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Risperidone sustained release microsphere composition

A composition and technology of risperidone, which are applied in the field of risperidone long-acting sustained-release microsphere composition and its preparation field, can solve the problems of changes in the release behavior of the microspheres, poor formulation stability and the like, so that the release behavior will not change. Effect

Active Publication Date: 2013-10-02
SHANDONG LUYE PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the patent application of CN101653422 only verified that the laboratory level (5L scale) can achieve the intended purpose
The applicant of the present invention has found that the risperidone microspheres provided in CN101653422 have drug crystallization during the scaled-up production process, and the preparation stability is poor. After long-term storage, the release behavior of the microspheres in vivo will obviously occur. Variety

Method used

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  • Risperidone sustained release microsphere composition
  • Risperidone sustained release microsphere composition
  • Risperidone sustained release microsphere composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Weigh 72g of PLGA with a molecular weight of 74,000 (75 / 25, 0.52A), 18g of PLGA with a molecular weight of 25,000 (50 / 50, 0.25A) and 110g of risperidone, stir and dissolve in 1000ml of dichloromethane to prepare Clear solution. This clear solution was added via a peristaltic pump to a microsphere preparation kettle containing 100 L of PVA solution (0.5%) cooled to 6 °C. The stirrer and homogenizer were turned on, and the clear solution was homogeneously emulsified at 380 rpm for 1 min. Afterwards, the rotation speed of the homogenizer is reduced, and the organic solvent is volatilized and removed for 3 to 5 hours. The residue was filtered through a mesh, washed with deionized water, and lyophilized to obtain the microspheres as a powder. No crystals were precipitated. The drug loading capacity of the microspheres was 45.9%, and the encapsulation efficiency was 83.5%.

Embodiment 2

[0052] Weigh 67.5g of PLGA with a molecular weight of 55,000 (75 / 25, 0.42A), 7.5g of PLGA with a molecular weight of 25,000 (50 / 50, 0.25A), and 75g of risperidone, stir and dissolve in 750ml of dichloromethane, A clear solution was prepared. This clear solution was added via a peristaltic pump to a microsphere preparation kettle containing 75 L of PVA solution (0.5%) cooled to 6 °C. The stirrer and homogenizer were turned on, and the clear solution was homogeneously emulsified at 380 rpm for 1 min. Afterwards, the rotation speed of the homogenizer is reduced, and the organic solvent is volatilized and removed for 3 to 5 hours. The residue was filtered through a mesh, washed with deionized water, and lyophilized to obtain powdered microspheres. No crystals were precipitated. The drug loading capacity of the microspheres was 40.2%, and the encapsulation efficiency was 80.4%.

Embodiment 3

[0054] Weigh 56g of PLGA with a molecular weight of 125,000 (75 / 25, 0.90A), 24g of PLGA with a molecular weight of 25,000 (50 / 50, 0.25A), and 120g of risperidone, stir and dissolve them in 1000ml of dichloromethane to prepare Clear solution. This clear solution was added via a peristaltic pump to a microsphere preparation kettle containing 100 L of PVA solution (0.5%) cooled to 6 °C. The stirrer and homogenizer were turned on, and the clear solution was homogeneously emulsified at 380 rpm for 1 min. Afterwards, the rotation speed of the homogenizer is reduced, and the organic solvent is volatilized and removed for 3-5 hours; the residue is filtered with a sieve, washed with deionized water, and freeze-dried to obtain powdered microspheres. No crystals were precipitated. The drug loading capacity of the microspheres was 51.5%, and the encapsulation efficiency was 85.8%.

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Abstract

A risperidone sustained release microsphere formulation is provided. The microsphere formulation comprise risperidone or 9-hydroxy risperidone or salts thereof, and a polymer blend having a first uncapped lactide-glycolide copolymer and a second uncapped lactide-glycolide copolymer, in which the first uncapped lactide-glycolide copolymer is a copolymer with a high intrinsic viscosity and the second uncapped lactide-glycolide copolymer is a copolymer with a low intrinsic viscosity. The sustained release microsphere formulation according to an embodiment of the present disclosure is suitable for large-scale industrialized production with improved stability, tthe in vivo release behavior of which will not change after long-term storage.

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] Schizophrenia is a serious, disabling mental illness. As social competition intensifies, the pace of life accelerates, and family structures change, people are under increasing pressure, resulting in increasingly prominent mental health problems. Schizophrenia is the most common mental illness. According to statistics, the prevalence rate of schizophrenia in China is 6.55‰, that is, more than 7.8 million patients with schizophrenia, and the global incidence rate is as high as 1.5%. [0003] Antipsychotic drugs, also known as neuroleptics, are effective in controlling the psychotic symptoms of schizophrenia. Common antipsychotic drugs first discovered in the 1950s, such as chlorpromazine or haloperidol, whose main pharmaco...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/519A61K47/34A61P25/18
CPCA61K47/34A61K31/519A61K9/0019A61K9/1647A61K9/14A61K9/19A61K9/16A61P25/18A61K9/4858A61K9/5031A61K9/5089
Inventor 孙考祥梁荣才王麒麟王文艳刘万卉李又欣
Owner SHANDONG LUYE PHARMA CO LTD
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