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GLP-I analogue liraglutide sustained-release microspheres and preparation method thereof

A sustained-release microsphere preparation and technology of sustained-release microspheres, which are used in drug combinations, pharmaceutical formulations, non-active components of polymer compounds, etc., can solve the problems of reduced dosing frequency and poor patient compliance.

Inactive Publication Date: 2013-06-12
SHENZHEN JYMED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Liraglutide injection has been proven to have a good effect in the treatment of type II diabetes, but it needs to be injected once a day, which makes the patient's compliance poor. Therefore, it is prepared as a sustained-release preparation, and the frequency of administration is significantly reduced. acceptance of

Method used

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  • GLP-I analogue liraglutide sustained-release microspheres and preparation method thereof
  • GLP-I analogue liraglutide sustained-release microspheres and preparation method thereof
  • GLP-I analogue liraglutide sustained-release microspheres and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0022] Weigh 20 mg of liraglutide and dissolve it in distilled water to obtain the inner water phase; weigh 1000 mg of PLGA (polymerization ratio = 1:3) and dissolve it in dichloromethane to obtain the oil phase. Preparation concentration is 50ml of the PVA solution of 5% and the PVA solution of 0.5% is 500ml. First transfer the liraglutide solution into the dichloromethane solution dissolved with PLGA, put it on an emulsification disperser at high speed (30000rpm) for 30 seconds at room temperature, and then transfer the obtained W / O emulsion to 20ml with a concentration of 5% Put it in the PVA solution of 5000rpm on the emulsification disperser, and mix it evenly for 1 minute to get the W / O / W type double emulsion. Stir at low speed for 2 hours, centrifuge, collect the obtained microspheres, wash with distilled water several times, then collect by centrifugation, freeze-dry, and pack into liraglutide sustained-release microsphere preparations with an actual drug loading of 4....

Embodiment 2

[0025]Weigh 15 mg of liraglutide and dissolve it in distilled water to obtain the inner water phase; weigh 1000 mg of PLGA (polymerization ratio = 1:1) and dissolve it in dichloromethane to obtain the oil phase. Preparation concentration is 50ml of the PVA solution of 5% and the PVA solution of 0.5% is 500ml. First transfer the liraglutide solution into the dichloromethane solution dissolved with PLGA, put it on an emulsification disperser at high speed (30000rpm) for 30 seconds at room temperature, and then transfer the obtained W / O emulsion to 20ml with a concentration of 5% In the PVA solution, place it on an emulsifying disperser at a speed of 5000rpm, and mix it evenly for 1 minute to obtain a W / O / W type double emulsion, move it into 500ml of 0.5% PVA solution, place it on a mechanical stirrer, Stir at low speed for 2 hours, centrifuge, collect the obtained microspheres, wash with distilled water several times, then collect by centrifugation, freeze-dry, and pack into lir...

Embodiment 3

[0028] Weigh 25 mg of liraglutide and dissolve it in distilled water to obtain the inner water phase; weigh 500 mg of PLA and 1500 mg of PLGA (polymerization ratio = 3:1) and dissolve it in dichloromethane to obtain the oil phase. Preparation concentration is 100ml of 5% PVA solution and 1000ml of 0.5% PVA solution. First transfer the liraglutide solution into the dichloromethane solution dissolved with PLA and PLGA, place it on an emulsification disperser at high speed (30000rpm) for 30 seconds at room temperature, and then transfer the obtained W / O emulsion to 20ml with a concentration of 5% PVA solution, placed on an emulsifying disperser at a speed of 5000rpm, and homogenized for 1 minute to obtain a W / O / W type double emulsion, moved into 500ml of 0.5% PVA solution, placed on a mechanical stirrer, and Stir at a low speed of 500rpm for 2 hours, centrifuge, collect the obtained microspheres, wash with distilled water several times, then collect by centrifugation, freeze-dry,...

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Abstract

The invention discloses a GLP-I analogue liraglutide sustained-release microspheres and a preparation method thereof. The GLP-I analogue liraglutide sustained-release microspheres comprise, by weight, 0.5 to 30% (w / w) of GLP-I analogue liraglutide, 70 to 99.5% of a polymer which has the molecular weight of 5000 to 300000 dalton, can be biodegraded and has biocompatibility, and 0 to 10% of pharmaceutically acceptable auxiliary materials. The GLP-I analogue liraglutide sustained-release microspheres have the average grain size of 5 to 40 micrometers and an encapsulation ratio more than 90%. The GLP-I analogue liraglutide sustained-release microspheres have a sustained-release period of several days or several months, obviously reduce use frequency, improve GLP-I analogue liraglutide bioavailability, reduce toxic and side effects and are conducive to clinical treatment.

Description

Technical field: [0001] The invention relates to a slow-release microsphere preparation for treating type II diabetes, in particular to a slow-release microsphere preparation containing a GLP-I analog liraglutide and a preparation method thereof. Background technique: [0002] Diabetes mellitus is a group of metabolic disorders characterized by hyperglycemia due to defective insulin secretion and / or insufficient insulin action. The chronic hyperglycemic state of diabetes is significantly associated with long-term complications, namely damage, dysfunction, and failure of numerous organs, especially the kidneys, eyes, nerves, heart, and blood vessels. The comprehensive treatment of diabetes should not only focus on reducing blood sugar to near normal levels, but also actively correct metabolic abnormalities and reduce cardiovascular risk factors. [0003] Diabetes is divided into type I diabetes and type II diabetes. Type I diabetes is caused by the failure of pancreatic beta...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K38/26A61K47/34A61K47/38A61K47/42A61P3/10
Inventor 支钦李新宇姚志勇
Owner SHENZHEN JYMED TECH
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