Liraglutide sustained-release microsphere preparation and preparation method thereof

A slow-release microsphere preparation, liraglutide technology, applied in the direction of pharmaceutical formulations, peptide/protein components, medical preparations of non-active ingredients, etc., can solve the problem of sudden release, unsatisfactory encapsulation rate and drug loading, Poor patient compliance, frequent dosing times and other issues, to achieve the effect of sustained slow release, high drug loading, and no obvious burst release

Inactive Publication Date: 2012-05-02
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This preparation has been proven to have a good effect in improving blood sugar control and weight loss. In order to control blood sugar smoothly, daily subcutaneous injections are required. Frequent injections make patients' compliance poor, and patients suffer terribly
[0009] Liraglutide microspheres prepared by conventional methods have the disadvantages of unsatisfactory burst release, encapsulation efficiency and drug loading, and frequent administration in medical applications

Method used

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  • Liraglutide sustained-release microsphere preparation and preparation method thereof
  • Liraglutide sustained-release microsphere preparation and preparation method thereof
  • Liraglutide sustained-release microsphere preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0048] Example 1 Preparation of liraglutide sustained-release microsphere preparation by S / 0 / W double emulsification-solvent evaporation method

[0049] PLGA-PCL (polylactic acid: glycolic acid ratio is 60:40, Mw=10,000, polylactic acid-glycolic acid copolymer: polycaprolactone ratio is 1:2) 200mg dissolved in 4.0ml organic solvent (dichloro The ratio of methane:ethyl acetate is 2:1) to make the oil phase, disperse 20mg of liraglutide into the colostrum of the oil phase, disperse to form S / 0, put 50m1 of the solution containing 2%PVA in a stirring container , quickly add colostrum into the external water phase under high-speed stirring (5,000rpm) and fully homogenize. After three minutes, reduce the speed to 300rpm, add 0.75% polyvinyl alcohol solution, stir at room temperature and under reduced pressure for 6 hours, and the microspheres After hardening, centrifuge and wash, then freeze-dry. The encapsulation efficiency of liraglutide microspheres was 87%, and the particle si...

Embodiment 2

[0050] Example 2 S / O / W 2 Preparation of Liraglutide Sustained-release Microspheres by Double Emulsification-Solvent Evaporation Method

[0051] PLGA-PCL (the ratio of polylactic acid: glycolic acid is 50:50, Mw=15,000, the ratio of polylactic acid-glycolic acid copolymer: polycaprolactone is 1:4) 250mg dissolved in 2.5m1 methylene chloride For the oil phase, add 50 mg of liraglutide to the above oil phase, disperse to form S / O colostrum, put 50 ml of a solution containing 1% polyvinyl alcohol (PVA) in a stirring container, and stir the colostrum at high speed ( 10,000rpm) and quickly added to the external water phase to fully homogenize. After one minute, reduce the speed to 600rpm, add 0.5% polyvinyl alcohol solution, stir at room temperature and reduced pressure for 6 hours, centrifuge and wash the microspheres after hardening. Just freeze dry. The encapsulation efficiency of liraglutide microspheres was 92%, and the particle size was <80um.

Embodiment 3

[0052] Example 3 Preparation of Liraglutide Sustained Release Microspheres by Spray Drying

[0053] Dissolve 100mg of PLGA (the ratio of polylactic acid:glycolic acid is 75:25, Mw=10,000) in 5.0ml of organic solvent (the ratio of dichloromethane:methanol is 3:1). Disperse 20 mg of liraglutide and 2.0 mg of trehalose into 2.0 ml of water for injection, and vortex to dissolve the drug completely. Add the liraglutide solution into the organic phase, stir at 15,000 rpm for three minutes at high speed to form a W / 0 emulsion, spray it into the low-temperature ethanol covered with liquid nitrogen through a spray dryer in an atomized state; the ethanol volatilizes The dichloromethane in the PLGA droplets was extracted; the liquid nitrogen was evaporated under freezing conditions, and the microspheres were obtained by freeze-drying. The encapsulation efficiency of liraglutide microspheres was 85%, and the particle size was <80um.

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Abstract

The invention relates to a formula of a liraglutide sustained-release microsphere preparation. The preparation mainly comprises 5 to 60 parts of liraglutide and 50 to 200 parts of biodegradable substrate material, wherein the biodegradable substrate material is polylactic acid (PLA), polylactic acid-glycollic acid (PLGA) block copolymer, glycolide-lactide (PLCG) copolymer, polyglycolic acid (PGA), polycaprolactone (PCL), polylactic acid-glycollic acid-polycaprolactone (PLGA-PCL) copolymer or PLCG-polycaprolactone (PLCG-PCL) or a mixture of any two or more than two of the compounds, preferably the PLGA-PCL copolymer. The sustained-release microspheres have a high encapsulating rate and a good sustained-release effect.

Description

technical field [0001] The invention relates to a liraglutide pharmaceutical composition and a preparation method thereof, in particular to a liraglutide sustained-release microsphere preparation and a preparation method thereof. Background technique [0002] With the rapid development of biotechnology, more and more peptide and protein drugs have been developed, and have shown many unique curative effects in clinical applications, such as liraglutide, teriparatide, alanorelin, etc. . However, due to the short biological half-life and poor stability of peptide and protein drugs, they are easily metabolized by enzymes in the body and difficult to absorb in the gastrointestinal tract, so long-term and frequent injections are required, which hinders their convenient, extensive and effective clinical application. use. [0003] Liraglutide is a human glucagon-like peptide-1 (GLP-1) analog developed by Novo Nordisk. It consists of 31 peptide amino acid residues, and its molecula...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/34A61K38/26A61P3/10
Inventor 颜携国潘俊锋马亚平袁建成
Owner HYBIO PHARMA
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