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Preparation method for degradable microcapsules with disulfide bonds

A technology of microcapsules and disulfide bonds, applied in the field of preparation of degradable microcapsules, can solve the problems of easy generation of drug resistance, short half-life, small molecular weight, etc., to change the pharmacokinetic characteristics and reduce the peak and valley concentration of blood drugs. Poor, the effect of increasing dwell time

Inactive Publication Date: 2016-01-06
ZHEJIANG SCI-TECH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Hepatitis B (hepatitis B) is a serious infectious disease caused by hepatitis B virus (HBV), and it is also an important pathogenic factor leading to liver cancer. With the rapid development of medical technology, the drugs currently used to treat hepatitis B Among them, interferon (IFN) is an active protein (mainly glycoprotein) with multiple functions, but ordinary interferon has the disadvantages of small molecular weight, short half-life, wide system distribution and high renal clearance rate, so it is easy to Drug resistance and other toxic side effects

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0017] Example 1: Take the following steps:

[0018] A) Take 150mL of MnSO with a concentration of 0.016mol / L 4 solution, add 30mL of absolute ethanol, and stir it with ultrasound for 1min at room temperature or magnetically at a speed of 400rpm for 5min to make the mixture evenly mixed;

[0019] B) Quickly add 150 mL of NH with a concentration of 0.16 mol / L to the mixture obtained in step A) under magnetic stirring at a speed of 400 rpm 4 HCO 3 Solution, keep stirring for 2min or ultrasonic for 20s, and then let it stand until all the generated particles are completely precipitated;

[0020] C) Centrifuge the mixture obtained in step B) at 3000rpm, discard the supernatant to obtain a precipitate, wash the precipitate three times with deionized water, and then disperse the precipitate in deionized water for later use, and the amount of deionized water used to submerge Sediment shall prevail;

[0021] D) Dissolve 50 mg of polyallylamine hydrochloride in 1 mL of NaOH solutio...

Embodiment 2

[0028] Example 2: Take the following steps:

[0029] A) Take 200mL of MnSO with a concentration of 0.016mol / L 4 solution, add 40mL of absolute ethanol, and stir it with ultrasound for 1.5min at room temperature or magnetically at a speed of 500rpm for 4.5min to make the mixture evenly mixed;

[0030] B) Quickly add 200 mL of NH with a concentration of 0.16 mol / L to the mixture obtained in step A) under magnetic stirring at a speed of 500 rpm 4 HCO 3 Solution, keep stirring for 1.5min or ultrasonic for 15s, and then let it stand until all the generated particles are completely precipitated;

[0031] C) Centrifuge the mixture obtained in step B) at 3000rpm, discard the supernatant to obtain a precipitate, wash the precipitate three times with deionized water, and then disperse the precipitate in deionized water for later use, and the amount of deionized water used to submerge Sediment shall prevail;

[0032] D) Dissolve 100 mg of polyallylamine hydrochloride in 2 mL of NaOH ...

Embodiment 3

[0039] Example 3: Take the following steps:

[0040] A) Take 250mL of MnSO with a concentration of 0.016mol / L 4 Add 50mL of absolute ethanol to the solution, and stir it ultrasonically for 2min at room temperature or magnetically at 600rpm for 4min to make the mixture evenly mixed;

[0041] B) Quickly add 250 mL of NH with a concentration of 0.16 mol / L to the mixture obtained in step A) under magnetic stirring at a speed of 600 rpm 4 HCO 3 Solution, keep stirring for 1min or ultrasonic for 10s, and then let it stand until all the generated particles are completely precipitated;

[0042] C) Centrifuge the mixture obtained in step B) at 3000rpm, discard the supernatant to obtain a precipitate, wash the precipitate three times with deionized water, and then disperse the precipitate in deionized water for later use, and the amount of deionized water used to submerge Sediment shall prevail;

[0043] D) Dissolve 150 mg of polyallylamine hydrochloride in 3 mL of NaOH solution with ...

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PUM

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Abstract

The invention discloses a preparation method for degradable microcapsules with disulfide bonds. According to the preparation method, disulfide bond covalent cross-linked (FITC-PAH / DPA)5 microcapsules are prepared by taking MnCO3 micro-particles as templates, taking 3,3'-dithiobispropionate as a cross-linking agent, and adopting a layer-by-layer assembly method; the prepared microcapsules can be kept in a stable state in an external environment, and can also release a drug directionally in cells, so that the drug ingredients of the microcapsules are protected to prolong the residence time of the drug ingredients in the cells; the characteristics of pharmacokinetics are changed; the peak-valley concentration difference of blood drug in vivo is reduced; adverse reactions are reduced; the preparation method is simple; the raw materials are chip; the preparation method is applicable to batch production.

Description

technical field [0001] The invention belongs to the field of biopharmaceuticals, in particular to a method for preparing degradable microcapsules with disulfide bonds, which are mainly used for loading drugs to treat hepatitis B. Background technique [0002] Hepatitis B (hepatitis B) is a serious infectious disease caused by hepatitis B virus (HBV), and it is also an important pathogenic factor leading to liver cancer. With the rapid development of medical technology, the drugs currently used to treat hepatitis B Among them, interferon (IFN) is an active protein (mainly glycoprotein) with multiple functions, but ordinary interferon has the disadvantages of small molecular weight, short half-life, wide system distribution and high renal clearance rate, so it is easy to Drug resistance and other toxic side effects. Therefore, how to use microcapsules to embed interferon to be degraded and released inside the cell, so as to protect its drug components and increase its residen...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/21A61K9/50A61K47/32C08J3/24A61P1/16A61P31/20
Inventor 刘建军王秉彭志勤胡智文
Owner ZHEJIANG SCI-TECH UNIV
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