Asenapine microsphere agent and preparation method thereof

A technology of microspheres and preparations, which is applied in the field of asenapine microsphere preparations and its preparation, can solve the problems of only 60% of the maximum effective drug utilization rate, high drug loss, poor transdermal properties of asenapine, etc., and achieve excellent Sustained release performance, high production efficiency, and low burst release rate

Inactive Publication Date: 2017-09-08
SHENZHEN FONCOO PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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 provi...

Method used

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  • Asenapine microsphere agent and preparation method thereof
  • Asenapine microsphere agent and preparation method thereof
  • Asenapine microsphere agent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Preparation of asenapine microspheres sustained release for 1 week

[0052] Table 1 Embodiment 1 prescription composition

[0053] Raw materials prescription one Asenapine Maleate 2.25g (calculated as Asenapine) PLGA (about 20000) 7.00g (Model 5050) Dichloromethane 120ml

[0054] Preparation

[0055] Take respectively asenapine maleate and PLGA (model is 5050, molecular weight is 20000) of recipe quantity, measure the dichloromethane of prescription quantity, PLGA is dissolved in dichloromethane, then asenapine maleate Gently add into the dichloromethane solution dissolved in PLGA, stir while adding, keep stirring and shearing for 10-15 minutes, ultrasonic for 1-2 minutes, to obtain a homogeneous oil phase. Spray-dry the homogeneous oil phase under stirring, adjust the spray atomization device, control the size of the sprayed droplets, control the drying temperature at 35-40°C, and control the particle size D50 of the prepared micro...

Embodiment 2

[0057] Preparation of Asenapine Microspheres Sustained Release for 2 Weeks

[0058] Table 2 embodiment 2 prescription composition

[0059] Raw materials Prescription two Asenapine Maleate 2.25g (calculated as Asenapine) PLGA (about 55000) 7.50g (Model 5050) Dichloromethane 125ml

[0060] Preparation:

[0061] Take respectively asenapine maleate and PLGA (model is 5050, molecular weight is 55000) of recipe quantity, measure the dichloromethane of recipe quantity, PLGA is dissolved in dichloromethane, then asenapine maleate Gently add into the dichloromethane solution dissolved in PLGA, stir while adding, keep stirring and shearing for 10-15 minutes, ultrasonic for 1-2 minutes, to obtain a homogeneous oil phase. Spray-dry the homogeneous oil phase under stirring, adjust the spray atomization device, control the size of the sprayed droplets, and control the drying temperature at 35-40°C, and control the particle size D50 of the prepared micro...

Embodiment 3

[0063] Preparation of Asenapine Microspheres Sustained Release for 3 Weeks

[0064] Table 3 Embodiment 3 prescription composition

[0065] Raw materials Prescription Three Asenapine Maleate 2.25g (calculated as Asenapine) PLGA (about 25000) 3.50g (model 5050) PLGA (about 55000) 4.50g (Model 7525) Dichloromethane 130ml

[0066] Preparation:

[0067] Take respectively the asenapine maleate of prescription quantity, the PLGA of different models and molecular weight (model is respectively 5050 and 7525; Molecular weight is 25000 and 55000 respectively), measures the dichloromethane of prescription quantity, PLGA is dissolved in two Add maleic acid asenanate slowly to the PLGA-dissolved dichloromethane solution in chloromethane, stir while adding, keep stirring and shearing for 10-15 minutes, and ultrasonic for 1-2 minutes to obtain a homogeneous oil phase. Spray-dry the homogeneous oil phase under stirring, adjust the spray atomization ...

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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...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/34A61K31/407A61P25/18
Inventor 黄伟棠王秋成闫鹏
Owner SHENZHEN FONCOO PHARMACEUTICAL CO LTD
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