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Sustained release system of clozapine solid liposome microparticle

A solid lipid, clozapine technology, applied in the directions of liposome delivery, nervous system diseases, medical preparations with inactive ingredients, etc. Speed, simple operation effect

Inactive Publication Date: 2007-05-30
SOUTH CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is mentioned in the patent specification that the tablet has certain sustained-release properties, but the release effect is not obvious

Method used

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  • Sustained release system of clozapine solid liposome microparticle
  • Sustained release system of clozapine solid liposome microparticle

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038]Under 85 ℃, the stearin of 5% (W / W, take emulsion as a benchmark, the same below) and 0.5% clozapine are mixed in dehydrated alcohol solvent, evaporate and recover solvent then; Disperse in an aqueous solution containing 2% lecithin / ox bile salt stabilizer at the same temperature under stirring; then process it with a high-shear dispersing emulsifier at 8000 rpm for about 15 minutes to form a highly dispersed O / W emulsion ; Finally, the emulsion is placed in a cold water bath at 5° C., and the fat phase is cooled and crystallized under mild magnetic stirring to obtain a suspension of clozapine solid lipid fine particles with an average particle size of 8 μm. Freeze-dry at a temperature of -50° C. and a pressure of 5.0 Pa for 24 hours to obtain dry microparticles.

Embodiment 2

[0040] 5% stearin and 0.5% clozapine were mixed in anhydrous ethanol solvent at 85°C, and then evaporated to recover the solvent; the molten mixture was dispersed at the same temperature containing 2% PVA (MW= 13000-23000) in the aqueous solution of the stabilizer; then treat it with a high-shear dispersing emulsifier at 10,000 rpm for about 15 minutes to form a highly dispersed O / W emulsion; finally place the emulsion in a cold water bath at 5°C, The lipid phase is cooled and crystallized under mild magnetic stirring to obtain a suspension of solid lipid microparticles with an average particle diameter of 5 μm encapsulating clozapine. Freeze-drying for 24 hours at a temperature of -50° C. and a pressure of 5.0 Pa to obtain dry microparticles.

Embodiment 3

[0042] 5% mixed esters (17% monoglyceride stearate, 54% diglyceride stearate, 29% triglyceride stearate) and 0.5% clozapine in absolute ethanol solvent at 85°C Mix and melt, then completely evaporate and reclaim the solvent; disperse the molten mixture in an aqueous solution containing 2% PVA (MW=13000-23000) stabilizer at the same temperature under magnetic stirring; then use 8000 rpm high shear Cut the dispersing emulsifier for about 15 minutes to form a highly dispersed O / W emulsion; finally place the emulsion in a cold water bath at 5°C, and cool and crystallize the lipid phase under gentle magnetic stirring to obtain the average particle size A suspension of clozapine solid lipid fine particles of 5 μm. Freeze-dry at a temperature of -50° C. and a pressure of 5.0 Pa for 24 hours to obtain dry microparticles.

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Abstract

The invention discloses a clozapine solid liposome microparticle control slow-release system, which is characterized by the following: adopting high-fusing point and biological compatible solid liposome as carrier material such as fatty acid ester, fatty acid, fatty alcohol or their two composition; making surface activator or macromolecule as stabilizer such as lecithin, poloxamer series, polysorbate series, cholate and so on.

Description

technical field [0001] The invention relates to a drug controlled release system for treating schizophrenia, in particular to a clozapine solid lipid microparticle controlled release system. Background technique [0002] Clozapine is an atypical antipsychotic drug, which is one of the commonly used drugs for the treatment of schizophrenia in China. It has a good clinical effect on both positive and negative symptoms of schizophrenia. [0003] Clozapine is a light yellow crystalline powder. Although clozapine hardly produces extrapyramidal side effects at a lower daily dose, because clozapine is very soluble in acidic solution, its common tablet can be taken orally After being quickly absorbed in the stomach, its bioavailability is low. While clozapine is almost insoluble in water (neutral environment), its release in the intestine is very little. Therefore, in order to ensure an effective blood drug concentration when using clozapine ordinary tablet treatment, it must be a...

Claims

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Application Information

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IPC IPC(8): A61K31/551A61K9/127A61K9/16A61K47/14A61K47/24A61K47/34A61P25/18A61K47/10A61K47/26
CPCA61K31/5513
Inventor 章莉娟钱宇刘磊李秀喜
Owner SOUTH CHINA UNIV OF TECH
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