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Sustained release microsphere containing risperidone and risperidone analogues and preparation method thereof

A technology of sustained-release microspheres and microspheres, which can be used in medical preparations containing active ingredients, medical preparations without active ingredients, and drug combinations, etc. Increased drug release and reduced porosity

Inactive Publication Date: 2013-06-05
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

[0009] The object of the present invention is to provide a long-acting injection microsphere of risperidone and its analogs and its preparation method, so as to overcome the problems of sudden release and release delay in the prior art, and improve the drug compliance of patients

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Example 1: Preparation of 9-hydroxyrisperidone sustained-release microspheres

[0033]28% of the total weight of the microspheres was 9-hydroxyrisperidone (commercially available), 70% of the total weight of the microspheres was PLGA (75:25 ratio of lactic acid and glycolic acid, molecular weight (MW) 100,000), Dibutyl phthalate containing 0.5% of the total weight of the microspheres was dissolved in a mixed solution of dichloromethane and methanol (the volume ratio of dichloromethane and methanol was 8:2), and the solution was added to a mechanically stirred solution at 2500 rpm. In 500 ml of 4% polyvinyl alcohol (PVA) aqueous solution, after 5 minutes, dilute the PVA solution by 1 times, continue stirring for more than 4 hours, then wash, centrifuge and dry to obtain microspheres with an average particle size of 80 μm.

Embodiment 2

[0034] Example 2: Preparation of 9-hydroxyrisperidone sustained-release microspheres

[0035] 28% of the total weight of the microspheres was 9-hydroxyrisperidone (commercially available), 70% of the total weight of the microspheres was PLGA (75:25 ratio of lactic acid and glycolic acid, molecular weight (MW) 100,000), The dibutyl phthalate of 1.9% of the total weight of the microspheres and the tert-butyl-p-hydroxyanisole of 0.1% of the total weight of the microspheres are dissolved in the mixed solution of dichloromethane and methanol (the volume ratio of dichloromethane and methanol is 8:2), add this solution to 500 ml of 3% polyvinyl alcohol (PVA) aqueous solution mechanically stirred at 2500 rpm, dilute the PVA solution 1 times after 5 minutes, continue stirring for more than 4 hours, then wash, centrifuge, and dry. Then take an appropriate amount of the above-mentioned microspheres, put them in a dichloromethane solution containing 300mg / ml PLGA, leave them for 30s, take...

Embodiment 3

[0036] Example 3: Preparation of risperidone sustained-release microspheres

[0037] 38% of the total weight of the microspheres was risperidone (commercially available), 60% of the total weight of the microspheres was PLGA (75:25 ratio of lactic acid and glycolic acid, molecular weight (MW) 150,000), and 60% of the total weight of the microspheres. 1% by weight of dibutyl phthalate and 1% of tert-butyl-p-hydroxyanisole in the total weight of the microspheres are dissolved in a mixed solution of dichloromethane and methanol (the volume ratio of dichloromethane and methanol is 8:2 ), add this solution to 500ml of 3% polyvinyl alcohol (PVA) aqueous solution mechanically stirred at 2500rpm, dilute the PVA solution 1 times with water after 5 minutes, continue stirring for more than 4 hours, then wash, centrifuge, and dry.

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Abstract

The invention provides a sustained release microsphere containing risperidone and risperidone analogues and a preparation method thereof, wherein the sustained release microsphere containing the risperidone and the risperidone analogues can be used for injections. The sustained release microsphere comprises an active substance risperidone, the risperidone analogues, biodegradable medicinal high polymer materials, plasticizers, antioxygen and the like. The preparation method of the sustained release microsphere containing the risperidone and the risperidone analogues can be an emulsion process, a spray drying process, a low-temperature spray extraction method, a supercritical fluid method and the like. A blank medicinal high polymer material layer can also be wrapped on the surface of the microsphere on the basis. The microsphere preparation solves the problems, of dumping, lag phase and the like, existing in a reported or a listed product. The composition is mainly used in treating acute and chronic mental diseases.

Description

technical field [0001] The invention relates to a sustained-release microsphere for injection, in particular to a biodegradable sustained-release microsphere of risperidone and its analogs and a preparation method. Background technique [0002] With the development of human society and economy and the improvement of people's living standards, mental and mental health problems are becoming more and more serious. Medical experts believe that human beings have entered the "mental disease era" from the "epidemic disease era" and the "physical disease era". Among them, schizophrenia is the most common and most difficult to describe severe mental illness, with a long course of disease, easy recurrence, and great harm. Conventional antipsychotics have side effects such as extrapyramidal reactions and tardive dyskinesia, so it has been argued that the efficacy of traditional antipsychotics is offset by their limitations. At present, a new generation of atypical antipsychotics has e...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/519A61K47/34A61K47/36A61P25/18
Inventor 梅兴国李志平刘燕
Owner INST OF PHARMACOLOGY & TOXICOLOGY ACAD OF MILITARY MEDICAL SCI P L A
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