A kind of glucagon-like peptide-1 analog sustained-release microsphere preparation and preparation method thereof

A slow-release microsphere preparation, glucagon technology, applied in the directions of polymer compound inactive ingredients, drug combinations, microcapsules, etc., can solve the instability of GLP-1 analog sustained-release preparation, encapsulation efficiency and load Unsatisfactory drug dosage, unable to solve problems such as polypeptide instability, achieve good drug release characteristics, improve drug safety, and improve drug compliance.

Active Publication Date: 2022-02-08
LUNAN PHARMA GROUP CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, no protective agent is added to the prescription, which cannot solve the problem of polypeptide instability
[0012] The GLP-1 analog sustained-release preparations prepared by methods in the prior art or conventional methods have many shortcomings such as instability, burst release, unsatisfactory encapsulation efficiency and drug loading, and short drug release cycle. , effective and stable long-acting glucagon-like peptide-1 analog sustained-release microspheres are necessary

Method used

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  • A kind of glucagon-like peptide-1 analog sustained-release microsphere preparation and preparation method thereof
  • A kind of glucagon-like peptide-1 analog sustained-release microsphere preparation and preparation method thereof
  • A kind of glucagon-like peptide-1 analog sustained-release microsphere preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] 1) Prescription

[0042]

[0043] 2) Preparation process:

[0044] a) Liraglutide and hydroxypropyl-β-cyclodextrin are dissolved in sterile water for injection as the inner water phase, and the mass-volume concentration of liraglutide in the inner water phase is 200 mg / mL;

[0045] b) The polymer blend and the release modifier are added to a mixed solution of dichloromethane and ethyl acetate (1:1, v / v) to dissolve, as the organic phase, the mass-volume of the polymer blend in the organic phase The concentration is 300mg / ml;

[0046] c) adding the internal aqueous phase of step a) to the organic phase of step b) under high-speed stirring at 23000 rpm, emulsifying for 30 seconds, and mixing evenly to obtain colostrum;

[0047] d) Add the colostrum obtained in step c) dropwise into the polyvinyl alcohol solution at 4°C under the stirring condition of 1500rpm, stir at a low speed of 600rpm to evaporate the organic solvent, and collect the microspheres through a 1200-m...

Embodiment 2

[0050] 1) Prescription

[0051]

[0052] 2) Preparation process: the preparation process is the same as in Example 1.

Embodiment 3

[0054] 1) Prescription

[0055]

[0056]

[0057] 2) Preparation process: the preparation process is the same as in Example 1.

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PUM

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a glucagon-like peptide-1 analog slow-release microsphere preparation and a preparation method thereof. The microsphere weight components include 10-25 parts of glucagon-like peptide-1 analog, 1-5 parts of β-cyclodextrin derivatives, 100 parts of PLGA and polycaprolactone mixture, 15-25 parts of PEG , wherein the mass ratio of PLGA and polycaprolactone is 1:0.2‑1. The drug-loaded microspheres loaded with glucagon-like peptide-1 analogs are prepared by double emulsion-emulsification solvent evaporation method. The microspheres prepared by the present invention have a long drug release period, good drug stability, high safety, and broad application potential. Application prospect.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a slow-release microsphere preparation of a glucagon-like peptide-1 analogue and a preparation method thereof. Background technique [0002] Diabetes is a global disease and one of the major threats to human health. In recent years, the number of diabetes patients in the world has increased dramatically. It is estimated that by 2030, the number of patients worldwide will exceed 300 million, of which type Ⅱ diabetes accounts for more than 90% of the total number of patients. [0003] Glucagon-like peptide-1 (GLP-1) is a glucose-dependent insulinotropic hormone that can increase insulin secretion. It only increases insulin secretion at high blood glucose concentrations, but does not There is no such effect; in addition, GLP-1 can also slow down the apoptosis of β cells and promote their regeneration, which provides a new option for the treatment of ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K9/50A61K47/34A61K47/40A61K47/10A61K38/26A61P3/10
CPCA61K9/5073A61K9/5031A61K47/40A61K47/10A61K38/26A61P3/10
Inventor 刘忠
Owner LUNAN PHARMA GROUP CORPORATION
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