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GLP-1 analogue and GC-C receptor agonist composite sustained release preparation and preparation method thereof

A receptor agonist and sustained-release preparation technology, which is applied in drug combination, drug delivery, and pharmaceutical formulations, can solve problems such as increasing the risk of adverse reactions in the gastrointestinal tract, and achieve prevention and relief of constipation, good curative effect, and improved life. quality effect

Pending Publication Date: 2018-04-20
南京星银药业集团有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, GLP-1 analogs can significantly increase the risk of gastrointestinal adverse reactions such as nausea, vomiting, diarrhea, and constipation

Method used

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  • GLP-1 analogue and GC-C receptor agonist composite sustained release preparation and preparation method thereof
  • GLP-1 analogue and GC-C receptor agonist composite sustained release preparation and preparation method thereof
  • GLP-1 analogue and GC-C receptor agonist composite sustained release preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] 1. Dissolve gelatin and glycerin of equal quality in sterile water to prepare an aqueous solution containing gelatin and glycerin, wherein the mass concentrations of gelatin and glycerin are both 5 mg / L, and dissolve liraglutide and linaclotide in a solution containing In the aqueous solution of gelatin and glycerin, the total mass concentration that obtains liraglutide and linaclotide is the water phase of 50mg / L; Add PVP in the water phase, obtain the mixture; The ester was dissolved in dichloromethane to obtain an oil phase with a mass concentration of 2400mg / L; wherein, the mass ratio of liraglutide and linaclotide was 1:1, and the ratio of polylactide and polylactide-glycolide The mass ratio is 1:3;

[0030] 2. Put the above mixture and the oil phase in the mixer, and mix evenly at a speed of 12000r / min to form a water-in-oil emulsion. Add the water-in-oil emulsion to water and mix evenly to obtain a water-in-oil-in-water emulsion. Double emulsion, wherein, the vo...

Embodiment 2

[0034]1. Dissolve gelatin and glycerin of equal quality in sterile water to prepare an aqueous solution containing gelatin and glycerin, wherein the mass concentrations of gelatin and glycerin are both 5 mg / L, and dissolve liraglutide acetate and plecanatide in In the aqueous solution containing gelatin and glycerin, the total mass concentration that obtains liraglutide acetate and plecanatide is the aqueous phase of 70mg / L; Add PVA in the aqueous phase, obtain mixture; Polylactide and the polylactide that molecular weight is 20000 and Polylactide-glycolide with a molecular weight of 20,000 was dissolved in ether to obtain an oil phase with a mass concentration of 540 mg / L; wherein, the mass ratio of liraglutide acetate and plecanatide was 20:1, and polylactide The mass ratio of polylactide to glycolide is 3:2;

[0035] 2. Put the above mixture and the oil phase in the mixer, and mix evenly at a speed of 12000r / min to form a water-in-oil emulsion. Add water to the water-in-oil...

Embodiment 3

[0039] 1. Dissolve gelatin and glycerin of equal quality in sterile water to prepare an aqueous solution containing gelatin and glycerin, wherein the mass concentrations of gelatin and glycerin are both 5 mg / L, and dissolve exenatide and linaclotide in a solution containing In the aqueous solution of gelatin and glycerin, the total mass concentration that obtains exenatide and linaclotide is the aqueous phase of 60mg / L; Add polysodium methacrylate in the aqueous phase, obtain mixture; 2, the molecular weight is 15000 Polylactide and polylactide-glycolide with a molecular weight of 20,000 were dissolved in acetone to obtain an oil phase with a mass concentration of 320 mg / L; wherein, the mass ratio of exenatide and linaclotide was 5:1, The mass ratio of polylactide and polylactide-glycolide is 1:1;

[0040] 2. Put the above mixture and the oil phase in the mixer, and mix evenly at a speed of 12000r / min to form a water-in-oil emulsion. Add the water-in-oil emulsion to water and ...

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Abstract

The invention a GLP-1 analogue and GC-C receptor agonist composite sustained release preparation and a preparation method thereof. The sustained release microsphere preparation consists of a GLP-1 analogue, a GC-C receptor agonist and a pharmaceutically acceptable polymer material. The GLP-1 analogue is selected from liraglutide or pharmaceutically acceptable salt thereof, semaglutide or pharmaceutically acceptable salt thereof, exenatide or pharmaceutically acceptable salt thereof, trulicity or pharmaceutically acceptable salt thereof and albiglutide or pharmaceutically acceptable salt thereof. The GC-C receptor agonist is selected from Llinaclotide or pharmaceutically acceptable salt thereof, and plecanatide or pharmaceutically acceptable salt thereof. The composition can be used for effectively treating diabetics, and meanwhile, the composition can be used for preventing and relieving diabetic constipation; and the composition has practical significance for relieving patient's painand improving patient's life quality.

Description

field of invention [0001] The present invention relates to the field of pharmaceutical compositions. More specifically, the present invention relates to a pharmaceutical composition containing two different pharmaceutically active peptides of GLP-1 analogue and GC-C receptor agonist. Background of the invention [0002] With the improvement of people's living standards, the incidence of diabetes in the world is increasing significantly, from 2.8% in 2000 to 4.3% in 2025, and the number of diabetic patients will also increase from 171 million in 2000 to 380 million in 2025. Diabetes is divided into gestational diabetes, specific diabetes, type I diabetes and type II diabetes. Among them, type II diabetes (type2diabetes) is a chronic disease characterized by insulin resistance and insufficient insulin secretion. As the main type of diabetes, patients with type II diabetes account for more than 90% of the total population of diabetes. It is estimated that the global populati...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/26A61K9/52A61K47/34A61P3/10A61P1/10A61K38/10
CPCA61K38/10A61K38/26A61K9/5031A61K2300/00
Inventor 刘铠豪刘庭福
Owner 南京星银药业集团有限公司
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