Olanzapine-pamoate sustained-release microparticle preparation and preparation method therefor

A technology for olanzapine pamoate and sustained-release microparticles, which is applied in the field of olanzapine pamoate sustained-release microparticle preparations and its preparation, and can solve the problems of low incidence of extrapyramidal reactions, application restrictions, and toxicity. side effects and other issues, to achieve the effect of improving compliance, easy operation, and eliminating side effects

Inactive Publication Date: 2021-04-02
长春斯菲尔生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since it went on the market, it has been sold well. It has a good effect on the positive and negative symptoms of schizophrenia and has a low incidence of extrapyramidal reactions (EPS). side effect
Due to the large burst release of ZYPREXA RELPREVV in the early stage, individual patients may experience side effects such as sedation (including coma) and / or delirium after medication, and need to be observed for 3 hours under professional medical conditions, so the application of ZYPREXARELPREVV is greatly limited

Method used

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  • Olanzapine-pamoate sustained-release microparticle preparation and preparation method therefor
  • Olanzapine-pamoate sustained-release microparticle preparation and preparation method therefor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] 1) Weigh 50 mg of PLGA 7525 7A, dissolve in 5 mL of dichloromethane, and dissolve with ultrasonic stirring;

[0017] 2) Weigh 150 mg of olanzapine pamoate powder, add it to the above solution, stir and suspend with ultrasonic, and set aside;

[0018] 3) Measure 20 mL of paraffin in a 100 mL beaker, set the homogenizer to 10000 rpm, and mix the above suspension with

[0019] Inject the 20 mL syringe into the beaker within 30 s and homogenize for 3 min;

[0020] 4) Magnetically stirred for 4 h, dichloromethane was volatilized, collected by suction filtration, washed three times with 120 mL of n-hexane, and obtained.

Embodiment 2

[0022] 1) Weigh 75 mg of PLGA 7525 7A, dissolve in 5 mL of dichloromethane, and dissolve with ultrasonic stirring;

[0023] 2) Weigh 150 mg of olanzapine pamoate powder, add it to the above solution, stir and suspend with ultrasonic, and set aside;

[0024] 3) Measure 20 mL of paraffin into a 100 mL beaker, set the homogenizer at 10000 rpm, inject the above suspension into the beaker with a 20 mL syringe within 30 s, and homogenize for 3 min;

[0025] 4) Magnetically stirred for 4 h, dichloromethane was volatilized, collected by suction filtration, washed three times with 120 mL of n-hexane, and obtained.

Embodiment 3

[0027] Olanzapine pamoate PLA sustained-release microparticles prepared by emulsification solvent evaporation method:

[0028] 1) Weigh 100 mg of PLGA 7525 7A, dissolve in 5 mL of dichloromethane, and dissolve with ultrasonic stirring;

[0029] 2) Weigh 150 mg of olanzapine pamoate powder, add it to the above solution, stir and suspend with ultrasonic, and set aside;

[0030] 3) Measure 20 mL of paraffin into a 100 mL beaker, set the homogenizer at 10000 rpm, inject the above suspension into the beaker with a 20 mL syringe within 30 s, and homogenize for 3 min;

[0031] 4) Magnetically stirred for 4 h, dichloromethane was volatilized, collected by suction filtration, washed three times with 120 mL of n-hexane, and obtained.

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Abstract

The invention provides an olanzapine-pamoate sustained-release microparticle preparation and a preparation method therefor. Sustained-release microparticles are prepared through encapsulating antischizophrenic drugs with high polymers, and the olanzapine-pamoate sustained-release microparticle preparation has the entrapment rate of 85%-95% and the particle size of 15 to 35 microns. According to the product provided by the invention, known toxic or side effects of the product are lowered or eliminated, sudden release of primary stage can be remarkably inhibited, the sustained-release cycle is prolonged, and the actions of lowering sudden release and prolonging sustained release can be obviously exerted. The compliance of mental illness sufferers is improved, and patients are not required tobe observed under professional medical conditions after medication.

Description

technical field [0001] The invention relates to an olanzapine pamoate sustained-release microparticle preparation and a preparation method thereof, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Schizophrenia is a psychotic disorder whose symptoms include positive and negative symptoms. Positive symptoms mainly include delusions, visual hallucinations, auditory hallucinations, and abnormal thinking, while negative symptoms mainly include apathy, aphasia, and decreased will and behavior. [0003] The anti-schizophrenia drug-olanzapine pamoate that the present invention relates to is a kind of atypical anti-schizophrenia drug. Through its lower solubility and unique slow-release effect, the administration cycle is every 2 Once a week or once every 4 weeks greatly reduces the frequency of administration and improves patient compliance. In 2009, Lilly launched ZYPREXA RELPREVV, a long-acting intramuscular injection of olanzapine ...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K47/34A61K31/551A61P25/18
CPCA61K9/5031A61K31/551A61P25/18
Inventor 李又欣李翔宇余昌会孙凤英滕乐生孟祥雪侯雨菲崔雅欣
Owner 长春斯菲尔生物科技有限公司
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