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Risperidone-loaded PLGA microsphere mixture and preparation method thereof

A technology containing risperidone and PLGA, applied in the cross-research field of bioactive drug controlled release preparations and biomedical polymer materials, can solve the problems of difficult to achieve long-term effective treatment effect, easy to appear burst release phenomenon, etc. Good, round shape, convenient medication effect

Inactive Publication Date: 2019-08-16
山东墨海生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The most commonly used solvent evaporation method, the microspheres prepared by this method are easy to release, prone to burst release phenomenon, and it is difficult to achieve long-term effective therapeutic effect

Method used

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  • Risperidone-loaded PLGA microsphere mixture and preparation method thereof
  • Risperidone-loaded PLGA microsphere mixture and preparation method thereof
  • Risperidone-loaded PLGA microsphere mixture and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Example 1: A mixture of risperidone-loaded PLGA microspheres is obtained by mixing risperidone-loaded PLGA composite microspheres with risperidone-loaded PLGA general microspheres in different proportions. In the PLGA composite microspheres loaded with risperidone drug and the PLGA general microspheres loaded with risperidone, PLGA is composed of lactide-glycolide copolymers with different molecular weights in proportion; among them, lactide-glycolide The molecular weight of the copolymer is 5,000; the ratio of lactide to glycolide is 75 / 25; the capping of the lactide-glycolide copolymer is ester capping.

Embodiment 2

[0054] Example 2: A mixture of risperidone-loaded PLGA microspheres is obtained by mixing risperidone-loaded PLGA composite microspheres with risperidone-loaded PLGA general microspheres in different proportions. In the PLGA composite microspheres loaded with risperidone drug and the PLGA general microspheres loaded with risperidone, PLGA is composed of lactide-glycolide copolymers with different molecular weights in proportion; among them, lactide-glycolide The molecular weight of the copolymer is 52,000, and the ratio of lactide to glycolide is 50 / 50; the capping of the lactide-glycolide copolymer is terminal hydroxyl group.

Embodiment 3

[0055] Example 3: A mixture of risperidone-loaded PLGA microspheres is obtained by mixing risperidone-loaded PLGA composite microspheres with risperidone-loaded PLGA general microspheres in different proportions. In the PLGA composite microspheres loaded with risperidone drug and the PLGA general microspheres loaded with risperidone, PLGA is composed of lactide-glycolide copolymers with different molecular weights in proportion; among them, lactide-glycolide The molecular weight of the copolymer is 159,000; the ratio of lactide to glycolide is 75 / 25; the capping of the lactide-glycolide copolymer is a carboxyl group.

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Abstract

The invention discloses a risperidone-loaded PLGA microsphere mixture and a preparation method thereof. With adopting of an improved double-emulsion-solvent evaporation method, that is, on the basis of the double-emulsion method, an inner core is a sustained-release gel formed by chelation of sodium alginate and calcium ions, PLGA is used as a microsphere carrier, risperidone is a wrapping object,and the drug-loaded microspheres are prepared. The shape is round, the particle size distribution is uniform, the average particle size distribution is about 30 microns, the drug loading amount is 30% or more, the encapsulation efficiency is about 50%, and the drug release in vitro conforms to the characteristics of long-acting preparations.

Description

technical field [0001] The invention relates to a polylactic-co-glycolic acid (PLGA) microsphere mixture loaded with risperidone and a preparation method thereof, belonging to the field of interdisciplinary research of bioactive drug controlled release preparations and biomedical polymer materials. Background technique [0002] Schizophrenia is one of the most common disorders of emotional thinking today. It affects the cognitive ability of patients and gradually endangers people's daily emotions and behaviors. Schizophrenia can be divided into positive and negative symptoms, which is determined by the difference in the type of symptoms and the severity of symptom responses. Among them, the positive symptoms are generally manifested as chaotic and loose thinking, prone to delusions or even hallucinations, and behavioral disorder and mania; negative symptoms are psychological depression, severe degradation of the ability to recognize and respond to the outside world, and loss...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/58A61K31/519A61P25/18
CPCA61K31/519A61K9/5084A61K9/5031
Inventor 聂宇邹孟玮钱林艺
Owner 山东墨海生物科技有限公司
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