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CT-visible mucous-adherence-type bifunctional microcapsules, and preparation method and application thereof

A microcapsule, dual-function technology, applied in the field of biomedical materials, can solve the problem of short intestinal retention time, inability to observe and evaluate the retention and colonization of exogenous probiotics in real time, and low colonization efficiency of exogenous probiotics and other problems, to achieve high-efficiency mucoadhesion performance, which is conducive to effective colonization and growth.

Active Publication Date: 2019-07-23
天益健康科学研究院(镇江)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, microcapsules, as probiotic carriers, often lead to low colonization efficiency of exogenous probiotics due to lack of effective adhesion and short intestinal retention time during oral administration, seriously affecting their therapeutic effect
At the same time, due to the lack of effective non-invasive monitoring methods, it is impossible to observe and evaluate the retention and colonization of exogenous probiotics in the intestinal tract in real time

Method used

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  • CT-visible mucous-adherence-type bifunctional microcapsules, and preparation method and application thereof
  • CT-visible mucous-adherence-type bifunctional microcapsules, and preparation method and application thereof
  • CT-visible mucous-adherence-type bifunctional microcapsules, and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] A preparation method of low-catechol modified multifunctional microcapsules:

[0038] (1) 1.625 mmol of chitosan was dissolved in 0.97% glacial acetic acid solution, and the pH was adjusted to 4.5.

[0039] (2) Dissolve 3.25mmol 3,4-dihydroxyphenylalanine in 5mL double distilled water, slowly add into the chitosan solution obtained in (1) and keep stirring.

[0040] (3) Dissolve 3.245 mmol of 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride in 50 mL of double distilled water and absolute ethanol (1:1) mixed solution, dropwise Slowly add the rapidly stirred 3,4-dihydroxyphenylalanine and chitosan mixed solution obtained in (2), vigorously stir at room temperature for 4 hours, and adjust the pH to 5.0.

[0041] (4) The mixed solution was dialyzed in the dark using a dialysis bag (molecular weight cut-off: 2000), dialyzed in double distilled water (pH5.0) for 2 days, PBS for 4 hours, and double distilled water for 1 day. Store at -20°C after lyophilization.

[0...

Embodiment 2

[0044] A kind of preparation method of the multifunctional microcapsule modified by medium catechol:

[0045] (1) 3.25 mmol of chitosan was dissolved in 0.97% glacial acetic acid solution, and the pH was adjusted to 4.5.

[0046] (2) 3.25 mmol of 3,4-dihydroxyphenylalanine was stirred and dissolved in 5 mL of double distilled water, slowly added into the chitosan solution obtained in (1) and kept stirring.

[0047] (3) Dissolve 3.245 mmol of 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride in 50 mL of double distilled water and absolute ethanol (1:1) mixed solution, dropwise Slowly add the rapidly stirred 3,4-dihydroxyphenylalanine and chitosan mixed solution obtained in (2), vigorously stir at room temperature for 4 hours, and adjust the pH to 5.0.

[0048] (4) The mixed solution uses a dialysis bag with a molecular weight cut-off of 2000, protected from light, dialyzed with double distilled water, pH 5.0, dialyzed for 2 days, PBS for 4 hours, and double distilled ...

Embodiment 3

[0051] A preparation method of multifunctional microcapsules modified with high catechol:

[0052] (1) 3.25 mmol of chitosan was dissolved in 0.97% glacial acetic acid solution, and the pH was adjusted to 4.5.

[0053] (2) 3.25 mmol of 3,4-dihydroxyphenylalanine was stirred and dissolved in 5 mL of double distilled water, slowly added into the chitosan solution obtained in (1) and kept stirring.

[0054] (3) Dissolve 6.49 mmol of 1-ethyl-(3-dimethylaminopropyl) carbodiimide hydrochloride in 50 mL of double distilled water and absolute ethanol (1:1) mixed solution, dropwise Slowly add the mixed solution of 3,4-dihydroxyphenylalanine and chitosan obtained in (2) with rapid stirring, stir vigorously at room temperature for 4 hours, and adjust the pH to 5.0.

[0055] (4) The mixed solution uses a dialysis bag with a molecular weight cut-off of 2000, protected from light, dialyzed with double distilled water, pH 5.0, dialyzed for 2 days, PBS for 4 hours, and double distilled water...

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Abstract

The invention discloses CT-visible mucous-adherence-type bifunctional microcapsules as well as a preparation method and application thereof. The preparation method of the CT-visible mucous-adherence-type bifunctional microcapsules comprises the following steps: preparing catecholated chitosan modified with catechol by utilizing a chemical grafting method; preparing alginate microspheres containingbarium sulfate by utilizing low-concentration alginic acid and a sodium sulphate solution as spray fluid as well as a barium chloride solution as receptor fluid by adopting an one-step electrostaticspray method; performing multi-layer surface coating on the alginate microspheres by utilizing the catecholated chitosan so as to obtain a chitosan / alginate microcapsule complex; and then, mixing the chitosan / alginate microcapsule complex with a trisodium citrate solution so as to obtain microcapsules. The microcapsules prepared by the preparation method have excellent mucous adherence characteristics and CT angiography properties; moreover, the microcapsules are also applicable in oral drug preparations, oral nutrient preparations and oral probiotics.

Description

technical field [0001] The invention belongs to the field of biomedical materials, in particular to a CT visualization and mucoadhesive dual-function microcapsule, a preparation method and an application thereof. Background technique [0002] Microcapsules are microscopic containers or packages with polymeric walls. Its size generally ranges from 5-200 μm, and its shape varies, depending on the raw material and preparation method. Among them, the embedded material is called the core material, and the material that embeds the core material to achieve microencapsulation is called the wall material. The preparation methods of microcapsules mainly include spray drying, in-situ polymerization, emulsion crosslinking and organic solvent phase separation. [0003] In recent years, microcapsule preparation technology and application fields have developed rapidly. The network structure wall of the microcapsules can stably and slowly release the drug, alleviate the damage of the dru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/04A61K9/62A61K47/10A61K47/36A61K35/741A61K35/747A61K31/341
CPCA61K49/0404A61K9/5036A61K9/5015A61K35/741A61K35/747A61K31/341
Inventor 杜凤移边高瑞吴云超张苗苗贾长生李珮铷
Owner 天益健康科学研究院(镇江)有限公司
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