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A method for preparing sustained-release microspheres containing risperidone

A technology of slow-release microspheres and risperidone, which is applied in the direction of microcapsules, pharmaceutical formulas, and medical preparations of non-active ingredients, which can solve the problems of frequency, impact on the lives of patients and family members, and reduce the frequency of dosing and avoid Effect of low toxicity and no solvent residue

Active Publication Date: 2021-04-27
LIVZON PHARM GRP INC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, bi-weekly injections are still too frequent and have a certain impact on the lives of patients and their families

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0023] Weigh 2 g of PLA polymers with a molecular weight of 100,000 and 3.0 g of risperidone.

[0024] The risperidone was pulverized by a ball mill at 30° C. for 10 minutes, and then sieved to collect particles below 800 mesh to obtain risperidone powder.

[0025] The PLA was pulverized by a ball mill at -10°C for 10 minutes, and then sieved to collect particles below 100 mesh to obtain PLA powder. Then heat it slowly to melt it, keeping the temperature at 65°C.

[0026] Add risperidone powder to the molten PLA, keep the temperature at 65° C., and stir for 30 minutes to obtain a molten mixture. Then put the above mixture into a Pharmll type twin-screw extruder (available from Thermo Fisher Scientific Company), adjust the melt extrusion temperature of the four-section temperature control zone of the extruder to about 60 ° C, and heat and compress the mixture to melt and extrude , the whole process time from feeding to extrusion is 30 minutes, and the obtained melted extrudat...

Embodiment 2

[0028] Weigh 2 g of PLA polymers with a molecular weight of 150,000 and 3.0 g of risperidone.

[0029] The risperidone was pulverized by a ball mill at 30° C. for 10 minutes, and then sieved to collect particles below 800 mesh to obtain risperidone powder.

[0030] The PLA was pulverized by a ball mill at -10°C for 10 minutes, and then sieved to collect particles below 100 mesh to obtain PLA powder. Then heat it slowly to melt it, keeping the temperature at 65°C.

[0031] Add risperidone powder to the molten PLA, keep the temperature at 65° C., and stir for 30 minutes to obtain a molten mixture. Then put the above mixture into a Pharmll type twin-screw extruder (available from Thermo Fisher Scientific Company), adjust the melt extrusion temperature of the four-section temperature control zone of the extruder to about 60 ° C, and heat and compress the mixture to melt and extrude , the whole process time from feeding to extrusion is 30 minutes, and the obtained molten extrudat...

Embodiment 3

[0032] Embodiment 3 The impact of polymers of different types and molecular weights on experimental results

[0033] Weigh 2 g of polymers of different types and molecular weights, and 3.0 g of risperidone.

[0034] The risperidone was pulverized by a ball mill at 30° C. for 10 minutes, and then sieved to collect particles below 800 mesh to obtain risperidone powder.

[0035] The polymer was pulverized by a ball mill at -10°C for 10 minutes, and then sieved to collect particles below 100 mesh to obtain polymer powder. Then heat it slowly to melt it, keeping the temperature at 65°C.

[0036] Add risperidone powder to the molten polymer, keep the temperature at 65° C., and stir for 30 minutes to obtain a molten mixture. Then put the above mixture into a Pharmll type twin-screw extruder (purchased from Thermo Fisher Scientific Company), adjust the melt extrusion temperature of the four-section temperature control zone of the extruder to about 60 ° C, and heat and compress the m...

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PUM

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Abstract

The invention provides a method for preparing risperidone sustained-release microspheres, comprising the following steps: (1) weighing a certain amount of PLA, controlling the melting temperature A, and heating to obtain molten PLA; (2) weighing a certain amount The risperidone powder is mixed with PLA in a molten state to obtain a risperidone PLA mixture; (3) controlling the melt extrusion temperature B to melt-extrude the risperidone PLA mixture to obtain a hot-melt extrudate; (4) Control the pulverization temperature C, cool and pulverize the hot-melt extrudate, and sieve to obtain sustained-release microspheres containing risperidone; wash, centrifuge, and freeze-dry to obtain finished microspheres.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a risperidone long-acting sustained-release microsphere composition and a preparation method and application thereof. Background technique [0002] Risperidone is a new generation of antipsychotics. It has high affinity with 5-HT2 receptor and dopamine D2 receptor. This product can also bind to α1 receptors, has low affinity to H1 receptors and α2 receptors, and does not bind to cholinergic receptors. This product is a powerful D2 receptor antagonist that can improve the positive symptoms of schizophrenia; but it causes less motor function inhibition and catalepsy than classic antipsychotics. The balance of 5-HT 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] The oral preparations of risperidone currently...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/52A61K47/34A61K31/519A61P25/18
CPCA61K9/0019A61K9/5031A61K31/519A61P25/18
Inventor 陈剑马思萌陈斌江晓漫
Owner LIVZON PHARM GRP INC
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