Long-acting non-water-carrier injection liquid and preparing method thereof

An injection and carrier technology, applied in the chemical field, can solve the problems of expensive equipment, difficult aseptic control, and larger particle size of aqueous nano-suspension, achieving less toxic and side effects, high sterility assurance factor, and improved physical stability sexual effect

Inactive Publication Date: 2015-11-04
SHENZHEN FONCOO PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Aqueous nano-suspensions have problems such as slowly increasing particle size, difficulty in aseptic control, and expensive equipment
[0012] Aripiprazole lauroyl and paliperidone palmitate are insoluble in water. To make an aqueous carrier nanosuspension, injection-grade carboxymethylcellulose is required. There is no related product in China at present.

Method used

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  • Long-acting non-water-carrier injection liquid and preparing method thereof
  • Long-acting non-water-carrier injection liquid and preparing method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Embodiment 1 prepares lauroyl aripiprazole soybean oil injection

[0043] Specification: 295mg / ml

[0044] prescription:

[0045] name

purpose

Amount added

Aripiprazole Lauroyl

Main drug

380g

Soybean Oil for Injection

injection oil

1000g

Lecithin for Injection

Emulsifier

120g

Glycerin for Injection

osmotic regulator

210g

[0046]Technological process: Aripiprazole lauroyl is pulverized to a D90 of less than 50 microns with a jet mill (TC-30 superfine pulverization classifier, Beijing Sinopharm Longli Technology Co., Ltd.). Then take lauroyl aripiprazole 380g, soybean oil for injection 1000g, lecithin for injection 120g, glycerin for injection 210g, carry out primary dispersion with solid / liquid dispersion mixing system (PJ90 type, Shanghai Fluke Technology Development Co., Ltd.) , and then the sample was added to a high-pressure jet homogenizer (Nilu Solvay, Italy), and the inlet tempe...

Embodiment 2

[0048] Embodiment 2 prepares paliperidone palmitate soybean oil injection

[0049] Specification: 156mg / ml

[0050] prescription:

[0051] name

purpose

Amount added

Paliperidone Palmitate

Main drug

203g

Soybean Oil for Injection

injection oil

1000g

Lecithin for Injection

Emulsifier

120g

Glycerin for Injection

osmotic regulator

210g

[0052] Technological process: pulverize paliperidone palmitate until the D90 is below 50 microns with a jet mill (TC-30 ultrafine pulverizer classifier, Beijing Sinopharm Longli Technology Co., Ltd.). Then get paliperidone palmitate 203g, soybean oil for injection 1000g, lecithin for injection 120g, glycerol 210g for injection, carry out primary with solid / liquid dispersion mixing system (PJ90 type, Shanghai Fluke Technology Development Co., Ltd.) Disperse, then join the sample in the high-pressure jet homogenizer (Italy Nilu Solvay Company), keep the inlet tempe...

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Abstract

The invention discloses long-acting non-water-carrier injection liquid and a preparing method thereof. The long-acting non-water-carrier injection liquid comprises mental drugs and non-water carriers and can be continuously released within at least four weeks. The mental drugs are lauroyl aripiprazole or paliperidone palmitate. The preparing method is completed through high-pressure homogeneous steps. The preparation of the long-acting non-water-carrier injection liquid can be released slowly within at least four weeks. The continuously-releasing injection preparation is more stable, simple in preparation form, free of freeze drying, simple in preparation, good in economical effect and convenient to use.

Description

technical field [0001] The invention relates to chemistry, in particular to a long-acting non-aqueous carrier injection and a preparation method thereof. Background technique [0002] Since mental illnesses such as schizophrenia require long-term medication, patient compliance is poor, and long-acting injections for two weeks or longer have shown great advantages in the treatment of such diseases. [0003] The long-acting preparations currently on the market include the suspension freeze-dried preparation of aripiprazole from Japan's Otsuka Pharmaceutical Co., Ltd., and the paliperidone palmitate sustained-release long-acting injection of the American Janssen Pharmaceutical Co., Ltd. Da, the English product name is )Wait. Among them, Paliperidone Palmitate Sustained-release Long-acting Injection was launched in the United States on July 31, 2009. It is currently the only one in China that can not only act quickly in the acute phase but also effectively prevent recurrence ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/496A61K31/519A61K47/44A61K47/24A61K47/10A61P25/18
Inventor 王秋成廖峰闫鹏李莹
Owner SHENZHEN FONCOO PHARMACEUTICAL CO LTD
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