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Lixisenatide controlled-release microspheres and preparation method thereof

A technology of sustained-release microspheres and lixisenatide, applied in the field of medicine, can solve the problems of unfavorable disease control, peak and valley of drug concentration, poor compliance with treatment, etc., and achieve stable and sustained drug release, good tissue compatibility, In vitro release smooth effect

Inactive Publication Date: 2014-12-31
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] However, the half-life of GLP-1 receptor agonists in the body is very short. Among the GLP-1 receptor agonist antidiabetic drugs, lixisenatide is a product that is administered once a day, which greatly limits its use in type 2 diabetes. application in therapy
Since diabetes is a chronic disease that requires long-term treatment, daily injections of lixisenatide make patients miserable and poor compliance with treatment
At the same time, repeated administration will produce peak and valley drug concentration in the body, making the drug effect unable to be continuously and stably exerted, which is not conducive to disease control

Method used

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  • Lixisenatide controlled-release microspheres and preparation method thereof
  • Lixisenatide controlled-release microspheres and preparation method thereof
  • Lixisenatide controlled-release microspheres and preparation method thereof

Examples

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Effect test

Embodiment 1

[0043] Embodiment 1: Preparation of lixisenatide sustained-release microspheres of the present invention

[0044] Dissolve 800mg of PLGA (LA:GA=50:50, Mw=10000) in 3.0ml of dichloromethane to make the oil phase, and dissolve 50mg of lixisenatide in 0.5ml of water for injection (containing 12.5mg of gelatin) to form the inner phase Water phase, add it to the above oil phase, ultrasonic emulsification to form W / O colostrum, put 50ml of pVA solution containing 2% (mass percentage) in a stirring container, and quickly add colostrum under high-speed stirring (5000rpm) Fully homogenize in the external water phase to obtain double emulsion. After three minutes, slow down the rotation speed to 300rpm to stir the double emulsion, stir at room temperature for 4 hours, separate and wash the microspheres after hardening, and freeze-dry them. Lixisenatide microspheres The encapsulation rate is 88%, 45μm≤particle size≤65μm.

[0045] Determination of the release rate of lixisenatide sustain...

Embodiment 2

[0046] Embodiment 2: Preparation of lixisenatide sustained-release microspheres of the present invention

[0047] Dissolve 250mg of PLGA (LA:GA=25:75, Mw=5000) in 5ml of ethyl acetate to form an oil phase, dissolve 29mg of lixisenatide in 0.75ml of water for injection (containing 12mg of gelatin) to form an inner water phase, Add it to the above oil phase, ultrasonic emulsification, to form W / O colostrum, put 50ml of pVA solution containing 3% (mass percentage) and 0.01% poloxamer solution in a stirring container, and put the colostrum under high-speed stirring (7000rpm) quickly added to the external water phase and fully homogenized to obtain double emulsion. After three minutes, slow down the speed (400rpm) to stir the double emulsion. Stir at 10-12°C for 4 hours. After hardening, the microspheres were separated and washed, and freeze-dried That is, the encapsulation efficiency of lixisenatide microspheres is 89%, and 45 μm≤particle size≤65 μm.

[0048] Determination of the...

Embodiment 3

[0049] Embodiment 3: Preparation of lixisenatide sustained-release microspheres of the present invention

[0050] Dissolve 96mg of PLGA (LA:GA=20:80, Mw=20000) in 1.0ml of dichloromethane to make the oil phase, dissolve 12mg of lixisenatide in 1.5ml of water for injection (containing 12.0mg of gelatin) to form the inner Water phase, add it to the above oil phase, ultrasonic emulsification to form W / O colostrum, put 50ml of 1% (mass percentage) pVA and 0.4% sodium chloride solution in a stirring container, and stir the colostrum at high speed Quickly add (3000rpm) into the external water phase to fully homogenize the double emulsion. After three minutes, slow down the rotation speed (50rpm) to stir the double emulsion, stir at 8-15°C for 4 hours, separate and wash the microspheres after hardening, and freeze Just dry, the encapsulation rate of lixisenatide microspheres is 90%, 45μm≤particle size≤65μm.

[0051] Determination of the release rate of lixisenatide sustained-release...

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Abstract

The invention related to the technical field of medicine and discloses lixisenatide controlled-release microspheres and a preparation method thereof. The lixisenatide controlled-release microspheres are prepared from lixisenatide, a biodegradable material and one or more stabilizing agents as controlled-release microsphere components and a surfactant aqueous solution as an external water phase by a water / oil / water multiple emulsion-solvent evaporation method, wherein the biodegradable material is polylactic acid, a lactic acid-glycolic acid polymer or polyglycolic acid and the one or more stabilizing agents are selected from polyol, sugar, inorganic salt, amino acids, polymers, human serum albumin and fatty glyceride. The lixisenatide controlled-release microspheres reduce administration frequency, can stably produce curative effects for a long time, have no toxic or side effect and good histocompatibility, can be applied by injection and non-injection methods and can be popularized and used in diabetes treatment.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to lixisenatide sustained-release microspheres and a preparation method thereof. Background technique [0002] Lixisenatide, known in English as lixisenatide, is a glucagon-like peptide-1 (GLP-1) receptor agonist based on the C-terminal 6 of the GLP-1 analogue Exendin-4 with hypoglycemic activity. A novel GLP-1 analogue synthesized by modifying two lysine residues can resist degradation by dipeptidyl peptidase IV (DPP4) in vivo. [0003] GLP-1 is a natural peptide substance in the human body. It can be produced and released by the small intestine within a few minutes after a meal. It can inhibit the secretion of glucagon from pancreatic α cells and stimulate the secretion of insulin from pancreatic β cells. It is inactive when blood sugar is normal or low. It is suggested that the risk of hypoglycemia is low when using GLP-1 receptor agonists. GLP-1 receptor agonists are now wid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K38/26A61P3/10
Inventor 郑春莲刘建马亚平袁建成
Owner HYBIO PHARMA
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