Thymalfasin sustained release micro-sphere preparation and preparing method thereof

Abstract

The invention provides a thymalfasin sustained release micro-sphere preparation and a preparing method thereof. The thymalfasin sustained release micro-sphere preparation comprises, by micro-sphere weight, 0.1%-30% of thymalfasin, 50%-99.9% of a biodegradable high polymer material which ranges from 5000 Dalton to 200000 Dalton in molecular weight and has the biocompatibility and 0%-20% of other acceptable auxiliary materials on pharmacy. The invention further provides the preparing method for preparing the thymalfasin sustained release micro-sphere preparation, namely a high-pressure static microcapsule molding method. By means of thymalfasin sustained release micro-spheres prepared with the method, effective embedding and sustained release of the thymalfasin are achieved, the sustained release effect can reach 40 days, the toxic and side effect of the thymalfasin can be effectively reduced, the bioavailability is improved, and the metabolic half-life is prolonged; and meanwhile, the number of drug administration times is decreased, and economic and mental burdens of a patient are relieved.

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...

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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.

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