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A kind of aripiprazole sustained-release microspheres and preparation method thereof

A technology of aripiprazole and sustained-release microspheres, which is applied in the field of aripiprazole sustained-release microspheres and its preparation, can solve problems such as difficult timely control of adverse drug reactions and complicated preparation techniques, and achieve improved compliance and enhanced Efficacy, the effect of reducing the frequency of administration

Active Publication Date: 2020-01-31
CHONGQING PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It has been found through research that although the technical scheme described in CN101742989B accounts for 55-95% of the drug dosage, it is a shelled microsphere, the preparation technology is relatively complicated, and the sustained release time of the body is more than 2 months. The amount of medicine, but a large amount of medicine is wrapped in the shell, and the one-time injection of medicine can be released for more than 2 months. If there is an adverse drug reaction, it is difficult to control it in time and other safety issues.

Method used

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  • A kind of aripiprazole sustained-release microspheres and preparation method thereof
  • A kind of aripiprazole sustained-release microspheres and preparation method thereof
  • A kind of aripiprazole sustained-release microspheres and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0027] Take by weighing 220.51mgPLGA (50 / 50-2A, molecular weight 25000 Daltons), 73.39mg aripiprazole, add 4mL methylene chloride and acetonitrile (3:1) in the mixed organic solvent, stir and dissolve, form oily phase (O ), the oil phase was quickly added dropwise to 100mL containing 1.5% PVA water phase (W), stirred and emulsified at a high speed of 10000rpm for 90s to form an O / W emulsion, and then the water phase was diluted by one time with purified water, and the obtained The O / W type emulsion was placed on a magnetic stirrer at 800 rpm and stirred overnight to volatilize and remove the organic solvent to solidify the microspheres, collect the microspheres by centrifugation, wash with purified water and freeze-dry in vacuum to obtain aripiprazole microspheres. The drug loading capacity is 20.63%, and the encapsulation efficiency is 82.52%.

Embodiment 2～7

[0029] See Table 1 for the prescription.

[0030] The prescription of table 1 embodiment 2~7 slow-release microspheres

[0031]

[0032] The microsphere preparation step of embodiment 2~7 is the same as embodiment 1

Embodiment 8～14

[0034] The prescription is shown in Table 2.

[0035] The prescription of table 2 embodiment 8~14 slow-release microspheres

[0036]

[0037] The microsphere preparation step of embodiment 8~14 is the same as embodiment 1

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Abstract

The invention relates to aripiprazole sustained-release microspheres and a preparation method thereof. The sustained-release microspheres include aripiprazole and a bio-degradable pharmaceutical high-molecular material PLGA, wherein the ratio of lactic acid to hydroxyacetic acid in the PLGA is 75:50-25:50. The PLGA is 25000-35000 Dolton in molecular weight. The addition weight ratio of the aripiprazole to the PLGA is 1:1-20. The aripiprazole accounts for 3.01-21.09% of total weight of the microsphere. The aripiprazole sustained-release microspheres have high drug embedding rate, is high in drug loading capacity, is smooth and round in surface and can release more than 90% of the drug in 30 days.

Description

technical field [0001] The invention relates to the field of pharmacy, in particular to an aripiprazole sustained-release microsphere and a preparation method thereof. Background technique [0002] Schizophrenia is a common major mental disorder, the etiology of which has not yet been fully elucidated. Most of the onsets are in young adults, and there are often obstacles in perception, thinking, emotion, and behavior. The course of the disease is often protracted. According to the estimation of the World Health Organization, the lifetime prevalence rate of schizophrenia in the world is about 3.8‰~8.4‰. Studies in the United States have shown that the lifetime prevalence rate is as high as 13‰, and the annual new cases and annual incidence rate are about 0.22‰. Once suffering from schizophrenia, patients need to take anti-schizophrenia drugs continuously for life. Years of clinical practice have proved that typical antipsychotic drugs have obvious limitations, which are sp...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/50A61K31/496A61K47/34A61P25/18
Inventor 张涛李璐邓杰
Owner CHONGQING PHARMA RES INST
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