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Sustained-release microspheres containing risperidone and its analogs and preparation method thereof

A technology of slow-release microspheres and microspheres, which is applied to medical preparations containing active ingredients, medical preparations with non-active ingredients, drug combinations, etc., can solve problems such as burst release and release delay, and achieve improved release behavior, Effect of reducing porosity and increasing drug release

Inactive Publication Date: 2016-08-03
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 microspheres containing risperidone and its analogs and preparation method thereof
  • Sustained-release microspheres containing risperidone and its analogs and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

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

[0033]9-Hydroxyrisperidone (commercially available) accounting for 28% of the total weight of the microspheres, PLGA (the ratio of lactic acid and glycolic acid is 75:25, and the molecular weight (MW) is 100,000), accounting for 70% of the total weight of the microspheres, Dibutyl phthalate of 0.5% of the total weight of the microspheres is dissolved in a mixed solution of methylene chloride and methanol (the volume ratio of methylene chloride and methanol is 8:2), and this solution is added to a mechanically stirred at 2500rpm In 500ml of 4% polyvinyl alcohol (PVA) aqueous solution, the PVA solution was diluted 1 time after 5 minutes, continued to stir for more than 4 hours, then washed, centrifuged, and dried to obtain microspheres with an average particle diameter of 80 μm.

Embodiment 2

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

[0035] 9-Hydroxyrisperidone (commercially available) accounting for 28% of the total weight of the microspheres, PLGA (the ratio of lactic acid and glycolic acid is 75:25, and the molecular weight (MW) is 100,000), accounting for 70% of the total weight of the microspheres, Dibutyl phthalate of 1.9% of the total weight of the microspheres and 0.1% of tert-butyl p-hydroxyanisole of the total weight of the microspheres are dissolved in a mixed solution of methylene chloride and methanol (the volume ratio of methylene chloride and methanol is 8:2), this solution was added in 500ml of 3% polyvinyl alcohol (PVA) aqueous solution with 2500rpm mechanical stirring, after 5 minutes the PVA solution was diluted 1 time, continued to stir more than 4 hours, then washed, centrifuged, dried. Then take an appropriate amount of the above-mentioned microspheres, place them in a dichloromethane solution conta...

Embodiment 3

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

[0037] Risperidone (commercially available) accounting for 38% of the total weight of the microspheres, PLGA (the ratio of lactic acid and glycolic acid is 75:25, molecular weight (MW) is 150,000) accounting for 60% of the total weight of the microspheres, accounting for the total weight of the microspheres Dibutyl phthalate of 1% by weight and tert-butyl p-hydroxyanisole accounting for 1% of the total weight of the microspheres were dissolved in a mixed solution of methylene chloride and methanol (the volume ratio of methylene chloride and methanol was 8:2 ), this solution was added in 500ml of 3% polyvinyl alcohol (PVA) aqueous solution with 2500rpm mechanical stirring, after 5 minutes the PVA solution was diluted 1 time with water, continued to stir for more than 4 hours, then washed, centrifuged, dried to obtain final product.

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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 era" and "the era of physical diseases". Among them, schizophrenia is the most common and most difficult to describe severe mental illness, with a long course of disease, easy relapse, and great harm. Traditional 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 antipsychotic drugs has emer...

Claims

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Application Information

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Patent Type & Authority Patents(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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