Thymalfasin slow release microsphere preparation and preparation method thereof

A new technology of sustained-release microsphere preparation and thymus method, which is applied in the fields of pharmaceutical formulations, antiviral agents, microcapsules, etc., and can solve problems such as high temperature, difficulty in separating and purifying products, and large changes in pH value

Inactive Publication Date: 2016-09-14
山东博创生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above traditional methods are prone to aggregation and fusion, and it is difficult to separate and purify products. Most of the time and cost are spent on removing residual solvents and redundant drugs, and are not suitable for industrial production. However, spray drying, melting, and salting out methods are simple and Good reproducibility, but the preparation process is relatively intense, the temperature used is high or the pH value changes greatly, and there are high requirements for the stability of the drug. It is not suitable for peptides, protein drugs or other heat-sensitive substances. In addition, the above Thymusfaxin slow-release microspheres prepared by the method have no pores on the surface, and hollow or unconnected cavities inside, which makes the drug loading of the microspheres low, which is unfavorable for drug administration.

Method used

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  • Thymalfasin slow release microsphere preparation and preparation method thereof
  • Thymalfasin slow release microsphere preparation and preparation method thereof
  • Thymalfasin slow release microsphere preparation and preparation method thereof

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Embodiment 1

[0026] 200 mg of L-polylactic acid (PLLA) was dissolved in 5 ml of dichloromethane to obtain an oil phase of polylactic acid copolymer, and 3 mg of stabilizer Pronroni F-127 was added. Dissolve 80mg of thymofasin, 15mg of gelatin, and 0.5ml of ammonium bicarbonate in 600ml of water for injection, add the oil phase to the water phase, and use a cell disruptor for ultrasonic emulsification for 1.5min (power 200W, ultrasound 1s, interval 1s ) to form a uniform and stable W / O emulsion. Add the above solution to the newly prepared 1000ml aqueous solution of sodium alginate with a mass fraction of 2%, and use a cell disruptor to ultrasonic emulsify for 1.5min. The ultrasonic emulsification conditions are the same as above to form a uniform and stable W / O / W emulsion. The W / O / W emulsion was immediately put into a syringe, and injected into 500ml of a prepared calcium chloride solution with a mass fraction of 10% through a high-pressure microcapsule forming device, and the emulsion was...

Embodiment 2

[0028] 300 mg of L-polylactic acid (PLLA) was dissolved in 10 ml of ethyl acetate to obtain an oil phase of polylactic acid copolymer, and 3.5 mg of stabilizer Pronroni F-127 was added. Dissolve 150mg of thymofasin, 20mg of trehalose, and 4.0ml of ammonium bicarbonate in 1000ml of water for injection, add the oil phase to the water phase, and use a cell disruptor for ultrasonic emulsification for 1.5min (power 200W, ultrasound 1s, interval 1s) A uniform and stable W / O emulsion is formed. Add the above solution to 1500ml of newly prepared sodium alginate aqueous solution with a mass fraction of 5%, and use a cell disruptor to ultrasonically emulsify for 1.5min. The ultrasonic emulsification conditions are the same as above to form a uniform and stable W / O / W emulsion. The W / O / W emulsion was immediately put into a syringe, and injected into 1000ml of a prepared calcium chloride solution with a mass fraction of 8% through a high-pressure microcapsule forming device, and the emulsi...

Embodiment 3

[0030]400 mg of L-polylactic acid (PLLA) was dissolved in 10 ml of methylene chloride to obtain an oil phase of polylactic acid copolymer, and 4.8 mg of stabilizer Pronroni F-127 was added. Dissolve 100mg of thymofasin, 10mg of trehalose, and 1.0ml of ammonium bicarbonate in 800ml of water for injection, add the oil phase to the water phase, and use a cell disruptor for ultrasonic emulsification for 1.5min (power 200W, ultrasound 1s, interval 1s) A uniform and stable W / O emulsion is formed. Add the above solution to 1200ml of newly prepared sodium alginate aqueous solution with a mass fraction of 5%, and ultrasonically emulsify for 1.5min with a cell disruptor. The emulsification conditions are the same as above to form a uniform and stable W / O / W emulsion. The / O / W emulsion is immediately filled into a syringe, injected into 1200ml of a prepared calcium chloride solution with a mass fraction of 6% through a high-pressure microcapsule forming device, stirred the emulsion by mag...

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Abstract

The invention provides a thymalfasin slow release microsphere preparation and a preparation method thereof. The thymalfasin slow release microsphere preparation is a preparation prepared from thymalfasin accounting for 0.1-30% of the weight of microspheres, a biodegradable and biocompatible polymer material accounting for 50-99.9% of the weight of the microspheres and having a molecular weight of 5000-200000dalton, and other pharmaceutically acceptable auxiliary materials accounting for 0-20% of the weight of the microspheres. The invention also provides the preparation method of the thymalfasin slow release microsphere preparation. The method is a high-voltage electrostatic microcapsule molding method. The thymalfasin slow release microsphere preparation realizes effective embedding and slow releasing of thymalfasin, can continuously release for 40d, and also has the advantages of effectively reduction of the toxic and side effects of thymalfasin, improvement of the bioavailability, prolongation of the metabolism half life, administration frequency reduction, and reduction of the economy and spirit burden of patients.

Description

technical field [0001] The invention belongs to the technical field of slow-release microsphere preparations, and relates to a long-acting slow-release microsphere preparation of an immunomodulator and a preparation method thereof, in particular to a thymus method new slow-release microsphere preparation and a preparation method thereof. Background technique [0002] Thymofasin, or thymosin α1, was discovered in 1984 and secreted by the thymus as an important regulator of T lymphocytes, which is related to the regulation of cellular immunity. Thymofasin is an N-terminal acetylated acidic polypeptide consisting of 28 amino acid residues, mainly used for chronic hepatitis B and as an immune response enhancer for patients with immune impairment. [0003] As an immunomodulator, thymofasin has been confirmed to have a good curative effect, and its clinical application prospect is promising. Hepatitis B virus (HBV) infection is one of the most common viral infections in humans. T...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K9/50A61K47/34A61K38/22A61P37/04A61P1/16A61P31/20A61P35/00A61P31/18
CPCA61K9/0002A61K9/5031A61K9/5089A61K38/22
Inventor 王蕾
Owner 山东博创生物科技有限公司
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