Application of fluorine-containing compound modified chitosan in preparation of transdermal delivery preparation

A technology for transdermal drug delivery and chitosanization, which is applied in the field of cationic polymers as drug transdermal carriers, can solve the problems of high toxicity, limited transdermal effect, low drug bioavailability and generalizability, etc. The effect of long, reduced administration area, and fast action speed

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, the existing technologies or products usually have one or more defects such as limited transdermal effect, low drug bioavailability, poor universal combination with various drugs, and high toxicity.

Method used

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  • Application of fluorine-containing compound modified chitosan in preparation of transdermal delivery preparation
  • Application of fluorine-containing compound modified chitosan in preparation of transdermal delivery preparation
  • Application of fluorine-containing compound modified chitosan in preparation of transdermal delivery preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0070] Example 1: Preparation of perfluoroheptanoic acid-modified chitosan as a carrier for transdermal application, transdermal delivery of insulin, and treatment of diabetes. The specific fluorinated chitosan preparation process of this embodiment is referred to embodiment 5.

[0071] specific method:

[0072] 1. Preparation of perfluoroheptanoic acid-modified chitosan-insulin complex: respectively dissolve perfluoroheptanoic acid-modified chitosan and insulin in a weak acid solution environment to dissolve evenly, mix well and add dropwise while stirring Weak base solution, adjust the pH to 6-7. Under neutral conditions, perfluoroheptanoic acid-modified chitosan and insulin combine together due to electrostatic adsorption to form a stable complex, in which perfluoroheptanoic acid-modified chitosan The preferred reaction mass ratio of sugar to insulin is 1:0.25-4, more preferably 1:0.5-2. After the reaction is complete, take it out, pre-add a freeze-drying protective agent...

Embodiment 2

[0080] Example 2: Preparation of perfluoroheptanoic acid-modified chitosan as a carrier transdermal ointment for transdermal delivery of apoptosis-ligand 1 antibody for treatment of melanoma on the body surface.

[0081] specific method:

[0082] 1. Prepare the chitosan-immunoglobulin G complex (hereinafter referred to as FCS-IgG) modified by perfluoroheptanoic acid: since immunoglobulin G has the same structure as the apoptosis-ligand 1 antibody, at the material level Immunoglobulin G was used as a template to study the preferred ratio of perfluoroheptanoic acid-modified chitosan binding to apoptosis-ligand 1 antibody. Add different amounts of immunoglobulin G into the aqueous solution of perfluoroheptanoic acid-modified chitosan, and stir at room temperature for 1 hour to form a stable complex. Wherein, the reaction mass ratio of perfluoroheptanoic acid-modified chitosan to immunoglobulin G is 1:0.25-4, and is further preferably 1:1 through dynamic light scattering particle...

Embodiment 3

[0099] Embodiment 3: prepare the chitosan (deacetylation degree ≥ 95%, viscosity 100-200mpa.s) of the different modification degree of 3-fluorobenzoic acid, wherein the feeding molar ratio of 3-fluorobenzoic acid and N-glucosamine unit is respectively 1:2.1, 1:4.2, 1:8.4, 1:16.8.

[0100] Synthetic method: (1) preparation of chitosan acetic acid aqueous solution: take by weighing 200mg fully dried chitosan and add in 10ml 1% acetic acid aqueous solution, also can adopt hydrochloric acid aqueous solution certainly, stir 30min to fully dissolve, then slowly add dropwise 1.6ml0. 5M sodium hydroxide, stirred until the solution was clear and the pH was around 6.5. From the point of view of alkalization solution, sodium hydroxide can be replaced by alkalis such as ammonia water and triethylamine, but the by-product of using sodium hydroxide is sodium chloride from the perspective of product technology, which is more suitable for industrialization. Prepare 4 parts of chitosan acetic...

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Abstract

The invention discloses a transdermal delivery preparation. The transdermal preparation comprises a transdermal preparation component (a), wherein the component (a) is a cationic polymer modified by afluorine-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 deacetylation degree of the chitosan is not less than 55%, and the viscosity range of the chitosan is 25-1000 centipoises. The cationic polymer modified by the fluorine-containing compound has the advantages of being capable of being universally combined with various medicines, promoting medicine absorption, improving thebioavailability of the medicines and reducing toxicity, good in effect, very wide in application and huge in commercial value, and the cationic polymer modified by the fluorine-containing compound iseasy to produce and has a commercial foundation.

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 drug transdermal carrier. Background technique [0002] Transdermal drug delivery refers to a drug delivery method that penetrates the skin, enters the blood circulation after being absorbed by capillaries, reaches an effective blood drug concentration, and then produces drug effects. Transdermal administration can avoid the hepatic first-pass effect of oral administration and avoid drug inactivation in the gastrointestinal tract. Especially for patients who need long-term administration, transdermal administration is a convenient and quick treatment method. However, as the first barrier of the human body, the skin can block the invasion of most exogenous substances. The rate of drug penetration through the skin is often slow, and the penetration amount is...

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 刘庄陈倩金秋桐朱文俊赵琪
Owner SUZHOU UNIV
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