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Polypeptide protein oral nano particle preparation

A nanoparticle and protein technology, applied in the field of medicine, to achieve good patient compliance, convenient oral administration, and improved bioavailability

Inactive Publication Date: 2003-11-12
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Based on all the retrieved literature, the preparation of lactic acid / glycolic acid nanoparticles, coated with chitosan and other polymers, thereby promoting the gastrointestinal absorption of insulin and improving the bioavailability of oral administration of proteins such as insulin has not been reported; in addition, It has not been reported that chitosan alone is used as a carrier to prepare its drug-loaded nanoparticles for oral administration to promote the gastrointestinal absorption of bioactive macromolecular drugs.

Method used

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  • Polypeptide protein oral nano particle preparation
  • Polypeptide protein oral nano particle preparation

Examples

Experimental program
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Effect test

Embodiment 1

[0022] Chitosan-coated insulin polyester nanoparticles: Take 15 mg and 30 mg of insulin and lactic acid / glycolic acid copolymer (PLGA), respectively dissolve them in 3.0 ml, 0.005 mol / L sodium hydroxide solution and 0.5 ml of In ethyl acetate, after being dissolved, keep the temperature at 20°C, take 0.1ml of the water phase and slowly inject it into the 0.5ml of the organic phase, and stir it magnetically at the same time. / o). The prepared colostrum was mixed with 2.0 ml of external water containing 1.0% poloxamer188, and ultrasonicated for 45 seconds in the same way to obtain insulin double emulsion (w / o / w). Then, the double emulsion is added dropwise into a certain concentration of chitosan acetic acid solution through a syringe, and the product is obtained by rotary evaporation under reduced pressure at room temperature until the ethyl acetate volatilizes completely.

Embodiment 2

[0024] Chitosan-coated insulin polyester nanoparticles containing polyvinyl alcohol in the inner water phase: just add a certain concentration of polyvinyl alcohol such as 0.5% to the inner water phase of insulin.

Embodiment 3

[0026] Insulin chitosan nanoparticles: prepare 3 mg / mL chitosan solution and 5 mL of sodium tripolyphosphate solution of the same concentration, mix 0.48 mL of 5 mg / mL insulin solution with 0.56 mL of sodium tripolyphosphate solution, and mix in Under magnetic stirring, drop the mixed solution into 2 mL of chitosan solution.

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Abstract

The invention is a polypeptide protein type oral nano granular preparation. It uses polymer or amphiphatic compound as coating material, and uses the hydrogenous bonds formed between the surfactants absorbed on the interface of the coating material and the oil-water, for examples, the amido in the swelling chitosan molecule in the chitosan coating polyester nano granule and the oxygen atom or the alcohol hydroxyl in the hydrophilic ehenoxy group form the hydrogenous bonds to make it; or the chitosan directly makes the gelation reaction with the multivalent anions to make the nano-granular preparation.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular it is an oral nanoparticle preparation of polypeptide and protein. Background technique: [0002] An oral dosage form of polypeptide and protein-an oral nanoparticle preparation prepared from bioadhesive materials or coated with polymers, with particle diameters in the range of 1-500nm. Specifically, it is a bioadhesive macromolecular material chitosan nanoparticle or polyester colloidal nanoparticle coated with this and other amphiphilic macromolecule. The nanoparticle can further protect insulin from damage, and the coating can reduce the burst release of nanoparticle drugs, improve the bioadhesion of nanoparticle, and prolong the residence time of the particle in the gastrointestinal tract after oral administration, which is beneficial to the promotion of insulin, etc. Gastrointestinal absorption of drugs. [0003] Oral administration of insulin is a hot and difficult researc...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/22A61K38/16A61K38/28A61P3/10
Inventor 潘研郑俊民
Owner SHENYANG PHARMA UNIVERSITY
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