Polypeptide sustained-release microsphere preparation and preparation method thereof

A slow-release microsphere preparation and polypeptide slow-release technology, which is applied in the field of medicine, can solve the problems of short half-life and poor patient compliance, and achieve the effects of good encapsulation rate, long drug release time and small particle size

Active Publication Date: 2017-05-17
SICHUAN KELUN PHARMA RES INST CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the short half-life, the product is injected twice a day, and frequent injections make patient compliance poor

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0102] Embodiment 1 microsphere preparation and preparation method thereof

[0103] (1) Dissolve 5g of purified 50:50 DLG 2A PLGA (polymerization ratio 1:1, PLGA inherent viscosity around 1, PLGA with carboxyl group at the end group), 0.3g of exenatide in 50ml of glacial acetic acid, forming a solution of polymer and drug;

[0104] (2) Mix 200ml of n-heptane and 200ml of silicone oil to prepare coagulant; shear the solution of polymer and medicine prepared in step (1), and add the coagulant prepared at the same time to obtain initial microspheres;

[0105] (3) Transfer the initial microspheres prepared in step (3) to a mixed solution of 1800ml n-heptane and 1800ml ethanol, and stir at 20°C for 1-2h;

[0106] (4) with 200ml 50% n-heptane-ethanol solution flushing the residual solvent on the microsphere surface that step (3) obtains;

[0107] (5) Using a multilayer sieve to collect the microspheres obtained in step (4), rinse with 50% n-heptane-ethanol solution. Dry at 4°C fo...

Embodiment 2

[0108] Embodiment 2 microsphere preparation and preparation method thereof

[0109] (1) Dissolve 5g of purified 50:50 DLG 3A PLGA, 0.3g of exenatide in 50ml of glacial acetic acid to form a solution of polymer and drug;

[0110] (2) Mix 200ml of n-heptane and 200ml of silicone oil to prepare coagulant; shear the solution of polymer and medicine prepared in step (1), and add the coagulant prepared at the same time to obtain initial microspheres;

[0111] (3) the initial microspheres prepared by step (2) are transferred to the mixed solution of 1500ml n-heptane and 1500ml ethanol;

[0112] (4) with 200ml 50% n-heptane-ethanol solution flushing the residual solvent on the microsphere surface that step (3) obtains;

[0113] (5) Using a multilayer sieve to collect the microspheres obtained in step (4), rinse with 50% n-heptane-ethanol solution. Dry at 4°C for 24h, vacuum dry at 25°C for 24h, and vacuum dry at 35°C for 24h.

Embodiment 3

[0114] Embodiment 3 microsphere preparation and preparation method thereof

[0115] (1) Dissolve 5g of purified 100 2A PLA and 0.3g of exenatide in 50ml of glacial acetic acid to form a solution of polymer and drug;

[0116] (2) Mix 200ml of n-heptane and 200ml of silicone oil to prepare coagulant; shear the solution of polymer and medicine prepared in step (1), and add the coagulant prepared at the same time to obtain initial microspheres;

[0117] (3) Transfer the initial microspheres prepared in step (2) to a mixed solution of 2100ml n-heptane and 2100ml ethanol, and stir at 20°C for 1-2h;

[0118] (4) with 200ml 50% n-heptane-ethanol solution flushing step (3) microsphere surface residual solvent that obtains;

[0119] (5) Using a multilayer sieve to collect the microspheres obtained in step (4), rinse with 50% n-heptane-ethanol solution. Dry at 4°C for 24h, vacuum dry at 25°C for 24h, and vacuum dry at 35°C for 24h.

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Abstract

The invention discloses a polypeptide sustained-release microsphere preparation. The preparation is composed of 3% to 10% by weight of exenatide or its salt as a raw material and 90% to 97% by weight of a polymer as an auxiliary material. An in-vitro initial release rate of the sustained-release microsphere preparation in 1h is less than 2%. The invention also provides a method for preparing the polypeptide sustained-release microsphere by an O/O phase coacervation method. The polypeptide sustained-release microsphere preparation has low microsphere sizes, low burst release and high entrapment efficiency, further prolongs long drug release time, can continuously release drugs for half a month or more in single-dose administration, can release drugs for 3 months, significantly reduces the frequency of administration, improves the patient's compliance, overcomes the defect of the existing peptide sustained-release microsphere preparation platform period and can get a near-zero order release curve.

Description

technical field [0001] The invention relates to a polypeptide sustained-release microsphere preparation and a preparation method thereof, belonging to the field of medicine. Background technique [0002] Most of the protein and peptide drugs with biological activity cannot be administered orally due to their low oral bioavailability. When administered by injection, the existence of proteases in the body makes the half-life of the drug in the body very short, requiring frequent injections, which increases the pain of the patient. In order to reduce dosing frequency and improve patient compliance, such drugs usually need to be developed into long-acting sustained-release preparations. [0003] Exenatide is a synthetic North American exendin, which consists of 39 amino acid residues and has a relative molecular weight of 4186.57. It is a glucagon-1 (GLP-1) receptor agonist. The known pharmacological effects of exenatide include: (1) increasing glucose-dependent insulin secret...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K47/34A61K38/22A61P3/10A61P9/12A61P3/04A61P9/04
CPCA61K9/0002A61K9/5031A61K9/5089A61K38/22
Inventor 李明苏正兴赵栋王利春王晶翼
Owner SICHUAN KELUN PHARMA RES INST CO LTD
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