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Exenatide release microsphere preparation, preparation method and application thereof

A technology of slow-release microsphere preparations and exenatide, which is applied in the direction of pharmaceutical formulations, peptide/protein components, and medical preparations of non-active ingredients, which can solve the problems of poor patient compliance and unacceptability, and reduce drug administration. Frequency, weight control, effect of improving treatment effect

Inactive Publication Date: 2010-03-03
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, because the half-life of exenatide is only 2.4 hours (Byetta instructions), in order to control blood sugar smoothly, subcutaneous injections need to be administered twice a day. Frequent injections make patients less compliant, especially those who need insulin injections more difficult to accept

Method used

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  • Exenatide release microsphere preparation, preparation method and application thereof
  • Exenatide release microsphere preparation, preparation method and application thereof
  • Exenatide release microsphere preparation, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Example 1 Preparation of Exenatide Sustained-release Microspheres by W1 / O / W2 Solvent Evaporation

[0078] Dissolve 800mg of PLGA (RG502H, LA:GA=50:50, Mw=10000) in 3.0ml of dichloromethane to make an oil phase, dissolve 20mg of exenatide in 0.05ml of double distilled water (containing 12.5mg of gelatin) Form the inner water phase, add it to the above oil phase, ultrasonic emulsification, form W1 / O colostrum, put 50ml of 2% PVA solution in a stirring container, quickly add the colostrum to the outer water under high-speed stirring (1200rpm) Fully homogenize in the phase, after three minutes, reduce the rotating speed to 400 rpm, add 0.75% polyvinyl alcohol solution, stir at room temperature for 4 hours, centrifuge and wash the microspheres after hardening, and freeze-dry. The encapsulation efficiency of the exenatide microspheres is 90%, and the particle size is less than 100 μm.

Embodiment 2

[0079] Example 2 Preparation of Exenatide Sustained-release Microspheres by W1 / O / W2 Solvent Evaporation

[0080] Dissolve 250mg of PLGA (RG502H, LA:GA=25:75, Mw=5000) in 2.5ml of dichloromethane to make an oil phase, and dissolve 10mg of exenatide in 0.05ml of double distilled water (containing 10mg of gelatin) to form For the inner water phase, add it to the above oil phase, ultrasonic emulsification, and form W1 / O colostrum, put 50ml of 1% PVA solution in a stirring container, and quickly add the colostrum to the outer water phase under high-speed stirring (1200rpm) After three minutes, reduce the rotation speed to 400rpm, add 0.5% polyvinyl alcohol solution, stir at room temperature for 4 hours, centrifuge and wash the microspheres after hardening, and freeze-dry. The encapsulation efficiency of the exenatide microspheres was 85%, and the particle size was less than 90 μm.

Embodiment 3

[0081] Example 3 Preparation of Exenatide Sustained-release Microspheres by W1 / O / W2 Solvent Evaporation

[0082] Dissolve 2000mg of PLGA (RG502H, LA:GA=75:25, Mw=20000) in 5.0ml of dichloromethane to make an oil phase, and dissolve 30mg of exenatide in 0.05ml of double distilled water (containing 15mg of gelatin) to form For the inner water phase, add it to the above-mentioned oil phase, ultrasonic emulsification, and form W1 / O colostrum, put 50ml of 3% PVA solution in a stirring container, and quickly add the colostrum to the outer water phase under high-speed stirring (1200rpm) After three minutes, reduce the rotation speed to 400rpm, add 1% polyvinyl alcohol solution, stir at room temperature for 4 hours, centrifuge and wash the microspheres after hardening, and freeze-dry. The encapsulation efficiency of the exenatide microspheres was 97%, and the particle size was less than 120 μm.

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Abstract

The invention discloses an Exenatide release microsphere preparation mainly comprising the following components in percentage by weight: 0.5-10 percent of Exenatide and 85-99 percent of polylactic acid-glycolic acid copolymer. The invention also discloses a preparation method and an application of the Exenatide release microsphere preparation. The Exenatide release microsphere preparation not onlycan prolong the action time of the Exenatide in the body and reduce the medicine application frequency, but also can maintain the effective blood-medicine concentration of the Exenatide and improve the treatment effect.

Description

technical field [0001] The invention relates to exenatide pharmaceutical preparations, in particular to an exenatide slow-release microsphere preparation and its preparation method and application. Background technique [0002] Exendin-4 is a natural glucagon-like peptide-1 isolated from the salivary glands of the Gila monster (Heloderma suspectum) distributed in southwestern North America. , an analog of GLP-1). Exenatide is a synthetic exendin (exendin-4), which consists of 39 amino acid residues, and its amino acid sequence is as follows: [0003] H-His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu- Trp-Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-Gly-Ala-Pro-Pro-Pro-Ser-NH2 (Eng et al., J. Biol. Chem., 267:7402-05, 1992) . [0004] Exenatide has 53% homology with mammalian GLP-1, 48% homology with human glucagon, and has a high degree of homology to GLP-1 receptor (GLP-1R). Affinity, its ability to bind to GLP-1R is 2.4 times that of...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K38/17A61K47/34A61P3/10A61P3/04
Inventor 钟延强高静宣吉明张翮邹豪鲁莹孙治国陈琰俞媛
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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