Sustained-release microsphere preparation of glucagon-like peptide-1 analogue and preparation method of microsphere preparation

A technology of sustained-release microsphere preparations and glucagon, which is applied in the direction of non-active ingredients of polymer compounds, pharmaceutical formulations, microcapsules, etc., and can solve the instability, encapsulation efficiency and loading of GLP-1 analog sustained-release preparations. Unsatisfactory drug dosage and unable to solve the problems of peptide instability, etc., to achieve good drug release characteristics, improve drug safety, and improve drug compliance

Active Publication Date: 2019-12-31
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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  • Sustained-release microsphere preparation of glucagon-like peptide-1 analogue and preparation method of microsphere preparation
  • Sustained-release microsphere preparation of glucagon-like peptide-1 analogue and preparation method of microsphere preparation
  • Sustained-release microsphere preparation of glucagon-like peptide-1 analogue and preparation method of microsphere preparation

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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Abstract

The invention belongs to the technical field of pharmaceutical preparation, and specifically relates to a sustained-release microsphere preparation of a glucagon-like peptide-1 analogue and a preparation method of the microsphere preparation. The weight components of the microsphere preparation comprise 10-25 parts of glucagon-like peptide-1 analogue, 1-5 parts of beta-cyclodextrin derivative, 100parts of PLGA and polycaprolactone mixture, and 15-25 parts of PEG, wherein the mass ratio of PLGA to polycaprolactone is 1:(0.2-1). The drug-loaded microspheres encapsulating the glucagon-like peptide-1 analogue are prepared by using a compound emulsion-emulsion solvent volatilization method. The microspheres prepared by the invention have a long drug-release period, good drug stability, high safety and broad application prospects.

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 Applications(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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