Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Exenatide composite microspheres and preparation method thereof

A technology of exenatide and composite microspheres, applied in the field of medicine, can solve the problems of protein polypeptide chain structure denaturation macromolecular aggregation, decreased drug activity, etc., and achieve uniform particle size distribution, low burst release rate, and protection of biological activity. Effect

Inactive Publication Date: 2018-08-17
SUN YAT SEN UNIV
View PDF3 Cites 6 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

On the other hand, the structure of protein polypeptide drugs is relatively fragile. During the preparation process, the drug will inevitably come into contact with organic solvents, and due to the amphiphilic structure of the drug, it will gather at the oil-water interface, which may eventually cause structural denaturation of the protein polypeptide chain or Irreversible aggregation of macromolecules, resulting in decreased drug activity

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
  • Exenatide composite microspheres and preparation method thereof
  • Exenatide composite microspheres and preparation method thereof
  • Exenatide composite microspheres and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] A kind of exenatide long-acting injection composite microsphere, which uses trehalose as the protective agent of exenatide, wraps exenatide in egg yolk lecithin to form exenatide phospholipid nanoparticles, and then Prepared by encapsulating polylactic acid-glycolic acid copolymer (PLGA, molecular weight 40,000).

[0040] The preparation method of the above-mentioned exenatide long-acting injection composite microspheres comprises the following steps:

[0041](1) Exenatide was dissolved in trehalose aqueous solution containing 1 mg / mL to obtain an aqueous solution containing exenatide at a concentration of 2 mg / mL; egg yolk lecithin was dissolved in tert-butanol to obtain an egg yolk lecithin concentration of 30mg / mL alcoholic solution. Under the conditions of a water bath at 37°C and a magnetic stirring rate of 1000 rpm, the alcohol solution was added dropwise into the aqueous solution, and the volume ratio of the alcohol solution to the aqueous solution was 1:3. Aft...

Embodiment 2

[0049] Example 2 provides an exenatide composite microsphere, the preparation method of which is basically the same as that of Example 1.

[0050] A kind of exenatide long-acting injection composite microsphere, which uses trehalose as the protective agent of exenatide, wraps exenatide in egg yolk lecithin to form exenatide phospholipid nanoparticles, and then encapsulated in poly(lactic-co-glycolic acid) (PLGA, Molecular weight 20000) prepared in-house.

[0051] The preparation method of the above-mentioned exenatide long-acting injection composite microspheres comprises the following steps:

[0052] (1) Exenatide was dissolved in trehalose aqueous solution containing 1 mg / mL to obtain an aqueous solution containing exenatide at a concentration of 2 mg / mL; egg yolk lecithin was dissolved in tert-butanol to obtain an egg yolk lecithin concentration of 30mg / mL alcoholic solution. Under the conditions of a water bath at 37°C and a magnetic stirring rate of 1000 rpm, the alco...

Embodiment 4

[0065] Detect the in vitro effects of exenatide long-acting injection composite microspheres and exenatide PLGA microspheres: accurately weigh the exenatide long-acting injection composite microspheres prepared in Example 1 and the exenatide long-acting injection composite microspheres prepared in Comparative Example 1. Put 10 mg of senatide PLGA microspheres in a 5 mL sample centrifuge tube, add 1 mL of phosphate buffer saline PBS (pH=7.4), place in an air-bath shaker, and shake at a constant temperature at 37 ° C and 100 rpm. On days 1, 2, 4, 7, 10, 15, 20, 25, 30, 35, 40, 45, 50, 55, and 60 days, samples were taken to detect the content of exenatide. When sampling, take the sample centrifuge tube out of the shaker, centrifuge at 12000rpm for 5min, and absorb all the supernatant as the test sample for in vitro release; in addition, add 1mL of PBS (pH=7.4) to the sample centrifuge tube and place it on the shaker Continuing to oscillate. The detection sample released in vitro...

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

PropertyMeasurementUnit
concentrationaaaaaaaaaa
concentrationaaaaaaaaaa
particle sizeaaaaaaaaaa
Login to View More

Abstract

The invention provides exenatide composite microspheres. The exenatide composite microspheres are characterized in that lecithin wraps exenatide and a protecting agent simultaneously, and after exenatide lipid nanoparticles are formed, a high-molecular polymer carrier encapsulates the exenatide lipid nanoparticles to prepare the exenatide composite microspheres; and the molecular weight of the high-molecular polymer carrier is 10000-90000, and the high-molecular polymer carrier is dissolved in a mixing organic solvent. The prepared composite microspheres are uniform in grain size, the encapsulation efficiency of the exenatide is high, the microspheres are spherical and have smooth surfaces, the mean grain size is between 1 mu m and 50 mu m, and by the characteristics of smooth surfaces, high encapsulation efficiency and uniform grain size, the releasing speed of the microspheres is stable, the microspheres can release for a long time, therefore, the drug-delivering frequency can be reduced, and the compliance of patients is good.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an exenatide composite microsphere and a preparation method thereof. Background technique [0002] At present, the clinical application of protein and polypeptide drugs is mainly in the form of injection and freeze-dried powder injection. In order to achieve the curative effect, frequent injections are often required, resulting in low drug compliance. In order to improve the bioavailability of protein and polypeptide drugs and reduce the frequency of administration, it is an effective way to develop long-acting preparations of protein and polypeptide drugs, among which long-acting injection microspheres have the most promising application prospects. [0003] Exenatide is a synthetic product of the GLP-1 analogue Exendin-4 isolated from the salivary gland of the giant monster lizard. It consists of 39 amino acids and is the first GLP-1 receptor approved by the US Food and Drug Ad...

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 Applications(China)
IPC IPC(8): A61K38/22A61K9/50A61K47/26A61K47/24A61K47/34A61K47/08A61K47/06A61P3/10A61P3/04
CPCA61K38/22A61K9/0019A61K9/5031A61K47/06A61K47/08A61K47/24A61K47/26A61P3/04A61P3/10
Inventor 吴传斌董妮朱春娥李静李醒
Owner SUN YAT SEN UNIV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com