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Slow-release composition of aripiprazole and derivative thereof and preparation method thereof

A sustained-release composition, aripiprazole technology, applied in the field of insoluble/slightly soluble drug sustained-release composition and its preparation, can solve problems such as injury and side effects of patients

Inactive Publication Date: 2017-05-31
AC PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, as shown in the release curves of Example 5 and Example 6 in the description of this patent, serious burst release phenomenon has occurred, and the release exceeds 10% on the first day. The concentration of the drug will cause serious side effects and even harm to the patient
At the same time, using drug granules as the core is similar to the effect of preparing drug granules with different particle sizes in the patent CN201110059685, and the effect of particle size on the dissolution rate also exists

Method used

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  • Slow-release composition of aripiprazole and derivative thereof and preparation method thereof
  • Slow-release composition of aripiprazole and derivative thereof and preparation method thereof
  • Slow-release composition of aripiprazole and derivative thereof and preparation method thereof

Examples

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Effect test

Embodiment 1

[0071] An embodiment of the sustained-release composition of aripiprazole and its derivatives of the present invention, the non-solvent preparation raw material of the sustained-release composition described in this embodiment contains the following components in mass percentage: lauroyl arabine 55% of ripiprazole and 45% of a poorly water-soluble polymer PLGA (mol ratio of lactide to glycolide: 85:15, weight average molecular weight of 50 kDa, viscosity of 0.44 dL / g, and carboxyl end).

[0072] The sustained-release composition described in this example is prepared by the following preparation method:

[0073] (1) dissolving the poorly water-soluble polymer in dichloromethane, the mass percentage of the poorly water-soluble polymer and dichloromethane is 7%, then adding lauroyl aripiprazole, dissolving evenly, forming an internal phase;

[0074] (2) PVA is dissolved in water to form an external phase, and the mass percentage of the PVA in the external phase is 0.1%;

[0075]...

Embodiment 2

[0078]An embodiment of the sustained-release composition of aripiprazole and its derivatives of the present invention, the non-solvent preparation raw material of the sustained-release composition described in this embodiment contains the following components in mass percentage: aripiprazole 60% and 40% of water insoluble polymer; Wherein, described water insoluble polymer is made of PLGA (the molar ratio of lactide and glycolide is 80:20, weight average molecular weight is 75kDa, viscosity is 0.63dL / g , with an ester group end) and PLA (with an ester group end, the weight average molecular weight of PLA is 80kDa, and the viscosity is 0.65dL / g), and the mass ratio of PLGA to PLA is 3:1.

[0079] The sustained-release composition described in this example is prepared by the following preparation method:

[0080] (1) dissolving the poorly water-soluble polymer in chloroform, the mass percentage of the poorly water-soluble polymer and chloroform being 5%, then adding aripiprazole...

Embodiment 3

[0085] An embodiment of the sustained-release composition of aripiprazole and its derivatives of the present invention, the non-solvent preparation raw material of the sustained-release composition described in this embodiment contains the following components in mass percentage: aripiprazole 45%, water insoluble polymer 55%; Wherein, described water insoluble polymer is PLGA (the molar ratio of lactide and glycolide is 95:5, weight average molecular weight is 25kDa, viscosity is 0.28dL / g , with ester-terminals) and PLGA (lactide-to-glycolide molar ratio of 85:15, weight-average molecular weight of 25 kDa, viscosity of 0.29 dL / g, with ester-terminals), PLGA (lactide The molar ratio to glycolide is 95:5, the weight-average molecular weight is 25kDa, the viscosity is 0.28dL / g, and has an ester terminal) and PLGA (the molar ratio of lactide to glycolide is 85:15, and the weight-average Molecular weight is 25kDa, viscosity is 0.29dL / g, has ester group end) mass ratio is 30:25.

...

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Abstract

The invention discloses a slow-release composition of aripiprazole and derivative thereof and a preparation method thereof. The non-solvent form of the slow-release composition of aripiprazole and derivative thereof is prepared from raw materials including aripiprazole or aripiprazole derivative and water-insoluble polymer. The slow-release composition of aripiprazole and derivative thereof disclosed by the invention avoids obvious phenomenon of release lag or burst release after administration to realize a good slow-release property, and can maintain stable therapeutic plasma concentration in several weeks or longer time; and moreover, with relatively high stability, the slow-release composition still can maintain the slow release behavior after long-time storage.

Description

technical field [0001] The invention relates to a sustained-release composition of poorly water-soluble / slightly soluble drugs and a preparation method thereof, in particular to a sustained-release composition of aripiprazole and its derivatives and a preparation method of the sustained-release composition. Background technique [0002] The bioavailability of common dosage forms made of many poorly water-soluble / slightly soluble drugs is low, and it is an ideal choice to develop them into long-acting sustained-release dosage forms, which can reduce the required concentration fluctuations caused by frequent administration and improve patients' health. compliance. [0003] Patent CN201110059685 discloses a method for preparing spherical particles of insoluble drugs, in which insoluble drugs (such as aripiprazole and olanzapine pamoate) are dissolved in a lipophilic solvent to prepare a dispersed phase, and then added to the An emulsion is formed in the immiscible continuous p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/34A61K31/496
CPCA61K9/0002A61K9/1641A61K31/496
Inventor 刘锋赖树挺曹付春郑阳连远发
Owner AC PHARMA CO LTD
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