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Microsphere preparation method for adjusting and controlling release behavior of risperidone microspheres and for controlling size thereof

A technology of risperidone and microspheres, which is applied in the fields of nervous system diseases, powder delivery, drug combination, etc., can solve the problems that the encapsulation rate is difficult to control, the problem of particle size cannot be overcome, and there is no innovation, so as to achieve good redispersibility Effect

Inactive Publication Date: 2011-09-21
SHANGHAI JIAO TONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Similarly, Shen Kaoxiang and others applied for "Risperidone Sustained Release Microspheres, Its Preparation Method and Use" and there is no innovation in the method of preparing microspheres, all of which are conventional methods, which cannot overcome the shortcomings of preparing risperidone microspheres, such as Particle size of microspheres, encapsulation efficiency and other issues and it is difficult to control the quality of microspheres

Method used

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  • Microsphere preparation method for adjusting and controlling release behavior of risperidone microspheres and for controlling size thereof
  • Microsphere preparation method for adjusting and controlling release behavior of risperidone microspheres and for controlling size thereof
  • Microsphere preparation method for adjusting and controlling release behavior of risperidone microspheres and for controlling size thereof

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Embodiment

[0035] ① Weigh a certain amount of PLGA or PLA and add it to 1g of dichloromethane, vortex to dissolve, and set aside;

[0036] ② Weigh 50 mg of risperidone and add it to shake to dissolve, then suspend an appropriate amount of alkali in this solution to obtain a suspension;

[0037] ③Then transfer the suspension to the SPG film emulsion instrument, select a film emulsion with a pore size of 19.96 μm, adjust the pressure, and transfer the prepared microspheres into 1L of 4%PVA+5%NaCl solution by weight, to Stir and solidify at a speed of 150 rpm for 3 hours.

[0038] ④Use a clean vial to collect the microspheres that have completed step ③, wash them 5 times with distilled water, put them in a -2°C refrigerator overnight, and then take them out and vacuum freeze-dry them for 24 hours at a pressure lower than 0.05mbar.

[0039] According to the degradation cycles of PLGA and PLA with different molecular weights provided by Lakershore Company, high-viscosity PLA (IV=0.71, MW=109...

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Abstract

The invention relates to a microsphere preparation method for adjusting and controlling the release behavior of risperidone microspheres and for controlling the size thereof, belonging to the technical field of nano-medicaments. The preparation method comprises the steps of: firstly, adding a sustained-release or controlled-release functional material to one or the mixture of dichloromethane, ethyl acetate and acetonitrile, swirling and dissolving to obtain an organic solution of the sustained-release or controlled-release functional material; then adding particles containing risperidone and an alkaline matter to the organic solution of the sustained-release or controlled-release functional material, i.e. stirring or swirling in the oil phase to evenly disperse to form even suspension; and adding the suspension to SPG (Shirasu Porous Glass) membrane emulsion with different bore diameters, enabling the suspension to enter brine containing a surfactant through the membrane emulsion by adjusting the pressure, stirring to form microspheres, and transferring into the brine for solidifying to finish preparation. The biodegradable risperidone microsphere sustained-release preparation prepared by the invention has quick effect taking speed and long drug release time, the particle size of the microspheres is controllable, the envelop rate is high, and the quality of the risperidone microspheres is controllable.

Description

technical field [0001] The invention relates to a method in the technical field of nanomedicine, in particular to a method for preparing microspheres for regulating the release behavior of risperidone microspheres and controlling the size of the microspheres. Background technique [0002] Risperidone is a derivative of benzisoxazole, which is a new generation of antipsychotics. Its active ingredient, risperidone, is a selective monoamine antagonist with unique properties. It has high affinity with 5-HT2 (serotonin) receptors and dopamine D2 receptors. Risperidone also binds to α1-adrenergic receptors, and with lower affinity to H1-histamine receptors and α2-adrenergic receptors. Risperidone does not bind to cholinergic receptors. [0003] Risperidone can be completely absorbed after oral administration, and reaches the peak plasma concentration within 1-2 hours, and its absorption is not affected by food. Risperidone can be rapidly distributed in the body, and the distrib...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/519A61P25/18
Inventor 袁伟恩金拓吴飞胡振华郑瑞媛许丹
Owner SHANGHAI JIAO TONG UNIV
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