Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Iloperidone slow releasing microsphere and preparation method thereof

A technology of sustained-release microsphere preparation and iloperidone, which can be used in nervous system diseases, bulk delivery, drug combination, etc., can solve the problems of narrow therapeutic window, tardive dyskinesia, etc. The particles are regular without sticking, and the in vitro release curve is smooth and flat

Inactive Publication Date: 2015-02-18
HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
View PDF3 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, these drugs have a relatively narrow therapeutic window, and excessive or long-term use can cause extrapyramidal side effects (EPS), such as dystonia (muscle spasms that can distort the face), inability to sit or stand, Parkinson's disease-like symptoms, Tardive dyskinesia and potentially fatal neuroleptic malignancy

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Iloperidone slow releasing microsphere and preparation method thereof
  • Iloperidone slow releasing microsphere and preparation method thereof
  • Iloperidone slow releasing microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Weigh 15mg of iloperidone, 300mg of PLGA (75 / 15, 0.48) with a molecular weight of 58,000 and add it into 4mL of dichloromethane to stir and dissolve the clear solution. Slowly add this solution dropwise to 20mL of PVA solution, and disperse and emulsify at 1000rpm for 1min. Then reduce the rotational speed, volatilize the organic solvent therein, and volatilize for 5 hours; centrifuge, wash the ball 4 times to obtain iloperidone sustained-release microspheres.

Embodiment 2

[0023] Weigh 15mg of iloperidone, 450mg of PLGA (75 / 15, 0.48) with a molecular weight of 58,000 and add it into 4mL of dichloromethane to stir and dissolve the clear solution. Slowly add this solution dropwise to 20mL of PVA solution, and disperse and emulsify at 1000rpm for 1min. Then reduce the rotational speed, volatilize the organic solvent therein, and volatilize for 5 hours; centrifuge, wash the ball 4 times to obtain iloperidone sustained-release microspheres.

Embodiment 3

[0025] Weigh 15mg of iloperidone and 225mg of PLGA (75 / 15, 0.48) molecular weight 58,000, add it into 4mL of dichloromethane and stir to dissolve the clear solution, slowly add this solution dropwise into 20mL of PVA solution, disperse and emulsify at 1000rpm for 1min, then Reduce the rotating speed to volatilize the organic solvent therein for a total of 5 hours; centrifuge and wash the balls 4 times to obtain the iloperidone sustained-release microspheres.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Intrinsic viscosityaaaaaaaaaa
Login to View More

Abstract

The invention provides an iloperidone slow releasing microsphere and a preparation method thereof. The microsphere contains an iloperidone and lactide-glycolide copolymer. The iloperidone slow releasing microsphere provided by the invention has the benefits that the drug loading capacity is higher, the slow releasing period is above 5 weeks, and an in vitro release curve is smooth and flat.

Description

technical field [0001] The invention relates to a psychotropic drug iloperidone (iloperidone) slow-release microsphere and a preparation method thereof. Background technique [0002] The pathogenesis of schizophrenia is due to the excessive secretion of dopamine (DA) in the brain or the sensitivity of dopamine receptors in the body, so anti-schizophrenia drugs mainly act on dopamine receptors. Atypical antipsychotic drugs are the main research objects of antipsychotic drugs now, and these drugs have no effect on dopamine D 2 Receptor affinity is relatively low, but for 5-HT and α 1 , α 2 High affinity for adrenergic receptors. [0003] Classic antipsychotics, such as haloperidol, block mesolimbic dopamine D 2 receptors to exert therapeutic effect. However, these drugs have a relatively narrow therapeutic window, and excessive or long-term use can cause extrapyramidal side effects (EPS), such as dystonia (muscle spasms that can distort the face), inability to sit or stan...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/16A61K31/454A61K47/34A61P25/18
Inventor 高子彬谷艳玲张丽男陈小龙齐献利张晓博孙勇军吴韶梅谢英花刘磊
Owner HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com