA, 10 mg of EDC, and 10 mg of NHS with a molecular weight of 80,000 and a molar ratio of 40:60 in 1.5 ml of N,N-dimethylformamide, stir and react at room temperature for 4 hours, add a large amount of water, precipitate appears, filter, collect the precipitate, and obtain PLGA -NHS; wheat germ agglutinin (WGA) 10mg, PLGA-NHS 20mg were dissolved in a mixed solvent of 6ml water and dichloromethane (volume ratio 1:2), reacted at 4°C for 24h, the reaction mixture was filtered to remove the precipitate, and the filtrate was dialyzed Dialyze in the bag, take out the dialysate, and freeze-dry to obtain the product wheat germ agglutinin-modified lactic acid-glycolic acid copolymer (PLGA-WGA).

Embodiment 3

[0018] Synthesis of Lactic-Glycolic Acid Copolymer Modified by Asparagus Pea Lectin

[0019] Dissolve 20 mg of PLGA, 5 mg of EDC, and 5 mg of NHS with a molecular weight of 10,000 and a molar ratio of 50:50 in 1 ml of dimethyl sulfoxide, stir and react at room temperature for 2 hours, add a large amount of water, precipitate appears, filter, collect the precipitate, and obtain PLGA-NHS; Tianmen Winter pea agglutinin (AL) 10 mg, PLGA-NHS 10 mg were dissolved in a mixed solvent of 2 ml of water and tetrahydrofuran (volume ratio 1:1), and reacted at 4°C for 24 hours. The reaction mixture was filtered to remove the precipitate, and the filtrate was dialyzed in a dialysis bag. The dialysate was freeze-dried to obtain the product asparagus pea lectin-modified lactic acid-glycolic acid copolymer (PLGA-AL).

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Abstract

The present invention discloses phytoagglutinin modified lactic acid-hydroxyacetic acid copolymer with specific adhesion to prolong the retention time or preparation in gastrointestinal tract obviously and raise the bioavailability of orally taken medicine greatly. The polymer consists of biodegradable material lactic acid-hydroxyacetic acid copolymer and bioadhesive material phytoagglutinin. Thephytoagglutinin modified lactic acid-hydroxyacetic acid copolymer is prepared through dissolving lactic acid-hydroxyacetic acid copolymer, 1-ethyl-3-carbodimide and N-hydroxy succinimide in non-proton type polar solvent, and reaction at room temperature via stirring for 2-12 hr; adding water, filtering and collecting precipitate to obtain PLGA-NHS; dissolving phytoagglutinin and PLGA-NHS in mixedsolvent of water and non-proton type polar solvent, filtering the reacted mixture, taking the dialysate, and freeze drying to obtain the phytoagglutinin modified lactic acid-hydroxyacetic acid copolymer.

Description

Technical field: [0001] The invention relates to the technical field of medicine, specifically a lectin-modified lactic acid-glycolic acid copolymer, a preparation method thereof and an application in preparation. Background technique: [0002] Biodegradable lactic acid-glycolic acid copolymer (PLGA) is a synthetic pharmaceutical polymer material approved by the US FDA for clinical use. Since the 1970s, it has been used as medical surgical sutures and injection microspheres, nanoparticles, and Materials such as implants are widely used. The copolymer can be gradually degraded into lactic acid and glycolic acid in the body, and finally converted into carbon dioxide and water through the tricarboxylic acid cycle. It has no accumulation problem in the human body, and is safe and non-toxic. Due to its good tissue compatibility and biodegradability, adjustable degradation rate and excellent encapsulation performance, lactic acid-glycolic acid copolymer has become the best choice...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K47/42A61K9/50A61K9/14A61K47/34
Inventor 尹雅姝陈大为
Owner SHENYANG PHARMA UNIVERSITY