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Application of fluorine-containing compound modified cationic polymer in preparation of transmucosal administration of drugs

A cationic polymer and compound technology, applied in the fields of polymer chemistry and medical biomaterials, can solve problems such as mucosal, epithelial damage, toxic and side effects of the body, and poor biocompatibility, and achieve the effects of simple operation, good effect and low cost.

Active Publication Date: 2020-10-30
SUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this delivery system has poor biocompatibility, has certain toxic and side effects on the body, and can easily cause mucosal and epithelial damage at high concentrations, and its clinical application faces bottlenecks.

Method used

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  • Application of fluorine-containing compound modified cationic polymer in preparation of transmucosal administration of drugs
  • Application of fluorine-containing compound modified cationic polymer in preparation of transmucosal administration of drugs
  • Application of fluorine-containing compound modified cationic polymer in preparation of transmucosal administration of drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0136] Example 1: Preparation of perfluoroheptanoic acid-modified chitosan as a carrier of oral drugs, oral delivery of insulin, diabetes treatment.

[0137] specific method:

[0138] 1. Preparation of perfluoroheptanoic acid-modified chitosan-insulin capsules: Dissolve perfluoroheptanoic acid-modified chitosan and insulin in a weak acid solution to make them evenly dissolved. After mixing, add a weak base solution dropwise while stirring , adjust the pH to 6-7, and under neutral conditions, the perfluoroheptanoic acid-modified chitosan and insulin combine together due to electrostatic adsorption to form stable nanoparticles. After the reaction is complete, take it out, pre-add a freeze-drying protective agent, and freeze-dry to obtain a perfluoroheptanoic acid-modified chitosan-insulin freeze-dried powder, which is packed into a capsule and wrapped with an enteric coating.

[0139] 2. The chitosan-insulin freeze-dried powder modified by reconstituted perfluoroheptanoic acid ...

Embodiment 2

[0146] Example 2: Preparation of perfluoroheptanoic acid-modified chitosan as a carrier oral capsule, oral delivery of apoptosis-ligand 1 antibody, observation of different proportions of perfluoroheptanoic acid-modified chitosan-apoptosis-ligand Transmucosal effects of body 1 antibody particles.

[0147] specific method:

[0148] 1. Preparation of perfluoroheptanoic acid-modified chitosan-apoptosis-ligand 1 antibody particles: Weigh 0.2 mg perfluoroheptanoic acid-modified chitosan and dissolve it in 0.5 mL ultrapure water to obtain 0.4 mg / mL perfluoroheptanoic acid-modified chitosan Fluoroheptanoic acid-modified chitosan, and serially diluted to obtain 0.4mg / mL, 0.2mg / mL, 0.1mg / mL, 0.05mg / mL, 0.0025mg / mL perfluoroheptanoic acid-modified chitosan solution . Use fluorescently-labeled immunoglobulin G as a template instead of the apoptosis-ligand 1 antibody, and drop into 0.5mL of 0.1mg / mL FITC-labeled immunoglobulin G of 0.02M pH=7.2 under the condition of constant stirring ...

Embodiment 3

[0185] Example 3: Using perfluoroheptanoic acid modified chitosan as a carrier to prepare perfluoroheptanoic acid modified chitosan-immune modulator particles, administered in the form of spray / inhalation, to investigate the ability of drug pulmonary delivery .

[0186] specific method:

[0187] 1. Preparation of perfluoroheptanoic acid-modified chitosan-antibody particles: Add apoptosis-ligand 1 antibody to perfluoroheptanoic acid-modified chitosan aqueous solution, and stir at room temperature for 1 hour to form stable nanoparticles.

[0188] 2. The perfluoroheptanoic acid-modified chitosan-antibody particles were delivered in aerosol through the pulmonary administration needle, and tissue sections were performed 24 hours after delivery to observe the retention of the fluorescent signal in the lung tissue. The result is as Figure 3-1 shown.

[0189] For experimental results, see Figure 3-1 , perfluoroheptanoic acid-modified chitosan-antibody particles can stay in the l...

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Abstract

The invention discloses an application of a fluorine-containing compound modified cationic polymer in preparation of transmucosal administration of drugs. The polymer comprises a transmucosal preparation component (a), wherein the component (a) is a cationic polymer modified by a fluorine-containing compound; the cationic polymer modified by the fluorine-containing compound is fluorinated chitosan; the fluorine-containing compound is covalently connected to a main chain of the chitosan, the molecular weight range of the chitosan is 1000-5000000, the degree of deacetylation of the chitosan is not less than 55%, the viscosity range of the chitosan is 25-1000 centipoises, and the mucosas comprise nasal mucosa, lung mucosa, vaginal mucosa, oral mucosa and gastrointestinal mucosa. The fluorine-containing compound modified cationic polymer, especially the fluorinated chitosan, provided by the invention has the advantages that the fluorine-containing compound modified cationic polymer can beuniversally combined with various medicines, the medicine absorption is promoted, the bioavailability of the medicines is improved, and the toxicity is reduced.

Description

technical field [0001] The invention relates to the technical fields of polymer chemistry and medical biomaterials, in particular to the related application of a fluorine-containing compound-modified cationic polymer as a transmucosal drug carrier. Background technique [0002] Seeking non-injection drug delivery methods has always been a research hotspot in the fields of pharmacy and biochemistry, involving drug delivery routes including oral, pulmonary, nasal, rectal, and vaginal drug delivery. These non-injection drug administration methods have the advantages of convenient medication, less pain for patients, and improved compliance of patients, and have become a hot spot in the research of external preparations. However, in practical applications, there is still the problem of low delivery efficiency of macromolecular drugs. One of the important reasons is that various mucous membranes of human organs (including nasal cavity mucous membrane, pulmonary mucous membrane, v...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/08A61K47/36A61K31/704A61P35/00
CPCC08B37/003A61K47/36A61K31/704A61P35/00Y02A50/30A61K31/196A61K9/0014A61K9/0048A61K8/492A61Q19/00A61K2800/10A61K8/736A61Q7/00A61K8/43A61K8/606A61K8/44A61Q19/02A61K2800/56A61K2800/54C08L5/08A61K47/61A61K47/542A61K47/54
Inventor 刘庄陈倩金秋桐陈林甫韦婷赵琪
Owner SUZHOU UNIV
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