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Sustained-release microsphere containing risperidone and preparation method thereof

A slow-release microsphere preparation, a technology of risperidone, which is applied in the directions of medical preparations containing active ingredients, medical preparations without active ingredients, microcapsules, etc. It is relatively expensive and other problems, and the preparation method is simple and easy to implement, the encapsulation rate is improved, and the irritation is reduced.

Inactive Publication Date: 2008-10-29
INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The risperidone long-acting injection launched in the UK in 2003 uses PLGA with a ratio of LA / GA of 75:25 for sustained release for 2 weeks, and the price is nearly 90 pounds, which is relatively expensive
Moreover, it was found through experiments that risperidone 60 It is easy to change color after Co irradiation sterilization. However, the microsphere preparation is not resistant to high temperature. There are only two sterilization methods at present. One is aseptic operation in the whole process, and the other is 60 Co irradiation
The cost of the former is very high, and it is still difficult to achieve in China

Method used

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  • Sustained-release microsphere containing risperidone and preparation method thereof
  • Sustained-release microsphere containing risperidone and preparation method thereof
  • Sustained-release microsphere containing risperidone and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0022] The preparation of the risperidone microspheres of embodiment 1 slow-release 30 days

[0023] Take 1.8 g of PLGA (molecular weight 20000, LA / GA 60:40) and tert-butyl p-hydroxyanisole (BHA) dissolved in an organic solvent to form an oil phase. The organic solvent is dichloromethane (DCM) or a mixture of dichloromethane and methanol. Dissolve 500mg of risperidone sample in the above oil phase, and mix evenly by ultrasonic. Weigh an appropriate amount of PVA in double-distilled water, dissolve it fully in a water bath at 50°C, and adjust its concentration to 5% as the water phase. Inorganic salts are added to the aqueous dispersion medium solution. Inject the above oil phase into 150ml of PVA solution, stir at 1500rpm, dilute the concentration of PVA in the water phase to 1.5% after 5 minutes, and stir magnetically at room temperature for 3-5 hours to obtain the risperidone microsphere suspension. Then washed, centrifuged and dried. The average particle size is about 1...

Embodiment 2

[0024] Preparation of risperidone microspheres of embodiment 2 sustained release for 45 days

[0025] Take 1.8g of PLGA (molecular weight is 25000, LA / GA 90:10) and BHA are dissolved in organic solvent to make oily phase. The organic solvent is dichloromethane (DCM) or a mixture of dichloromethane and methanol. Dissolve 500mg of risperidone sample in the above oil phase, and mix evenly by ultrasonic. Weigh an appropriate amount of PVA in double-distilled water, dissolve it fully in a water bath at 50°C, adjust the concentration to 5% as the water phase, and add inorganic salts to the water phase dispersion medium solution. Inject the above oil phase into 150ml of PVA solution, stir at 1500rpm, dilute the concentration of PVA in the water phase to 1.5% after 5 minutes, and stir magnetically at room temperature for 3-5 hours to obtain the risperidone microsphere suspension. Then washed, centrifuged and dried. The average particle size is about 15 μm.

Embodiment 3

[0026] Example 3 Preparation of Risperidone Microspheres by Single Emulsion Method

[0027] 1.8 g of PLGA (molecular weight 20000, LA / GA 60:40) was dissolved in an organic solvent to form an oil phase. The organic solvent is ethyl acetate (DCM) or a mixture of ethyl acetate and methanol. Dissolve 500mg of risperidone sample in the above oil phase, and mix evenly by ultrasonic. Weigh an appropriate amount of PVA in double-distilled water, dissolve it fully in a water bath at 50°C, adjust the concentration to 5% as the water phase, and add inorganic salts to the dispersion medium solution of the water phase. Inject the above oil phase into 150ml of PVA solution, stir at 1500rpm, dilute the concentration of PVA in the water phase to 1.5% after 5 minutes, and stir magnetically at room temperature for 3-5 hours to obtain the risperidone microsphere suspension. After washing, centrifuging and drying, add a small amount of methionine solution and freeze-dry.

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Abstract

The invention relates to a sustained-release microsphere of antipsychotic drug risperidone and the preparation method thereof.

Description

technical field [0001] The invention relates to slow-release microspheres of antipsychotic drug risperidone and a preparation method thereof. Background technique [0002] Risperidone is a selective monoamine antagonist with unique properties in that it has high affinity for 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. Risperidone is a potent D2 antagonist that can improve the positive symptoms of schizophrenia, but it causes less motor depression and catalepsy than classical antipsychotics. The balance of serotonin and dopamine antagonism on the central system can reduce the possibility of extrapyramidal side effects and extend its therapeutic effect to the negative symptoms and affective symptoms of schizophrenia. [0003] Risperidone is partially metabolized in the body into 9-hyd...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K9/50A61K31/517A61K47/34A61P25/18A61K47/32
Inventor 梅兴国王襄平
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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