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Biodegradable high molecular gel medicine composition, its prepn. method and use thereof

A polymer gel and biodegradation technology, applied in the field of medical polymer materials, can solve the problems of low drug packaging rate, troublesome clinical application, and unsatisfactory biodegradable gel drug carrier, etc., and achieve the effect of large volume change range.

Inactive Publication Date: 2006-11-29
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Although the above biodegradable gels have their own characteristics, their common disadvantages are that the degradation rate is slow or only partially degradable, the drug inclusion rate is low, the drug release rate is fast, and the dosage is large during use, which not only causes troubles in clinical application. , but also increased treatment costs
Therefore, there is no satisfactory biodegradable gel drug carrier for clinical application so far.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1: 20g malic acid was mixed with 2g SnCl at 100°C and 100mmHg vacuum 2 For catalyst polycondensation for 120 hours, the resulting polymer was dissolved in tetrahydrofuran, filtered to remove SnCl 2 According to the ratio of malic acid unit: HEMA: DCC = 5: 1: 1.2, HEMA was grafted onto the side group of polymalic acid. The grafting reaction was carried out under stirring at -20°C, and the reaction time was 100 hours. The grafted solution was filtered, and the filtrate was concentrated, precipitated in ether, and dried under vacuum at room temperature for 24 hours. Dissolve 5 g of dried polymalic acid in 20 g of distilled water, add 1.5 g of camptothecin and 0.05 g of photoinitiator 2959, and irradiate under a UV lamp for 1 hour. The intensity of the UV light is 0.1 mW / cm 2 , the biodegradable polymer gel pharmaceutical composition containing camptothecin can be obtained.

Embodiment 2

[0038] Embodiment 2: 20g malic acid is under 130 ℃ and 0.01mmHg vacuum, catalyst-free polycondensation 1 hour, the polymkeric substance obtained is dissolved in N, N-dimethylformamide, press malic acid unit: HEMA: DCC=5 HEMA was grafted onto the side group of polymalic acid at a ratio of 5:5, and the grafting reaction was carried out under stirring at 100° C., and the reaction time was 100 hours. The grafted solution was filtered, and the filtrate was concentrated, precipitated in ether, and dried under vacuum at room temperature for 24 hours. Dissolve 5 g of dried polymalic acid in 20 g of distilled water, add 2.5 g of paclitaxel and 0.5 g of photoinitiator 369, and irradiate under a UV lamp for 120 seconds. The intensity of the UV light is 16 mW / cm 2 , the biodegradable polymer gel pharmaceutical composition containing the drug paclitaxel can be obtained.

Embodiment 3

[0039] Embodiment 3: With 20g citric acid and 20gPEG (weight average molecular weight is 400) under 250 ℃ and 0.01mmHg vacuum, take 0.2gZnO as catalyst polycondensation 50 hours, the polymkeric substance obtained is dissolved in N,N-dimethylethylene Amide, according to the ratio of citric acid unit: HEMA: DCC = 10: 1: 1.5, HEMA is grafted to the side group of the citric acid and PEG copolymer, and the grafting reaction is carried out under stirring at room temperature, and the reaction time is 36 hours. The grafted solution was filtered, and the filtrate was concentrated, precipitated in ether, and dried under vacuum at room temperature for 24 hours. Dissolve 20g of the dried copolymer in 100mL N, N-dimethylacetamide, add 10g of 5-fluorouracil and 0.5g of photoinitiator 651, and irradiate for 10 minutes under a UV lamp. The intensity of the UV light is 200mW / cm 2 , the biodegradable polymer gel pharmaceutical composition containing the drug 5-fluorouracil can be obtained.

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PUM

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Abstract

A biodegradable high-molecular gel used as the carrier of composite medicine for controlling release of medicine features that its main chain is the biodegradable polyester and the polyester-polyether copolymer and carries functional lateral groups (carboxy, amino and hydroxy). Its preparing process includes such steps as preparing said main chain by polycondensing the monomer moleculae with more function groups, grafting to molecule containing unsaturated double bond to the functional lateral groups, grafting the molecule with function group to the rest of functional lateral groups, mixing medicine moleculae with the solution of grafted biodegradable high moleculae, and UV irradiating for cross linking to form gel.

Description

technical field [0001] The invention relates to a biodegradable polymer gel pharmaceutical composition, a preparation method and application thereof, and belongs to the field of medical polymer materials. Background technique [0002] A gel is a three-dimensional polymer network that is swellable but insoluble in a solvent through physical or chemical crosslinking. Due to the three-dimensional polymer network structure of the gel, it can contain a large number of different types of drugs, and it can be used as a carrier for drug controlled release and applied to a drug controlled release system. The drug is released from the gel through diffusion and penetration in the gel, changing the chemical structure and performance of the gel, and can control the release speed and mode of the drug to achieve the purpose of controlled release of the drug. Due to the advantages mentioned above, gels have been more and more widely used in drug controlled release systems. [0003] With t...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K47/34A61K45/00A61K38/28A61K31/337A61K31/505A61K31/475A61K31/167A61K31/405A61K31/407A61K47/59
Inventor 何斌罗祥林
Owner SICHUAN UNIV
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