Asenapine microsphere agent and preparation method thereof

Abstract

The invention discloses an asenapine slow-release microsphere agent and a preparation method thereof. The microsphere agent is prepared from asenapine or salts and polyesters thereof, wherein the weight percentage of the asenapine or salts thereof counted by asenapine is 5-50%, and the weight percentage of the polyesters is 50-95%. The preparation method comprises the following steps: (1) conducting weighing; (2) adding the polyester material into an organic solvent for completely dissolving the polyester material to obtain a settled solution, then dissolving or suspending the medicine asenapine or the salts thereof into the settled solution to be used as an oil phase; stirring or shearing the oil phase at high speed to form a homogeneous oil phase; and in case of need, adding a right amount of acid for salifying the asenapine; and (3) preparing the microsphere agent by a microdroplet generating device, or a spray drying method, or an atomizing extraction method. The microsphere agent provided by the invention has relatively high production efficiency, the D50 particle sizes of the prepared microspheres are all below 80mu m, are controllable and are concentrated in distribution, the drug-loading rate is as high as 45%, and the encapsulation rate is above 85%.

Description

technical field [0001] The invention relates to the field of asenapine medicine, in particular to an asenapine microsphere preparation and a preparation method thereof. Background technique [0002] Schizophrenia is a disease that seriously affects human health. Currently, patients account for about 1% of the world's total population. Schizophrenia has positive symptoms such as hallucinations, delusions, thinking and behavior disorders, and negative symptoms such as apathy, poor thinking, and decreased will. Once suffering from schizophrenia, patients need to take anti-schizophrenia drugs continuously for life. How to improve the curative effect of antipsychotic drugs, reduce adverse reactions such as extrapyramidal side effects, reduce the number of administrations, and improve patient compliance is a current direction for the development of antipsychotic drugs. [0003] Asenapine (asenapine) is a new atypical antipsychotic drug for the treatment of adults with acute schi...

AI Technical Summary

Problems solved by technology

[0016] CN201380039623 discloses a patch of asenapine and its manufacture method, but the transdermal property of asenapine is relatively poor, need to add quantitative penetration enhancer to improve the skin permeability of medicine, even so, The maximum effective utilization rate of the drug is only about 60%

Although it is convenient to use, the drug loss is also high

[0017] CN102596172A discloses an injection containing asenapine and a treatment method for the period of use. An aqueous buffer solution containing suspended particles of asenapine hemipamoate is used to provide reservoir administration through IM injection, which can last for 2 weeks. , 3 weeks or 4 weeks of effective treatment, but according to the clinical manifestations of administration-related extreme sedation and reversible coma events caused by olanzapine pamoate suspension particle injection in the same dosage form, the suspension particle injection of this product still exists Risk of burst and rapid release, FDA approved only for depot injection under strict patient monitoring conditions

Therefore, there are still certain limitations in the use of dosage forms of this design.

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