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Synthesis and preparation method of disulfiram entrapped polylactic acid microspheres having pH responsiveness and application thereof

A technology of polylactic acid microspheres and disulfiram, which is applied in the directions of organic active ingredients, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc., can solve the problem of easy decomposition by gastric acid, instability, and difficulty in ensuring drugs targeting issues

Inactive Publication Date: 2018-11-06
常荷玥
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Oral administration is unstable in the process of gastrointestinal blood transport, and it is easily decomposed by gastric acid; intravenous injection is difficult to ensure drug targeting, so a new solution is needed to improve clinical application ability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Step 1: Preparation of Lactide

[0027] Using lactic acid as a raw material, adding stannous octoate as a catalyst (volume ratio of 25:1), dehydration of lactic acid below 160°C and under reduced pressure (40kPa) first forms PLA oligomers, and the molecular weight of the PLA oligomers Less than 2000, the water generated by polycondensation is removed under reduced pressure to break the balance and make the reaction beneficial to polycondensation; then at a higher temperature of 200°C and a certain pressure of 95kPa, the PLA oligomers are depolymerized into rings to generate crude lactide; finally After 5 times of recrystallization, the crude product was purified to obtain the lactide product;

[0028] Step 2: Preparation of pH-sensitive polylactic acid materials containing acetal bonds

[0029] First prepare polylactic acid;

[0030] Take an appropriate amount of lactide obtained in step 1, the obtained stannous isooctanoate, and ethylene glycol (initiator) and mix ev...

Embodiment 2

[0037] Step 1: Preparation of Lactide

[0038] Using lactic acid as a raw material, adding stannous octoate as a catalyst (volume ratio of 25:1), dehydration of lactic acid below 160°C and under reduced pressure (40kPa) first forms PLA oligomers, and the molecular weight of the PLA oligomers is Less than 2000, the water generated by polycondensation is removed under reduced pressure to break the balance and make the reaction beneficial to polycondensation; then at a higher temperature of 250°C and a certain pressure of 100kPa, the PLA oligomers are depolymerized into rings to generate crude lactide; finally After 5 times of recrystallization, the crude product was purified to obtain the lactide product;

[0039] Step 2: Preparation of pH-sensitive polylactic acid materials containing acetal bonds

[0040] First prepare polylactic acid;

[0041] Take an appropriate amount of lactide obtained in step 1, the obtained stannous isooctanoate, and ethylene glycol (initiator) and mi...

Embodiment 3

[0048] Step 1: Preparation of Lactide

[0049] Using lactic acid as a raw material, adding stannous octoate as a catalyst (volume ratio of 25:1), dehydration of lactic acid below 160°C and under reduced pressure (40kPa) first forms PLA oligomers, and the molecular weight of the PLA oligomers Less than 2000, the water generated by polycondensation is removed under reduced pressure to break the balance and make the reaction beneficial to polycondensation; then at a higher temperature of 285°C and a certain pressure of 110kPa, the PLA oligomers are depolymerized into rings to generate crude lactide; finally After 5 times of recrystallization, the crude product was purified to obtain the lactide product;

[0050] Step 2: Preparation of pH-sensitive polylactic acid materials containing acetal bonds

[0051] First prepare polylactic acid;

[0052] Take an appropriate amount of lactide obtained in step 1, the obtained stannous isooctanoate, and ethylene glycol (initiator) and mix e...

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Abstract

Provided are a synthesis and preparation method of disulfiram entrapped polylactic acid microspheres having pH responsiveness and application thereof. A pH sensitive polylactic acid material containing acetal bonds and disulfiram are prepared as model drugs by preparing lactide, polylactic acid macromolecules containing acetal bonds serve as a carrier material, the polylactic acid microspheres having pH responsiveness can be obtained by preparing polylactic acid drug carrying microspheres through a W1 / O / W2 double-emulsification solvent evaporation method, the synthesized and prepared disulfiram entrapped polylactic acid microspheres having pH responsiveness are applied to inhibition of tumor activity, biodegradable macromolecular drug carrying microspheres can be prepared by injecting thepolylactic acid material containing acetal bonds and coat disulfiram and Cu<2+>, the specificity is improved, and the success rate of tumor treatment is greatly improved.

Description

technical field [0001] The present invention relates to the technical fields of synthesis of polylactic acid polymer main chain prepared by ring-opening polymerization, pH response realization targeting and drug loading, in particular to the synthesis and preparation of disulfiram-loaded polylactic acid microspheres with pH responsiveness. its application. Background technique [0002] The morbidity and mortality of malignant tumors are increasing year by year in the world. At present, tumor treatment mainly adopts surgical resection, combined with chemotherapy, radiotherapy, gene therapy, immunotherapy and other methods. With the in-depth study of tumor molecular biology, it was found that the biodegradable polymer drug-loaded microspheres made of pH-sensitive polylactic acid materials containing acetal bonds have higher targeting, stability and compatibility, increasing The drug dissolves and reduces toxicity; at the same time, disulfiram, originally used as an alcohol-ab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/145A61K47/34A61P35/00
CPCA61K9/5031A61K31/145A61P35/00
Inventor 常荷玥
Owner 常荷玥
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