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Transdermal delivery type hydrogel as well as preparation method and application thereof

A transdermal drug delivery and hydrogel technology, which can be used in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. effect and other issues, to achieve a good hypoglycemic effect, reduce the dosage, and facilitate transdermal absorption.

Inactive Publication Date: 2018-10-16
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

With the continuous development of biotechnology, a large number of new drugs are emerging, and traditional drug delivery methods (such as oral or injection) will affect the efficacy of some biosynthetic drugs based on DNA or protein
The pain of injection administration will bring psychological discomfort to some people, while oral administration has problems such as fluctuations in blood drug concentration, stimulation of gastrointestinal tract, and liver first-pass effect.

Method used

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  • Transdermal delivery type hydrogel as well as preparation method and application thereof
  • Transdermal delivery type hydrogel as well as preparation method and application thereof
  • Transdermal delivery type hydrogel as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Example 1 Preparation of hydrogel (Gel 2: PEG-DA / U-Arg-PEA / Insulin / TD-1)

[0062] 1. The synthesis of unsaturated polyester amide (U-Arg-PEA) of arginine, including the following steps:

[0063] (1) Stir fumaryl chloride and p-nitrophenol in acetone containing triethylamine at 0°C for 2 h, then overnight at room temperature to obtain monomer I, which is recrystallized three times in ethyl acetate;

[0064] (2) After mixing arginine and 1,4-butanediol, add it to toluene containing p-toluenesulfonic acid monohydrate, heat to 130°C, and stir and reflux for 24 h, then stir the product at 75°C Dissolve in isopropanol, and precipitate three times at 4°C to obtain monomer II;

[0065] (3) After adding monomer I and monomer II into dimethyl sulfoxide and mixing evenly, add triethylamine dropwise until the monomers are completely dissolved; after stirring at 75°C for 48 h, precipitate with ethyl acetate , dissolved in methanol, and then purified by repeated precipitation with ...

Embodiment 2

[0076] Example 2 Preparation of hydrogel

[0077] Other conditions are the same as in Example 1, and the only difference is: the sum of the mass percentages of the unsaturated polyester amide of arginine and polyethylene glycol diacrylate is 20%, insulin, transdermal peptide, photoinitiator and water The sum of the mass percentages is 80%.

[0078] The hydrogel prepared in this example has a good transdermal absorption effect, can efficiently and rapidly reduce blood sugar concentration, and has a complete shape, good elasticity, and good mechanical strength. Its elastic modulus is 0.47 ± 0.15 MPa after testing .

Embodiment 3

[0079] Example 3 Preparation of Hydrogel

[0080] Other conditions are the same as in Example 1, and the only difference is: the sum of the mass percentages of the unsaturated polyester amide of arginine and polyethylene glycol diacrylate is 10%, insulin, transdermal peptide, photoinitiator and water The sum of the mass percentages is 90%.

[0081] The hydrogel prepared in this example is easy to absorb through the skin, has the effect of obviously promoting the transdermal absorption of insulin, has a good hypoglycemic effect, and has a complete shape, good resistance, and good mechanical strength. The volume is 0.39 ± 0.20 MPa.

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Abstract

The invention discloses transdermal delivery type hydrogel as well as a preparation method and application thereof. The hydrogel is prepared from an active component, permeation enhancing peptide, unsaturated polyesteramide of arginine, polyethylene glycol diacrylate, a photoinitiator and water, wherein the sum of the mass percent of the unsaturated polyesteramide of arginine and polyethylene glycol diacrylate is 10 percent to 20 percent; the sum of the mass percent of the active component, the permeation enhancing peptide, the photoinitiator and the water is 80 percent to 90 percent. The hydrogel disclosed by the invention has the advantages of easiness for transdermal absorption, good biocompatibility and no cytotoxicity; a protein-type drug can be loaded very well and insulin is given to patients with diabetes mellitus in a transdermal delivery manner, so that the hydrogel has an efficient blood glucose lowering effect and the utilization dosage of the drug can be greatly reduced; controllable slow release drug administration is also realized in a disease treatment process; the transdermal delivery type hydrogel has high safety and is convenient to use, so that the transdermal delivery type hydrogel is an ideal transdermal patch for clinically treating the diabetes mellitus and has a good application prospect.

Description

technical field [0001] The invention belongs to the technical field of biomedicine. More specifically, it relates to a transdermally administrable hydrogel and its preparation method and application. Background technique [0002] Transdermal administration refers to smearing or applying drugs on the surface of the skin, so that the drugs can pass through the skin (stratum corneum, epidermis and dermis), reach the subcutaneous tissue, and finally reach the lesion through internal circulation to achieve the effect of drug treatment . With the continuous development of biotechnology, a large number of new drugs are constantly emerging, and the traditional drug delivery methods (such as oral or injection) will cause the efficacy of some biosynthetic drugs based on DNA or protein to be affected. The pain of injection administration will bring psychological discomfort to some people, while oral administration has problems such as fluctuations in blood drug concentration, stimula...

Claims

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Application Information

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IPC IPC(8): A61K9/06A61K47/34A61K47/14A61K47/42A61K38/28A61P3/10
CPCA61K9/0014A61K9/06A61K38/28A61K47/14A61K47/34A61K47/42A61P3/10
Inventor 吴钧张少瀚顾志鹏
Owner SUN YAT SEN UNIV
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