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Bile acid modified oral granule

A bile acid and granule technology, applied in the field of biomedicine, can solve the problems of drugs that are unstable to pH or temperature, hinder the oral administration of drugs, and have low bioavailability

Inactive Publication Date: 2018-08-10
北京凯宾鸿生物医药科技有限公司
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  • Abstract
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AI Technical Summary

Problems solved by technology

[0002] Many therapeutic drugs are limited by various factors after oral administration, including poor intestinal permeability, resulting in low bioavailability, unstable pH or temperature leading to drug decomposition, and some drugs are degraded by proteases, etc. Oral administration
Some chronic treatment drugs such as diabetes drugs, anticancer drugs, neuropathy and other drugs need to be taken orally for a long time. If they are made into injections, it will bring many side effects and inconvenience

Method used

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  • Bile acid modified oral granule
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  • Bile acid modified oral granule

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Embodiment Construction

[0025] The main reason for the low efficacy of oral drugs is the poor absorption of drugs in the intestinal wall. Bile acid transporter is an important carrier for the absorption of therapeutic drugs. Bile acids secreted by the liver are absorbed from the ileum by intestinal epithelial cells, and transported to the liver through the portal vein. Therefore, the drug-loaded particles with surface-modified bile acids have higher absorption in vivo. Because of the action of bile acid transporters in the terminal ileum, the absorption of drug particles into the blood is promoted.

[0026] Taurocholic acid (TCA) is an abundant bile acid, which accounts for about 45% of human intestinal fluid. TCA can be used as a carrier of therapeutic drugs, mainly in the terminal ileum, and maximize intestinal cell absorption through terminal bile acid transporters. Therefore, drug transport from the terminal ileum to the portal vein and into the systemic circulation can be facilitated by the bi...

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Abstract

The invention belongs to the technical field of biological medicine, and particularly relates to an oral surface modification bile acid granule, composition of entrapped treatment medicine in the granule and a preparation method. Firstly, a positively charged compound of entrapped treatment medicine is prepared; then, a bile acid polymer with negative ions is used for coupling to form granules. Abile acid-phospholipid compound is inserted into a wrapped granule surface to form the bile acid modified granule. The medicine wrapped granule can be lipidosome, micelle, emulsion, microspheres, nanometer particles and the like. After the granule is orally taken in the body, the granule is selectively absorbed into blood in the intestinal tract under the effect of enterohepatic circulation; the bioavailability of oral medicine can be improved. The medicine is prepared from gene, protein, polypeptide, antibodies, nucleic acid, viruses and small molecule medicine.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and clarifies an oral therapeutic composition of bile acid modified on the surface of particles. These compositions include cationic complexes and bile acid-containing anionic complexes that are coupled by electrostatic interactions to form particles. The granules contain drugs and modify bile acids. Alternatively, bile acid-phospholipid complexes are inserted into the surface of the encapsulated particles to form bile acid-modified particles. The drug-encapsulated particles can be liposomes, micelles, emulsions, microspheres, nanoparticles, etc. These compositions contain therapeutic drugs such as genes, proteins, polypeptides, antibodies, and small molecule drugs. Background technique [0002] Many therapeutic drugs are limited by various factors after oral administration, including poor intestinal permeability, resulting in low bioavailability, instability to pH or temperature leading t...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/28A61K47/24A61K47/36A61K47/34A61K47/42A61K47/54A61K47/61A61K47/64A61K47/59A61K38/28A61K31/704A61K48/00A61P3/10A61P35/00
CPCA61K9/1617A61K9/1641A61K9/1652A61K9/1658A61K31/704A61K38/28A61K47/544A61K47/554A61K47/59A61K47/61A61K47/64A61K48/005A61P3/10A61P35/00
Inventor 高钟镐申红艺金红妍
Owner 北京凯宾鸿生物医药科技有限公司
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