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Icariin controlled release microsphere, preparation method thereof and application thereof

A technology of icariin and microspheres, which is applied in the field of medicine and health, can solve the problems that diseases in the upper end of the colon cannot effectively function, and achieve the effects of prolonging the residence time of the colon, good pH responsiveness, and promoting drug release

Inactive Publication Date: 2017-01-11
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The traditional way of drug administration for colon diseases mainly includes oral and rectal administration. Due to the special physiological structure of the colon, oral administration of drugs is difficult to reach the colon. Although rectal administration can release the drug locally, it is not effective for upper colon diseases. Can not effectively play a role, the present invention loads icariin into chitosan / calcium alginate slow-controlled release microspheres and prepares an oral colon-localized drug delivery system for the treatment of peptic ulcer, which has not been reported so far

Method used

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  • Icariin controlled release microsphere, preparation method thereof and application thereof
  • Icariin controlled release microsphere, preparation method thereof and application thereof
  • Icariin controlled release microsphere, preparation method thereof and application thereof

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Experimental program
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Effect test

Embodiment 1

[0070] The preparation of embodiment 1 epimedium / glycoside chitosan / calcium alginate microspheres

[0071] 1. Prepare the solution

[0072] 1-1) Preparation of sodium alginate solution

[0073] Add accurately weighed sodium alginate into pure water, mix, heat and keep at 45±5°C, stir to fully dissolve the sodium alginate to obtain a sodium alginate solution, and wait until it drops to room temperature (20 -25°C or so) and stored in a refrigerator at 4°C, heated to 45°C before use, and set aside. Among them, the ratio of the mass of sodium alginate in the sodium alginate solution to the volume of water is 0.5:100, that is, the sodium alginate solution The concentration is 1.0% (w / v);

[0074] 1-2) Prepare film-forming solution (ie chitosan-acetic acid solution)

[0075] Add accurately weighed chitosan into 0.5% glacial acetic acid (v / v, volume percent concentration) aqueous solution, after mixing, heat up and keep at 45±5°C, stir to make chitosan fully Dissolve to prepare c...

Embodiment 2

[0101] 1. Prepare the solution

[0102] 1-1) Preparation of sodium alginate solution

[0103] Add accurately weighed sodium alginate into pure water, mix, heat and keep it at 45±5°C, stir to fully dissolve the sodium alginate, and prepare a sodium alginate solution. Store in the refrigerator at ℃, heat to 45 ℃ before use, and set aside, wherein the ratio of the mass of sodium alginate to the volume of water in the sodium alginate solution is 1.5%;

[0104] 1-2) Prepare chitosan-acetic acid solution (film-forming solution)

[0105] Add accurately weighed chitosan into 1% glacial acetic acid (v / v, volume percent concentration) aqueous solution, after mixing, heat up and keep at 45 ± 5 ° C, stir, so that the chitosan is fully Dissolve, make chitosan-acetic acid solution (film-forming solution), treat it to drop to room temperature and store in 4 ℃ of refrigerators, adjust the pH of chitosan-acetic acid solution before use to be 5.5, for subsequent use, wherein, chitosan- The q...

Embodiment 3

[0124] 1. Prepare the solution

[0125] 1-1) Preparation of sodium alginate solution

[0126] Add accurately weighed sodium alginate into pure water, mix, heat and keep at 45±5°C, stir to fully dissolve the sodium alginate to obtain a sodium alginate solution. Store in the refrigerator at 4°C, heat to 45°C before use, and set aside, wherein the ratio of the mass of sodium alginate to the volume of water in the sodium alginate solution is 2%;

[0127] 1-2) Prepare chitosan-acetic acid solution (film-forming solution)

[0128] Add accurately weighed chitosan into 2% glacial acetic acid (v / v, volume percent concentration) aqueous solution, after mixing, heat up and keep at 45 ± 5 ° C, stir, so that the chitosan is fully Dissolve to prepare chitosan-acetic acid solution (i.e. film-forming solution), and store it in a refrigerator at 4°C after it is lowered to room temperature. Before use, adjust the pH of chitosan-acetic acid solution to be 5.5, for subsequent use, wherein chito...

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Abstract

The invention discloses an icariin controlled release microsphere, a preparation method thereof and application thereof. The controlled release microsphere is used for pH response controlled release microsphere for treating colon disease, high-molecular polymers including chitosan, sodium alginate and like are used as carrier materials, the icariin is used as the active ingredient to construct an oral colon specific drug delivery system with biological controlled release targeting ability. The biological controlled release targeting microsphere disclosed by the invention has good pH responsiveness, the drug release amount under stomach low pH environment is low, the drug release can be promoted under the colon high pH environment, and the colon residence time of the drug is prolonged; the drug absorption is increased, and the local bioavailability of the oral drug for treating the colon disease is improved.

Description

technical field [0001] The invention belongs to the field of medicine and health, and relates to a preparation method and application of a new drug dosage form of drug microspheres, in particular to a pH-responsive targeted controlled-release microsphere, its preparation method, and drug application. The drug microspheres are used for Prevention, alleviation and / or treatment of colon diseases, including irritable bowel syndrome, ulcerative colitis, Crohn's disease, rectal cancer and other conditions. Background technique [0002] With the continuous development and progress of society, the pressure of work and life increases, irregular work and rest diet, long-term mental anxiety, nervousness, etc., often lead to health problems such as immune disorders and flora disorders. Traditional Chinese medicine believes that ulcerative colitis belongs to the category of diarrhea and intestinal addiction, while modern medicine believes that it is an autoimmune disease or accompanied b...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/61A61K47/36A61K31/7048A61P1/00A61P1/04A61P35/00
CPCA61K31/7048
Inventor 王强松崔元璐周洁王贵芳刘天军
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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