Unlock instant, AI-driven research and patent intelligence for your innovation.

Mineralized exenatide slow-release system and its preparation method and application

A technology of exenatide and system, applied in the field of new exenatide sustained-release preparations, can solve problems such as easy fibrosis, immune rejection of the body, and affecting the biological activity of exenatide

Active Publication Date: 2021-04-20
SHANGHAI THERANOSTICS BIOTECH CO LTD
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Facts have proved that the first way is easy to affect the biological activity of exenatide, for example, the use of polyethylene glycol to modify exenatide will reduce its ability to stimulate cells to produce cAMP
In addition, the introduction of polymer materials can easily trigger the body's immune rejection
Proteins in blood and interstitial fluid are easily adsorbed on the surface of the polymer. With the participation of immune and inflammatory cells, the surface of the polymer is prone to fibrosis, which hinders its long-term effect on the biological system
[0007] In order to overcome the disadvantages of existing exenatide preparations that easily affect its biological activity and easily induce matrix immune responses, and provide long-acting drug therapy, it is necessary to develop a new exenatide sustained-release system

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Mineralized exenatide slow-release system and its preparation method and application
  • Mineralized exenatide slow-release system and its preparation method and application
  • Mineralized exenatide slow-release system and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1: Preparation of Mineralized Exenatide

[0036] Weigh 2 mg of exenatide and dissolve it in 1 ml of DMEM cell culture medium, and place the solution at 37 degrees Celsius for 24 hours. Weigh 110 mg of calcium chloride solid and dissolve it in 1 ml of ultrapure water to obtain a 1 mol / L calcium chloride solution. Add 10 microliters of calcium chloride solution to 1 milliliter of exenatide DMEM solution, and react at 37 degrees Celsius in a 5% carbon dioxide environment for 24 hours. The obtained solution was centrifuged by ultrafiltration, the molecular weight cut-off was 100k, the centrifugation speed was 6000 rpm, and the centrifugation time was 20 minutes. The obtained mineralized exenatide utilizes transmission electron microscopy to observe the morphology, and it can be known that the mineralized exenatide is a nanoparticle system composed of exenatide at the center and its surrounding biomimetic mineral calcium phosphate (such as figure 1 shown), using a ...

Embodiment 2

[0037] Example 2: In Vitro Release of Exenatide

[0038] The mineralized exenatide particles prepared in Example 1 were dispersed in 1 ml of DMEM solutions containing different calcium ion concentrations (0.9, 2.5 or 5 mmol / L). At the time points of 0, 0.5, 1, 2, 24, 48, 72, 96, 120, 144, 168, and 192 hours, the reaction system was centrifuged by ultrafiltration (100k molecular weight cut-off, 6000 rpm, 20 minutes), The remaining solid was separated from the supernatant. The drug concentration in the supernatant was determined using a commercial exenatide ELISA kit. Finally, the residual particles were reacted in the pH 5 solution environment for 24 hours to dissolve the particles completely, measure the maximum release amount, set it as 100%, and calculate the relative release amount at each time point (such as image 3 shown). The structure of the released exenatide was determined by circular dichroism chromatography and compared with exenatide without any treatment (eg F...

Embodiment 3

[0039] Example 3: In vivo release of exenatide

[0040] Cysteine ​​was connected to position 39 of exenatide to form a new reactive site (side chain of -SH group), which was labeled with near-infrared fluorescent dye IRdye 800CW. The specific operation is as follows: first, N-hydroxysuccinimide-modified IRdye 800CW (25 microliters, 10 mmol / liter) was added to 500 microliters of dimethyl sulfoxide, and then 20 microliters of N-( 2-Aminoethyl) maleimide trifluoroacetate (3 mg / ml dimethyl sulfoxide solution), stirred for 4 hours. Then, 1 mg of exenatide with one cysteine ​​inserted at the C-terminus was added to the above reaction system and reacted overnight (about 12 hours). The resulting product was separated using high performance liquid chromatography, and its structure was characterized using Funky. Thereafter, the near-infrared fluorescent dye-labeled exenatide and its mineralized particles were injected subcutaneously, and the fluorescent signal at the injection point w...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

The present invention provides a mineralized exenatide slow-release system, which is a mineralized exenatide nano-system composed of exenatide in the center and bionic mineral calcium phosphate around the exenatide, wherein, according to In terms of weight percentage, exenatide accounts for 15-20% of the whole nano system, calcium phosphate accounts for 75-78% of the whole nano system, and the balance is crystal water. The mineralized exenatide slow-release system of the present invention can efficiently maintain the biological activity of exenatide, and at the same time avoid the immune response in the body. The present invention also provides a method for preparing the mineralized exenatide sustained-release system, and the application of the mineralized exenatide sustained-release system in the preparation of type II diabetes treatment drugs.

Description

technical field [0001] The invention relates to the fields of biomedical technology and drug controlled release technology, in particular to a novel exenatide sustained-release preparation, its preparation method and application. Background technique [0002] According to the International Diabetes Federation, as of 2015, there were approximately 415 million diabetics worldwide. also. It is estimated that by 2040, the number of patients will reach 642 million, of which type 2 diabetes patients account for about 90% of the total number of patients, which mainly show the characteristics of decreased insulin sensitivity (insulin resistance) and attenuation of insulin secretion function of pancreatic beta cells. It is worth noting that human glucagon-like peptide-1 (GLP-1) can be used as an effective drug for the treatment of type 2 diabetes, which can stimulate the regeneration of β cells, promote insulin secretion, and inhibit pancreatic hypertrophy. Glucagon secretion, slow...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/22A61K47/02A61P3/10
CPCA61K9/0002A61K38/22A61K47/02
Inventor 陈小元陈伟
Owner SHANGHAI THERANOSTICS BIOTECH CO LTD
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com