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Thymalfasin sustained-release microspheres and preparation method thereof

A thymosin, slow-release microsphere technology, applied in the field of medicine, can solve the problems of reduced product purity, solvent residue, preparation hazards, etc., and achieve the effect of stable drug release, less impurities, and continuous release.

Inactive Publication Date: 2013-12-11
HYBIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the active ingredient can be fully dispersed into the polymer in this case, there will be a problem of solvent residue, which will cause certain harm to the preparation in therapeutic applications, and the organic solvent has low toxicity, and it is often necessary to completely remove the solvent residue. Expensive and complicated, but also lead to a decrease in the purity of the product and an increase in impurities
In addition, during the preparation process, the contact of thymofasin with the water phase and the oil-water interface of the organic phase caused the denaturation of the polypeptide protein, the formation of multimers and the initiation of immunogenicity, resulting in toxic reactions to the human body

Method used

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  • Thymalfasin sustained-release microspheres and preparation method thereof
  • Thymalfasin sustained-release microspheres and preparation method thereof
  • Thymalfasin sustained-release microspheres and preparation method thereof

Examples

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Effect test

Embodiment 1

[0035] Example 1: Preparation of new sustained-release microspheres of thymus method of the present invention

[0036] The commercially available Thymus Faxin is dissolved in water, filtered and sterilized, and then lyophilized and sieved to collect Thymus Faxin powder below 500 mesh. PLGA (polylactic acid glycolic acid, LA:GA=50:50, purchased from Lakeshore Biomaterials, intrinsic viscosity 0.15-0.25dL / g) was pulverized by a ball mill at 10℃, and then sieved to collect powder below 80 mesh . The trehalose is pulverized by a ball mill, and then sieved to collect powder below 500 mesh.

[0037] Add 40g of PLGA, 0.2g of trehalose and 3g of thymus method powder into the mixer and mix for 10 minutes. Put the above mixture into a twin-screw extruder (purchased from Thermo Fisher Scientific), and adjust the melt extrusion temperature of the four sections of the extruder at different temperature control zones to 80°C (rotating speed 160 revolutions per minute). Carry out heating compre...

Embodiment 2

[0039] Example 2: Preparation of new sustained-release microspheres of thymus method of the present invention

[0040] The commercially available Thymus Faxin is dissolved in water, filtered and sterilized, and then lyophilized and sieved to collect Thymus Faxin powder below 500 mesh. The PLGA (polylactic acid glycolic acid, LA: GA=75:25, purchased from Lakeshore Biomaterials, with an intrinsic viscosity of 0.32-0.44dL / g) was pulverized by a ball mill at 12°C, and then sieved to collect powder below 80 mesh .

[0041] Add 40g of PLGA and 2g of Thymus Faxin powder into the mixer and mix for 10 minutes. Put the above mixture into a twin-screw extruder (purchased from Thermo Fisher Scientific), adjust the melt extrusion temperature of the four sections of the extruder at different temperature control zones to 85°C (rotating speed 160 revolutions per minute). Carry out heating compression melt extrusion, the obtained molten extrudate is drawn into a long strip with a diameter of 2mm ...

Embodiment 3

[0043] Example 3: Preparation of new sustained-release microspheres of thymus method of the present invention

[0044] The commercially available Thymus Faxin is dissolved in water, filtered and sterilized, and then lyophilized and sieved to collect Thymus Faxin powder below 500 mesh. The polylactic acid (intrinsic viscosity 0.25-0.35dL / g, purchased from Lakeshore Biomaterials) was pulverized by a ball mill at 12° C., and then sieved to collect powder with 80 meshes or less.

[0045] Add 30 g of polylactic acid and 2 g of thymus method powder into the mixer and mix for 10 minutes. Put the above mixture into a twin-screw extruder (purchased from Thermo Fisher Scientific), and adjust the melt extrusion temperature of the four sections of the extruder at different temperature control zones to 95°C (rotating speed 160 revolutions per minute). Carry out heating compression melt extrusion, the obtained molten extrudate is drawn into a long strip with a diameter of 2mm on a tractor, and ...

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Abstract

The invention relates to the technical field of medicines and discloses thymalfasin sustained-release microspheres and a preparation method thereof. The method comprises the following steps: freeze-drying and sieving an aqueous solution of thymalfasin; collecting the thymalfasin powder; grinding and sieving polylactic acid or a polylactide-co-glycolide acid (PLGA); mixing the obtained polymer powder and the thymalfasin powder to obtain a mixture of raw and accessory materials; melting and extruding the mixture of raw and accessory materials to obtain a hot-melting extrudate; cooling to cure the hot-melting extrudate; cutting, grinding and sieving to obtain the thymalfasin sustained-release microspheres. According to the invention, the thymalfasin sustained-release microspheres are prepared by a hot-melting extrusion technology without needing an organic solvent, the problem of residual organic solvent is completely avoided, a few impurities are contained, and the drug release is steady; an advantage of continuously releasing the thymalfasin dose is realized, thus the administration time is reduced, the administration pain of a patient is eased, and the thymalfasin sustained-release microspheres are suitable to be popularized and applied to treatment.

Description

Technical field [0001] The invention relates to the technical field of medicine, in particular to a new sustained-release microsphere by thymus method and a preparation method thereof. Background technique [0002] Thymosin, or thymosin a1, is an N-terminal acetylated acidic peptide consisting of 28 amino acid residues. It is mainly used for chronic hepatitis B and as a vaccine immune response enhancer for immunocompromised patients. [0003] As an immunomodulator, Thymus method is often used clinically to treat patients with chronic viral infections, tumors and immunodeficiency as adjuvant therapy, and as a vaccine enhancer, the clinical application prospect is very broad. As far as hepatitis B is concerned, hepatitis B virus (HBV) infection is one of the most common viral infections in humans. There are about 300 million people with chronic HBV infection in the world, most of which are in Asia. Chronic HBV carriers account for about 10%-15% of the population in my country, and ...

Claims

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Application Information

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IPC IPC(8): A61K38/22A61K9/16A61K9/10A61K47/34A61J3/00A61P1/16A61P31/14A61P31/20A61P37/02A61P37/04A61P35/00
Inventor 刘慧陶安进马亚平袁建成
Owner HYBIO PHARMA
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