A preparation of yeast cell wall particles that promotes the oral absorption of protein and polypeptide drugs

Abstract

The invention belongs to the field of a medicine preparation, and particularly relates to a yeast cell wall microparticle preparation for promoting oral absorption of protein polypeptide medicine. Protein or polypeptide medicine is entrapped in yeast cell wall microparticles. The stability of the protein or polypeptide medicine in the gastrointestinal tract is further improved through the inside gelation; and the fast leakage degradation of the protein or the polypeptide medicine in the gastrointestinal tract is ensured to be avoided. The yeast cell wall microparticles can specifically target M cells of Peyer's Patches in the intestinal tract, and enters the lymphokinesis through M cell transportation to improve the oral administration bioavailability of protein polypeptide medicine. Through animal experiments, the result shows that the yeast cell wall microparticle preparation has the advantages that the oral administration bioavailability of insulin can be obviously improved; and the obvious application prospects are realized in the field of protein or polypeptide oral administration.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a preparation of yeast cell wall particles capable of promoting oral absorption of proteins or polypeptides and a preparation method thereof. Background technique [0002] In recent years, more and more protein and peptide drugs have entered the clinical trial or clinical treatment stage. The main way of administration is injection. The compliance is extremely poor; therefore, the development of non-injection protein and polypeptide preparations has become a hot spot in the field of pharmacy research, and it is also a topic that needs key breakthroughs in related fields. Clinical practice shows that oral administration is the most convenient and safest way of clinical drug administration, but protein and peptide drugs have the following problems, resulting in low oral bioavailability and inability to achieve a good therapeutic effect: 1. In gastric juice Un...

AI Technical Summary

Problems solved by technology

Clinical practice shows that oral administration is the most convenient and safest way of clinical drug administration, but protein and peptide drugs have the following problems, which lead to low oral bioavailability and cannot achieve a good therapeutic effect: 1. In gastric juice Unstable and easily degraded by pepsin; 2. Can be degraded by protease in the intestine; 3. Protein and polypeptide drugs are highly hydrophilic and have poor cell membrane permeability; 4. Large protein molecular weight leads to poor membrane permeability a reason

At present, the research on improving the oral absorption of protein polypeptide drugs has been very extensive, mainly including the following methods: 1. The use of penetration enhancement and protease inhibitors can improve its bioavailability to a certain extent, but due to its relatively serious toxicity, its The development prospect is still unpredictable; 2. Using transferrin (Tf), cell penetrating peptide TAT and other modifications to improve cell permeability; 3. Using microparticle drug delivery system to improve the oral bioavailability of insulin is the most popular research at present On the one hand, the microparticle drug delivery system can protect the drug from the degradation of enzymes to a certain extent, and at the same time can improve the ability of the drug to cross the membrane. At present, the main ones are nanoparticles, liposomes, microemulsions, and double emulsions; The drug delivery system still cannot significantly improve its bioavailability, mainly because the particles cannot transport drugs across the intestinal cell membrane in large quantities

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