Melittin complex nanometer granule for oral dosing and preparation method thereof

Abstract

The invention belongs to the technical field of medicines and discloses melittin complex nanoparticles for oral administration and a preparation method thereof. Water-soluble melittin and an amphiphilic substance are dissolved into a hydrosolvent A to form a hydrophobic protein ion pairing complex; the complex and a suitable polymer material are dissolved into a nonaqueous solvent B; an emulsion solvent diffusion method in a liquid phase is adopted to wrap the complex into the polymer material; and microparticles with the particle diameter between 10 and 1000nm are formed after the solvent is volatilized. The hydrosolvent A is distilled water, double distilled water, deionized water, physiological saline, or a phosphate buffer solution or an acetate buffer solution or a Tris buffer solution with the pH value of between 1 and 11; and the nonaqueous solvent B is a single or mixed solvent of alcohol, acetone, ethyl acetate, methylene dichloride, chloroform and dimethyl sulfoxide. The complex has high fat solubility, and the encapsulation rate of the nanoparticles is more than 90 percent. The preparation process is mild and can assure the biological activity of medicines. The preparation method is suitable to prepare oral administration preparations.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a melittin complex nanoparticle for oral administration and a preparation method thereof. Background technique [0002] With the development of biomedical technology, more and more protein and peptide drugs have been researched and developed and applied clinically. Bee Venom (bee venom, referred to as bee venom) is a kind of venom that is produced by the bee venom gland and stored in the poison sac. When the bee is stimulated, it is discharged from the sting needle of its tail. Peptide, histamine, phospholipase A 2 And hyaluronidase, etc., are biologically active substances containing a variety of natural peptides and enzymes, and have a long history of clinical application in my country. The main component of bee venom, melittin is a polypeptide composed of 26 amino acids, accounting for about 50% of the dry weight of bee venom. It has antibacterial, anti-inflammatory, anti-r...

AI Technical Summary

Problems solved by technology

[0004] Pharmacists at home and abroad have used various methods to load water-soluble polypeptide macromolecules into nanomaterials to improve oral bioavailability, but there is still no breakthrough

Especially for water-soluble protein drugs, not only the preparation process requires severe conditions such as high temperature, high shear, and ultrasound, but also its hydrophobicity makes the encapsulation rate of water-soluble protein drugs low (<60%) (Yan P, HY Zhao, Hui X, et al.Effect of experimental parameters on the encap sulation of insulin2loadedpoly(lactide2co2glycolide) nanoparticles p prepared by a doubleemulsion method[J].J Chin Pharma Sci, 2002,11(1):38241.) Therefore, a suitable dosage form was developed , Improving the encapsulation rate of water-soluble protein peptide drugs, and then improving their bioavailability is a major problem for pharmaceutical workers to be overcome

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