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Nanometer transdermal slow-release preparation based on insulin loaded on PAMAM (polyamide-amine) dendrimers and preparation method thereof

The technology of a dendrimer and sustained-release preparation is applied in the application of the treatment of diabetes, in the field of preparation of nano-transdermal preparations, and can solve the problems of affecting local insulin absorption and reducing the efficacy of the drug, so as to avoid physical and psychological pain and reduce drug use. number of times, the effect of improving solubility

Inactive Publication Date: 2018-08-31
FUZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Long-term insulin injection sites will lead to the formation of fat pads. The existence of such fat pads will seriously affect the absorption of local insulin, leading to insulin resistance and reduced drug efficacy.

Method used

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  • Nanometer transdermal slow-release preparation based on insulin loaded on PAMAM (polyamide-amine) dendrimers and preparation method thereof
  • Nanometer transdermal slow-release preparation based on insulin loaded on PAMAM (polyamide-amine) dendrimers and preparation method thereof
  • Nanometer transdermal slow-release preparation based on insulin loaded on PAMAM (polyamide-amine) dendrimers and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] A: Weigh 55mg of insulin and dissolve it in 5ml 75% (V / V) ethanol to form a drug-containing organic solution; weigh 125mg of PAMAM solution and dissolve it in 5ml of water; weigh 0.1ml of glycerin, carboxymethylcellulose 200mg, manna Alcohol 1g, Azone 100mg, Carbomer 5mg, Polyacrylate pressure-sensitive adhesive 150mg, N, N-methylenebisacrylamide 3mg.

[0035] B: Add excipients glycerin, carboxymethyl cellulose, mannitol, azone, carbomer, polyacrylate pressure-sensitive adhesive, N, N-methylenebisacrylamide to PAMAM aqueous solution, and take 5 mL insulin ethanol solution Add it dropwise into the PAMAM aqueous solution, and stir for 1 h at room temperature to obtain the drug-loaded layer.

[0036] C: Apply the drug-loaded layer evenly on the backing layer, cover with a protective layer, pass the inspection, vacuumize and seal, and the product is ready.

Embodiment 2

[0038]A: Weigh 55mg of insulin and dissolve in 5ml of 75% (V / V) ethanol to form a drug-containing organic solution; weigh 125mg of PAMAM solution and dissolve in 5ml of water; weigh 0.1ml of glycerin, carboxymethylcellulose 160mg, mannitol 1g, Azone 100mg, Carbomer 5mg, Polyacrylate Pressure Sensitive Adhesive 150mg, N, N-Methylenebisacrylamide 3mg.

[0039] B: Add excipients glycerin, carboxymethyl cellulose, mannitol, azone, carbomer, polyacrylate pressure-sensitive adhesive, N, N-methylenebisacrylamide to PAMAM aqueous solution, and take 5 mL insulin ethanol solution Add it dropwise into the PAMAM aqueous solution, and stir for 1 h at room temperature to obtain the drug-loaded layer.

[0040] C: Apply the drug-loaded layer evenly on the backing layer, cover with a protective layer, pass the inspection, vacuumize and seal, and the product is ready.

Embodiment 3

[0042] A: Weigh 55mg of insulin and dissolve it in 5ml 75% (V / V) ethanol to form a drug-containing organic solution; weigh 125mg of PAMAM solution and dissolve it in 5ml of water; weigh 0.1ml of glycerin, carboxymethylcellulose 100mg, manna Alcohol 1g, Azone 100mg, Carbomer 5mg, Polyacrylate pressure-sensitive adhesive 150mg, N, N-methylenebisacrylamide 3mg.

[0043] B: Add excipients glycerin, carboxymethyl cellulose, mannitol, azone, carbomer, polyacrylate pressure-sensitive adhesive, N, N-methylenebisacrylamide to PAMAM aqueous solution, and take 5 mL insulin ethanol solution Add it dropwise into the PAMAM aqueous solution, and stir for 1 h at room temperature to obtain the drug-loaded layer.

[0044] C: Apply the drug-loaded layer evenly on the backing layer, cover with a protective layer, pass the inspection, vacuumize and seal, and the product is ready.

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Abstract

The invention belongs to the technical field of medicinal preparations, and particularly relates to preparation of a nanometer transdermal slow-release preparation based on insulin loaded on PAMAM (polyamide-amine) dendrimers and application thereof to diabetes resistance. The nanometer transdermal slow-release preparation comprises a backing layer, a medicine carrying layer and an anti-sticking layer, wherein the medicine carrying layer comprises components of nanocrystallized insulin, a pressure-sensitive adhesive, a penetration enhancer, a crosslinker and a matrix; the medicine carrying layer is enclosed in a gel form between the backing layer and the anti-sticking layer. By virtue of slow-release properties of nanoparticles of the insulin loaded on the PAMAM dendrimers, the acting timeof a medicine can be prolonged, the dosage of the medicine is reduced under the precondition that the action of the medicine is guaranteed, and toxic and / or side effects of the medicine are reduced or avoided; moreover, the insulin nanoparticles are loaded into a transdermal medicine administering system, so that the nanometer transdermal slow-release preparation is more convenient to use.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to the preparation of a nano transdermal preparation based on PAMAM dendrimers loaded with insulin and its application in treating diabetes. Background technique [0002] Diabetes is a metabolic disease characterized by high blood sugar, and has become the "third killer" that endangers human health after cardiovascular and cerebrovascular diseases and tumors. According to the report of the International Diabetes Federation (IDF), there were 425 million people with diabetes worldwide in 2017, among which the number of people with diabetes in China was as high as 114.4 million, ranking first in the world. For diabetic patients, once the blood sugar is not well controlled for a long time, it is likely to lead to serious complications: diabetic retinopathy will lead to blindness in patients, and diabetic nephropathy will lead to chronic renal failure in p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/28A61K9/70A61K47/34A61P3/10A61K9/51
CPCA61K9/5146A61K9/70A61K38/28A61K47/34A61P3/10
Inventor 邵敬伟林娟芳郭燕
Owner FUZHOU UNIV
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