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Somaglutide microneedle patch capable of reducing blood glucose and reducing weight as well as preparation method and application thereof

A microneedle patch and peptide hypoglycemic technology, applied in the field of semaglutide hypoglycemic and weight loss microneedle patch and its preparation, can solve the problems of reducing the dosage of semaglutide, high bioavailability, and low treatment cost , to achieve the effect of improving the effect, increasing the permeability and ensuring the activity of the drug

Pending Publication Date: 2021-01-29
广州新济薇娜生物科技有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Based on this, the present invention provides a semaglutide hypoglycemic and weight loss microneedle patch, which can increase the absorption and penetration rate of semaglutide in the skin to reduce the dosage of semaglutide, So that it can not only improve the problem of poor compliance of transdermal injection, but also have higher bioavailability than oral administration, less dosage, and lower treatment cost

Method used

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  • Somaglutide microneedle patch capable of reducing blood glucose and reducing weight as well as preparation method and application thereof
  • Somaglutide microneedle patch capable of reducing blood glucose and reducing weight as well as preparation method and application thereof
  • Somaglutide microneedle patch capable of reducing blood glucose and reducing weight as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0059] This example provides a semaglutide hypoglycemic and weight loss microneedle patch, which includes a microneedle body and a microneedle base, and its preparation method includes the following steps:

[0060] ① Needle solution preparation: in parts by weight, weigh 1 part of semaglutide, 55 parts of sodium hyaluronate (molecular weight: 5KD), 25 parts of polyvinylpyrrolidone (molecular weight: 17000), 2 parts of N-8 -(2-Hydroxybenzamido) octanoic acid sodium, 17 parts of mannose, 10 parts of 0.2mol / L acetic acid / sodium acetate buffer, 90 parts of purified water (wherein, semaglutide, penetration-promoting components, small molecule The total amount of protective agent and macromolecular framework material is 100 parts, the total amount of buffer solution and purified water is 100 parts). First, mix the acetic acid / sodium acetate buffer solution with purified water to obtain an aqueous solution with a pH of 4.0, then dissolve the semaglutide active ingredient in the above...

Embodiment 2

[0065] This example provides a semaglutide hypoglycemic and weight loss microneedle patch, which includes a microneedle body and a microneedle base, and its preparation method includes the following steps:

[0066] ① Needle solution preparation: in parts by weight, weigh 0.8 parts of semaglutide, 45 parts of sodium hyaluronate (molecular weight: 5KD), 25 parts of dextran (molecular weight: 2000), 3.5 parts of N-8 -(2-Hydroxybenzamido) octanoic acid sodium, 25.7 parts of mannose, 20 parts of citric acid / sodium citrate buffer, 80 parts of purified water (among them, semaglutide, penetration-promoting ingredients, small molecule protective agents and The total amount of macromolecular framework material is 100 parts, the total amount of buffer solution and purified water is 100 parts). First, mix the citric acid / sodium citrate buffer solution with purified water to obtain an aqueous solution with a pH of 4.3, then dissolve the semaglutide active ingredient in the above solution, ...

Embodiment 3

[0071] This example provides a semaglutide hypoglycemic and weight loss microneedle patch, which includes a microneedle body and a microneedle base, and its preparation method includes the following steps:

[0072] ① Needle solution preparation: in parts by weight, weigh 1 part of semaglutide, 35 parts of sodium hyaluronate (molecular weight: 5KD), 22 parts of polyvinylpyrrolidone (molecular weight: 17000), 15 parts of N-( 2-hydroxypropyl) methacrylamide copolymer (molecular weight is 3000), 1 part of azone, 1 part of propylene glycol, 25 parts of trehalose, 10 parts of 0.2mol / L acetic acid / sodium acetate buffer solution, 90 parts of purified water (Wherein, the total amount of semaglutide, penetration-promoting components, small molecule protective agent and macromolecular framework material is 100 parts, and the total amount of buffer solution and purified water is 100 parts). First, mix the acetic acid / sodium acetate buffer with purified water to obtain an aqueous solution ...

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Abstract

The invention relates to a somaglutide microneedle patch capable of reducing blood glucose and reducing weight as well as a preparation method and application thereof. The microneedle patch comprisesa microneedle body and a substrate, wherein the microneedle body is prepared from the following components in parts by weight: 0.01-5 part of somaglutide, 0.1-5 part of a penetration promoting component, 10-50 parts of a small molecular protective agent, 45-85 parts of a macromolecular framework material and 65-200 parts of an aqueous solution containing a pH buffer agent; the permeation promotingcomponent is selected from one or more of N-(8-(2-hydroxy benzoyl) amino) caprylate, azone and propylene glycol; the small molecule protective agent is selected from one or more of mannose, glucose,fructose and trehalose; and the macromolecular framework material is selected from one or more of hyaluronic acid or sodium salt thereof, polyvinylpyrrolidone, an N-(2-hydroxypropyl) methacrylamide copolymer and glucan. The microneedle patch can improve the absorption permeability of the somaglutide in the skin so as to reduce the dosage of the somaglutide.

Description

[0001] field of invention [0002] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a semaglutide hypoglycemic and weight-reducing microneedle patch and a preparation method and application thereof. Background technique [0003] In recent years, with the development of biotechnology, the glucagon-like peptide-1 (GLP-1) series of hypoglycemic drugs are more effective and safe for the treatment of type 2 diabetes. GLP-1 is a peptide hormone encoded by the human islet glucagon gene and secreted by intestinal L cells. It belongs to the incretin family, and its secretion is regulated by eating activities. The effect is strong, the risk of hypoglycemia is low, and at the same time, it can effectively reduce the weight of the users, and has multiple clinical advantages such as good weight loss effect and improvement of cardiovascular diseases. As a blockbuster product among GLP-1 drugs, semaglutide has a good hypoglycemic effe...

Claims

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Application Information

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IPC IPC(8): A61K38/26A61K9/00A61K9/70A61K47/36A61K47/32A61K47/18A61K47/26A61K47/12A61K47/22A61K47/10A61P3/10A61P3/04A61M37/00
CPCA61K38/26A61K9/0021A61K9/7023A61K47/36A61K47/32A61K47/18A61K47/26A61K47/12A61K47/22A61K47/10A61P3/10A61P3/04A61M37/0015A61M2037/0053A61M2037/0046
Inventor 温新国张敏敏陈航平李峰冯地桑杨蓓蓓
Owner 广州新济薇娜生物科技有限公司
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