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Intestinal tract targeting and pH-sensitive complex coacervation microcapsule transmission system and preparation method and application thereof

A technology of complex coacervation and microcapsules, which is applied in the delivery system of intestinal-targeted pH-sensitive complex coacervation microcapsules and its preparation, can solve problems such as unsuitable for intestinal-targeted delivery, easy dissociation, and release of core materials. Achieve the effect of good market application prospect, simple and easy production process, and easy large-scale production

Active Publication Date: 2015-11-04
QINGDAO AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these complex coacervation delivery systems are easy to dissociate when the pH deviates from the optimal preparation, and are unstable in the strongly acidic environment of gastric juice, resulting in the release of the core material, making these systems unsuitable for intestinal targeted delivery.

Method used

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  • Intestinal tract targeting and pH-sensitive complex coacervation microcapsule transmission system and preparation method and application thereof
  • Intestinal tract targeting and pH-sensitive complex coacervation microcapsule transmission system and preparation method and application thereof
  • Intestinal tract targeting and pH-sensitive complex coacervation microcapsule transmission system and preparation method and application thereof

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Experimental program
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Embodiment 1

[0025] In this embodiment, the preparation method of the intestinal-targeted pH-sensitive complex coacervation microcapsule delivery system includes the following steps:

[0026] 1. Take O-carboxymethyl chitosan and gum arabic as polycations and polyanions respectively to form a complex coacervation system, specifically 1% (w / v) O-carboxymethyl chitosan solution and 4% (w / v) Mix equal volumes of the gum arabic solution, stir evenly, adjust the pH to 3.0 at 25°C, and stir at 200r / min for 1h;

[0027] 2. After centrifuging to remove the supernatant, collect the complex condensed phase, divide the complex condensed phase into 3 equal parts, put into 0.01% (w / v), 0.03% (w / v) and 0.05% (w / v) Beijing Nepene aqueous solution was reacted at room temperature for 6 hours, and the cross-linked complex coacervate phase was freeze-dried to obtain a complex coacervate microcapsule delivery system.

[0028] At the same time, a comparison group was set up, and the wall material was complete...

Embodiment 2

[0033] In this embodiment, the preparation method of the intestinal-targeted pH-sensitive complex coacervation microcapsule delivery system includes the following steps:

[0034] 1. Mix 1% (w / v) N,O-carboxymethyl chitosan solution and 3% (w / v) gum arabic solution in equal volumes, stir evenly, adjust the pH to 4.5 at 45°C, 200r / min Stir the reaction for 1h;

[0035] 2. After centrifuging to remove the supernatant, collect the complex coacervate phase, divide the prepared complex coacervate phase into 3 equal parts, put them into 0.05% (w / v) genipin aqueous solution, and react at room temperature for 2h, 6h and 12h respectively , freeze-dry the cross-linked complex coacervate phase to obtain the complex coacervate microcapsule delivery system.

[0036] At the same time, a comparison group was set up. The complex coacervation microcapsule system without genipin crosslinking was soaked in pH 1.2 for 1 hour, and the wall material was completely dissociated. Table 2 shows the swe...

Embodiment 3

[0041] In this embodiment, the preparation method of the intestinal-targeted pH-sensitive complex coacervation microcapsule delivery system includes the following steps:

[0042]1. Mix 1% (w / v) O-carboxymethyl chitosan solution and 5% (w / v) gum arabic solution in equal volumes, stir evenly, adjust the pH to 6.0 at 35°C, and stir at 200r / min for reaction 1h;

[0043] 2. After centrifuging to remove the supernatant, collect the complex coacervate phase, divide the prepared complex coacervate phase into 3 equal parts, put them into 0.05% (w / v) genipin aqueous solution, and react at room temperature for 2h, 6h and 12h respectively , freeze-dry the cross-linked complex coacervate phase to obtain the complex coacervate microcapsule delivery system.

[0044] At the same time, a comparison group was set up. The complex coacervation microcapsule system without genipin crosslinking was soaked in pH 1.2 for 1 hour, and the wall material was completely dissociated. Table 3 shows the swe...

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Abstract

The present invention provides an intestinal tract targeting and pH-sensitive complex coacervation microcapsule transmission system and a preparation method and an application thereof. Carboxymethyl chitosan and arabic gum are polycations and polyanions to constitute a complex coacervationsystem. By adjusting pH value, the carboxymethyl chitosan and the arabic gum are subjected to complex coacervation reaction, and the complex coacervation phase is collected by centrifugation, crosslinked by genipin, and freeze-dried to obtain the intestinal tract targeting and pH-sensitive complex coacervation microcapsule transmission system. The intestinal tract targeting and pH-sensitive complex coacervation microcapsule transmission system can be used either for embedding water-soluble functional components, but also for embedding fat-soluble functional components, can protect core materials against damage caused by strongly acidic gastric environment, safely delivery the core materials to the intestinal tracts to conduct targeted releases, and expand the practical application field of the complex coacervation microencapsulation technology. The intestinal tract targeting and pH-sensitive complex coacervation microcapsule transmission system does not dissociate in a simulated gastric fluid and swells in a simulated intestinal fluid, and has a strong stability, and the process is simple, safe, efficient, and easy for mass production.

Description

technical field [0001] The invention belongs to the technical field of microcapsules, and in particular relates to an intestinal-targeting pH-sensitive complex coacervation microcapsule transport system, a preparation method and application thereof. Background technique [0002] Functional factors play a very important role in regulating the physiological functions of the human body. They have functions such as strengthening the brain and improving intelligence, protecting eyesight, lowering blood pressure, anti-aging, regulating immunity, and improving intestinal flora imbalance. They are research hotspots in the field of food. However, many functional factors are easily destroyed by the strong acidic conditions and proteases in the stomach, which greatly affects the stability and actual efficacy in the body. Microencapsulation is an effective means to improve the stability of the core material, achieve controlled release and change the physical state. There are many metho...

Claims

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Application Information

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IPC IPC(8): A23P1/04
CPCA23V2002/00A23V2200/224A23V2250/5028A23V2250/511
Inventor 肖军霞黄国清韩晓娜程玲云
Owner QINGDAO AGRI UNIV
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