Preparation method of olanzapine dihydroxynaphthoate sustained-release particle preparation spray

A technology of olanzapine pamoate and slow-release microparticles, which is applied in the direction of pharmaceutical formulas, medical preparations with no active ingredients, medical preparations containing active ingredients, etc., and can solve the problem of low incidence of extrapyramidal reactions, Application restrictions, toxic and side effects, etc., to achieve the effect of improving compliance, easy operation, and eliminating toxic and side effects

Inactive Publication Date: 2021-03-30
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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  • Preparation method of olanzapine dihydroxynaphthoate sustained-release particle preparation spray
  • Preparation method of olanzapine dihydroxynaphthoate sustained-release particle preparation spray

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] 1) Weigh 400 mg of PLGA 7525 7A, dissolve in 50 mL of dichloromethane, and dissolve with ultrasonic stirring;

[0019] 2) Weigh 600 mg of olanzapine pamoate powder, add it to the above solution, and ultrasonically stir to suspend, and set aside;

[0020] 3) The solution is spray-dried with a laboratory-scale BUCHI B-290 spray dryer with a 60 cm long drying column and a nozzle with a diameter of 0.7 mm. The conditions of the dryer are as follows: inlet temperature = 45 ° C, outlet temperature = 32 ℃, air flow = 50 cubic meters; collected after drying.

Embodiment 2

[0022] 1) Weigh 500 mg of PLGA 7525 7A, dissolve in 50 mL of dichloromethane, and dissolve with ultrasonic stirring;

[0023] 2) Weigh 500 mg of olanzapine pamoate powder, add it to the above solution, and ultrasonically stir to suspend, and set aside;

[0024] 3) The solution is spray-dried with a laboratory-scale BUCHI B-290 spray dryer with a 60 cm long drying column and a nozzle with a diameter of 0.7 mm. The conditions of the dryer are as follows: inlet temperature = 45 ° C, outlet temperature = 32 ℃, air flow = 50 cubic meters; collected after drying.

Embodiment 3

[0026] 1) Weigh 600 mg of PLGA 7525 7A, dissolve in 50 mL of dichloromethane, and dissolve with ultrasonic stirring;

[0027] 2) Weigh 400 mg of olanzapine pamoate powder, add it to the above solution, and ultrasonically stir to suspend, and set aside;

[0028] 3) The solution is spray-dried with a laboratory-scale BUCHI B-290 spray dryer with a 60 cm long drying column and a nozzle with a diameter of 0.7 mm. The conditions of the dryer are as follows: inlet temperature = 45 ° C, outlet temperature = 32 ℃, air flow = 50 cubic meters; collected after drying.

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Abstract

The invention relates to a preparation method of an olanzapine dihydroxy naphthoate sustained-release particle preparation spray, which comprises the following steps: dissolving 600 mg of PLGA 7525 7Ain 50 mL of dichloromethane, adding 400 mg of olanzapine dihydroxy naphthoate, and carrying out ultrasonic suspension; carrying out spray drying on the suspension by using a spray dryer, and collecting particles, wherein the spray dryer adopts a drying column with the length of 60 cm and a nozzle with the diameter of 0.7 mm; wherein the inlet temperature is 45 DEG C, the outlet temperature is 32DEG C, and the air flow is 50 cubic meters; the olanzapine dihydroxynaphthoate sustained-release particle preparation prepared by spraying has a particle size of 10-20 [mu]m and an encapsulation efficiency of 90% or more. The product provided by the invention reduces or eliminates the known toxic and side effects of current market products, can significantly inhibit early-stage burst release, prolong the slow release period and improve the compliance of patients with mental diseases, and the patients do not need to be observed under professional medical conditions after taking the medicine.

Description

technical field [0001] The invention relates to a spray preparation method of olanzapine pamoate sustained-release microparticle preparation, and belongs 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 pamo...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/551A61K47/34A61P25/18
CPCA61K31/551A61K9/1647A61P25/18
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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