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.
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[0061] Example 1 Preparation of hydrogel (Gel 2: PEG-DA / U-Arg-PEA / Insulin / TD-1)
[0062] 1. The synthesis of arginine unsaturated polyester amide (U-Arg-PEA) includes the following steps:
[0063] (1) Stir fumaryl chloride and p-nitrophenol in acetone containing triethylamine at 0°C for 2 h, and then overnight at room temperature to obtain monomer I, which is recrystallized 3 times in ethyl acetate;
[0064] (2) After mixing arginine and 1,4-butanediol, add to toluene containing p-toluenesulfonic acid monohydrate, heat to 130°C, stir and reflux for 24 hours, then stir the product at 75°C Dissolve in isopropanol, and precipitate 3 times at 4°C to obtain monomer II;
[0065] (3) After adding monomer I and monomer II to dimethyl sulfoxide and mixing uniformly, add triethylamine dropwise until the monomer is completely dissolved; after stirring at 75°C for 48 h, precipitate with ethyl acetate After being dissolved in methanol, it was purified by repeated precipitation with ethyl acetate ...
Example Embodiment
[0076] Example 2 Preparation of hydrogel
[0077] Other conditions are the same as in Example 1, 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 reduce blood glucose concentration efficiently and quickly, and has a complete shape, good elasticity, and good mechanical strength. After testing, its elastic modulus is 0.47 ± 0.15 MPa .
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[0079] Example 3 Preparation of hydrogel
[0080] Other conditions are the same as in Example 1. The only difference is that 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 transdermal absorption, has the effect of significantly promoting the transdermal absorption of insulin, has a good blood sugar lowering effect, and its shape is complete, its properties are good, and its mechanical strength is good. The amount is 0.39 ± 0.20 MPa.
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