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 Good curative effect and uniform effect

Active Publication Date: 2016-02-10
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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  • Aripiprazole sustained-release microspheres and preparation method thereof
  • Aripiprazole sustained-release microspheres and preparation method thereof
  • Aripiprazole sustained-release microspheres and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Weigh 220.51mg of PLGA (50 / 50-2A, molecular weight 25000 Daltons), 73.39mg of aripiprazole, add 4mL of dichloromethane and acetonitrile (3:1) mixed organic solvent, stir to dissolve, and form an oil phase (O ), quickly drop the oil phase into 100mL of PVA water phase (W) containing 1.5%, and emulsify at 10000rpm for 90s at high speed to form an O / W emulsion, and then dilute the water phase with purified water to double the obtained The O / W type emulsion was placed on a magnetic stirrer at 800 rpm and stirred overnight to volatilize the organic solvent to solidify the microspheres. The microspheres were collected by centrifugation, washed with purified water, and then vacuum freeze-dried to obtain aripiprazole microspheres. The drug loading was 20.63%, and the encapsulation efficiency was 82.52%.

Embodiment 2～7

[0030]

[0031] The microsphere preparation step of embodiment 2~7 is the same as embodiment 1

Embodiment 8～14

[0034] The prescription of table 2 embodiment 8~14 slow-release microspheres

[0035]

[0036] 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 Applications(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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