Colon-targeted gel microsphere with controllable core-shell ratio, and preparation and application of colon-targeted gel microsphere

A gel microsphere and colon-targeting technology, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, microcapsules, etc., can solve uncontrollable core-shell ratio, limited application, cumbersome operation, etc. question

Active Publication Date: 2021-09-14
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Patent CN106702597A discloses a core-shell structure nanofiber membrane and its preparation method and application. The nanofiber membrane prepared by coaxial electrospinning has a single-layer core-shell structure and the core-shell ratio is uncontrollable. The wall

Method used

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  • Colon-targeted gel microsphere with controllable core-shell ratio, and preparation and application of colon-targeted gel microsphere
  • Colon-targeted gel microsphere with controllable core-shell ratio, and preparation and application of colon-targeted gel microsphere
  • Colon-targeted gel microsphere with controllable core-shell ratio, and preparation and application of colon-targeted gel microsphere

Examples

Experimental program
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Effect test

Embodiment 1

[0057] Example 1 Preparation of colon targeting gel microspheres with controlled core-shell ratio loaded with alcohol-soluble capsaicin (core-shell ratio is 0.60)

[0058] (1) 1g chitosan powder, 3g calcium chloride, 3g Tween 20 are dissolved in 94mL 2% (v / v) acetic acid aqueous solution under 600rpm stirring condition, obtain shell layer solution; 1.5g low-ester pectin Powder and 1.5g of sodium alginate powder were dissolved in 97mL of third-grade water under 600rpm stirring and 200W ultrasonic conditions to obtain an inner shell solution; 0.075g capsaicin powder and 0.05g zein powder were vortexed and 200W ultrasonic Dissolve in 4.6mL80% (v / v) ethanol aqueous solution under the condition to obtain the nuclear layer solution;

[0059] (2) Set the coaxial electrostatic spray parameters as follows for preparation: the voltage is 11kV, the injection rate of the inner shell layer is 1.5mL / h, the injection rate of the core layer is 0.5mL / h, the coaxial electrostatic spray nozzle a...

Embodiment 2

[0062] Example 2 Preparation of colon-targeted gel microspheres with a controllable core-shell ratio loaded with alcohol-soluble curcumin (the core-shell ratio is 0.58)

[0063] (1) 1g chitosan powder, 2g calcium chloride, 3g Tween 20 are dissolved in 94mL 2% (v / v) acetic acid aqueous solution under 600rpm stirring condition, obtain shell layer solution; 2g sodium alginate powder is in 600rpm stirring and 200W ultrasonic conditions were dissolved in 97mL of three-grade water to obtain the inner shell solution; 0.05g curcumin powder and 0.15g zein powder were dissolved in 4.6mL 80% ( v / v) in an aqueous ethanol solution to obtain a nuclear layer solution;

[0064] (2) Set the coaxial electrostatic spray parameters as follows to prepare: the voltage is 14kV, the injection rate of the inner shell layer is 2mL / h, the injection rate of the nuclear layer is 0.5mL / h, the coaxial electrostatic spray nozzle and the surface of the outer shell solution The distance is 120mm, the temperat...

Embodiment 3

[0067] Example 3 Preparation of colon-targeting gel microspheres loaded with water-soluble oleuropein with a controllable core-shell ratio (core-shell ratio is 0.86)

[0068] (1) 2g chitosan powder, 1g calcium chloride, 1g Tween 20 are dissolved in 94mL 2% (v / v) acetic acid aqueous solution under 600rpm stirring condition, obtain shell layer solution; 4g low-ester pectin powder Dissolve in 97mL of tertiary water under 600rpm stirring and 200W ultrasonic conditions to obtain the inner shell solution; dissolve 0.05g oleuropein powder and 0.15g kafirin powder in 4.6mL70% under vortex oscillation and 200W ultrasonic conditions (v / v) in acetic acid aqueous solution, obtain nuclear layer solution;

[0069] (2) Set the coaxial electrostatic spray parameters as follows for preparation: the voltage is 15kV, the injection rate of the inner shell layer is 1mL / h, the injection rate of the nuclear layer is 0.5mL / h, the coaxial electrostatic spray nozzle and the surface of the outer shell s...

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Abstract

The invention provides a colon-targeted gel microsphere with a controllable core-shell ratio, and preparation and application of the colon-targeted gel microsphere. The gel microsphere comprises a core layer, an inner shell layer and an outer shell layer from inside to outside in sequence, wherein the core layer comprises cereal prolamin and an active matter; the inner shell layer comprises gel polysaccharide; the outer shell layer comprises chitosan, a cross-linking agent and a suspending aid. The inner shell layer and the core layer form core-shell structure fog drops through a coaxial electrostatic spraying technology, in an outer shell layer solution, the inner shell layer gel polysaccharide of the core-shell structure fog drops is cross-linked with the cross-linking agent and is subjected to electrostatic layer-by-layer adsorption with chitosan, and therefore, the colon-targeted gel microsphere is prepared. The particle size of the gel microsphere is 100-600 [mu] m, the core-shell ratio is 0.5-0.9, the encapsulation efficiency of a water-soluble active matter is as high as 60%, the encapsulation efficiency of an alcohol-soluble active matter is as high as 90%, the release amounts in a stomach simulation liquid and a small intestine simulation liquid within 1 h and 3 h can be as low as 10% and 25%, and the gel microsphere can be efficiently delivered and targeted to the colon.

Description

technical field [0001] The invention belongs to the technical field of colon delivery system preparation. More specifically, it relates to a colon-targeting gel microsphere with a controllable core-shell ratio and its preparation and application. Background technique [0002] Colon diseases are divided into inflammatory colon diseases, ischemic colon diseases, neoplastic colon diseases, etc., and the current treatment methods for colon-related diseases are limited, mainly including oral administration and rectal administration. Discomfort and the range of administration is limited, the drug cannot reach the upper part of the colon, and has little effect on the inflammation that occurs in the cecum and upper colon. For oral administration, in order to make the drug reach the colon and release it smoothly, and improve the efficiency of action, the colon-targeted delivery of drug materials is a current research hotspot. [0003] As a type of colon-targeted delivery material, ...

Claims

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Application Information

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IPC IPC(8): A61K9/62A61K9/06A61K47/42A61K47/36A61K45/00A61K31/165A61K31/12
CPCA61K9/5036A61K9/5089A61K9/5073A61K9/06A61K9/0053A61K47/42A61K47/36A61K45/00A61K31/165A61K31/12A61K31/7048A61K31/352A61K31/216A61P1/00Y02A50/30
Inventor 肖杰王浩楠陆午辉
Owner SOUTH CHINA AGRI UNIV
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