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Preparation method of controlled release carrier of glucose-responsive drug

A technology for controlled release and responsiveness of drugs, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, and non-active ingredients of polymer compounds, etc. It can solve problems such as complex processes, simplify preparation steps, facilitate large-scale production, The effect of avoiding the loss of raw materials

Active Publication Date: 2013-07-10
江阴智产汇知识产权运营有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a preparation method of a glucose-responsive drug controlled release carrier, which uses a divinyl sulfone capable of reacting with multiple functional groups such as hydroxyl, amino, and mercapto groups to combine Con A with a polymer matrix containing sugar units Direct immobilization and cross-linking, forming a glucose-responsive drug controlled release microgel carrier through the inverse emulsion dispersion method, which solves the need for Con A and its sugar ligands in the preparation of glucose-responsive drug controlled release carriers in the prior art Polymer modification, lack of complex process

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] 1) Dissolve dextran (molecular weight 70kDa) in 0.01mol / L sodium hydroxide aqueous solution to make a solution with a mass fraction of 10%, stir evenly at a speed of 300rpm, then add divinyl sulfone, divinyl sulfone The molar ratio to the hydroxyl group in dextran is 0.5:1, keep the same rotation speed and react at room temperature for 10 minutes, then adjust the pH value to 5 with 1 mol / L hydrochloric acid to stop the reaction. The solution after the reaction was dialyzed in deionized water (dialysis membrane molecular weight cut-off 5kDa) for 7 days, and then freeze-dried to obtain dextran with a vinyl sulfone group with a substitution degree of 20% (the substitution degree was calculated by NMR spectrum) .

[0018] 2) Preparation of Con A activation solution: Dissolve Con A in a solution containing 0.1mol / L KCl, 0.1mmol / L CaCl 2 ,0.1mmol / L MnCl 2 In the pH7.0 phosphate buffer solution, the initial concentration of Con A was 5mg / mL, and it was allowed to stand for 6...

Embodiment 2

[0022] 1) Dissolve dextran (molecular weight 100kDa) in 0.1mol / L sodium hydroxide aqueous solution to make a solution with a mass fraction of 2%, stir evenly at a speed of 500rpm, then add divinyl sulfone, divinyl sulfone The molar ratio to the hydroxyl group in dextran is 1.25:1, keep the same rotation speed and react at room temperature for 15 minutes, then adjust the pH value to 4 with 5mol / L sulfuric acid to stop the reaction. The reacted solution was dialyzed in deionized water (dialysis membrane molecular weight cut-off 3kDa) for 7 days, and then freeze-dried to obtain dextran with a substitution degree of 40% with vinyl sulfone groups.

[0023] 2) Preparation of Con A activation solution: Dissolve Con A in a solution containing 0.1mol / L KCl, 0.1mmol / L CaCl 2 ,0.1mmol / LMnCl 2 In the tris-hydrochloric acid buffer solution with pH 7.0, the initial concentration of Con A was 10mg / mL, and it was allowed to stand for 6h.

[0024] 3) Dissolve dextran with vinyl sulfone group...

Embodiment 3

[0027] 1) Dissolve dextran (molecular weight 40kDa) in 1mol / L sodium hydroxide aqueous solution to make a solution with a mass fraction of 5%, stir evenly at a speed of 500rpm, then add divinyl sulfone, divinyl sulfone and The molar ratio of hydroxyl groups in dextran was 2.5:1, and the reaction was carried out at room temperature for 30 minutes at the same speed, and then the pH value was adjusted to 5 with 5 mol / L nitric acid to stop the reaction. The reacted solution was dialyzed in deionized water (the molecular weight cut-off of the dialysis membrane was 5kDa) for 7 days, and then freeze-dried to obtain dextran with a vinyl sulfone group with a substitution degree of 90%.

[0028] 2) Preparation of Con A activation solution: Dissolve Con A in a solution containing 0.1mol / L KCl, 0.1mmol / L CaCl 2 ,0.1mmol / LMnCl 2 In the pH7.4 phosphate-citric acid buffer solution, the initial concentration of Con A was 10mg / mL, and it was allowed to stand for 6h.

[0029] 3) Dissolve the ...

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Abstract

The invention provides a preparation method of a controlled release carrier of a glucose-responsive drug, solves insufficiencies that ConA and sugar ligands thereof are needed to be modified in prior art. The method comprises: (1) dissolving sugar-containing polymer units in a lye, adding divinyl sulfone, adjusting a pH to stop reaction, and dialyzing to obtain a sugar-containing polymer with vinyl sulfone groups; (2) dissolving the prepared substances in a buffer solution, adding a ConA activating solution; (3) adjusting pH of the mixture obtained in step (2) by using the buffer solution, adjusting the pH, adding drop by drop the product into a mixed solution of cyclohexane and an emulsion stabilizer, reacting, removing an oil phase at an upper level, and depositing a lower level to obtain the glucose-responsive carrier. By introducing the divinyl sulfone into the ConA-sugar-containing polymer carrier, the preparation steps for the carrier can be simplified, the sugar-containing polymer can be directly crosslinked with the ConA, thereby being simple and high-efficiency to fix the ConA, low in cost, convenient to implement, and beneficial for large-scale production.

Description

technical field [0001] The invention relates to a preparation method of a drug carrier with glucose responsiveness and capable of adjusting drug release according to the change of environmental glucose concentration, especially a glucose-responsive drug controlled release carrier based on the specific interaction between concanavalin and sugar units The preparation method belongs to the technical field of drug controlled release and biomaterials. Background technique [0002] Diabetes mellitus is a serious lifelong disease (divided into type I and type II). Patients with imbalanced blood glucose metabolism usually manifest as persistent hyperglycemia. The main cause is absolute or relative insufficient secretion of insulin caused by damage to pancreatic β cells. The most effective treatment for diabetes (type 1 and severe type 2 patients) is multiple daily subcutaneous injections of insulin, which help maintain normal blood sugar levels. Unfortunately, this widely used trea...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/42A61K47/36
Inventor 王克敏殷瑞雪
Owner 江阴智产汇知识产权运营有限公司
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