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Application of chitosan oligosaccharide in improving intestinal permeability and serving as oral absorption enhancer of BCSIII drugs

An absorption enhancer, chitosan oligosaccharide technology, applied in the field of application of chitosan oligosaccharides in improving intestinal permeability and as an oral absorption enhancer for BCS III drugs, can solve problems such as unclear mechanism, and achieve oral absorption , Improving the permeability and improving the effect of bioavailability

Active Publication Date: 2021-12-21
SOUTHWEST UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has been reported in the literature that chitosan and its derivatives can promote the transmembrane transport of water-soluble small molecule drugs, but the mechanism is still unclear

Method used

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  • Application of chitosan oligosaccharide in improving intestinal permeability and serving as oral absorption enhancer of BCSIII drugs
  • Application of chitosan oligosaccharide in improving intestinal permeability and serving as oral absorption enhancer of BCSIII drugs
  • Application of chitosan oligosaccharide in improving intestinal permeability and serving as oral absorption enhancer of BCSIII drugs

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Embodiment 1

[0030] The application of oligochitosan in improving intestinal permeability: combined with the experiment of oligochitosan to promote intestinal absorption of drugs, it is confirmed that oligochitosan can be used as an oral drug absorption enhancer after oligochitosan opens the intestinal permeability For the application of improving the bioavailability of BCS Ⅲ drugs, the experimental process and results are as follows:

[0031] 1. Rat isolated valgus intestinal sac test: SD rats aged 8-10 weeks and weighing about 200 g were selected and fasted for 24 hours before the experiment. After being killed, the abdominal cavity was opened along the midline of the abdomen. The 10 cm segment of the intestine was placed in Tyrode's solution at 37°C for flushing and 95% oxygen was introduced, and the mesentery and adipose tissue were removed with tweezers until no content flowed out. Tie one end of the cleaned intestine with a thin cotton thread, carefully turn the intestine over with a...

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Abstract

The invention relates to application of chitosan oligosaccharide in improving intestinal permeability and serving as an oral absorption enhancer of BCSIII drugs, and belongs to the technical field of chitosan oligosaccharide application. The application of the chitosan oligosaccharide in improving the intestinal permeability is based on the principle that the chitosan oligosaccharide can open tight connection between intestinal microvilli epithelial cells to improve the intestinal permeability, and the application of promoting in-vivo absorption of low-permeability drugs is developed. In addition, the invention further discloses the application of the chitosan oligosaccharide serving as the oral absorption enhancer of the BCSIII drugs. The main component in the BCSIII drugs is triflumurin, the chitosan oligosaccharide is taken first to open the tight connection between the intestinal microvilli epithelial cells, then the BCSIII drugs are taken, after the chitosan oligosaccharide and the intestinal mucosa act for a certain time, the opening degree of the tight connection between the epithelial cells is the maximum, and the water-soluble small molecule drugs enter blood circulation from the epithelial cells through trans-cell bypass transport. The chitosan oligosaccharide can be used for promoting oral absorption of the BCSIII drugs difficult to absorb, and the bioavailability of the BCSIII drugs is remarkably or extremely remarkably improved.

Description

technical field [0001] The invention belongs to the technical field, and relates to the application of chitosan oligosaccharide in improving intestinal permeability and as an oral absorption accelerator for BCS III drugs. Background technique [0002] Oral administration has many advantages such as high safety, good compliance, easy operation and avoiding pain, so it is still the most common route of administration. After oral administration, the drug reaches the stomach from the mouth, pharynx, and esophagus, dissolves, disperses or disintegrates in the stomach, and reaches the small intestine. There are ring-shaped folds, villi and microvilli on the surface of the small intestinal mucosa, and the drug is absorbed into the capillary through the microvilli. Blood vessels and chylous lymphatic vessels then enter the systemic circulation. The small intestine is the primary site of absorption for most orally administered drugs due to its large absorptive surface area and high ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K47/26A61K9/00A61K31/7072
CPCA61K47/36A61K47/26A61K31/7072A61K9/0053
Inventor 罗雷祁一鸣任琼赭伍清华金铭罗永煌
Owner SOUTHWEST UNIVERSITY
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