Preparation method of brexpiprazole tablets

A technology of breiprazole tablets and breiprazole, which is applied to medical preparations with no active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, can solve problems such as difficulty in improving the dissolution rate, and achieve high temperature suppression Degradation, ensuring drug stability, and reducing the effect of extrusion temperature

Pending Publication Date: 2021-01-05
浙江诺得药业有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Bripiprazole is almost insoluble in water. When prepared under conventional hot-melt conditions, the dispersed particles of breiprazole are prone to degradation during high-temperature hot-melt, and it is difficult to improve the dissolution rate of breiprazole when low-temperature hot-melt.

Method used

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  • Preparation method of brexpiprazole tablets
  • Preparation method of brexpiprazole tablets
  • Preparation method of brexpiprazole tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The prescription technology of embodiment 1-5 is shown in Table 1, and the unit of all components is: g.

[0028] Table 1

[0029]

[0030] Preparation:

[0031] Potassium citrate, sorbitol and brepiprazole are heated and melted in a hot-melt extruder, and then the melted material is extruded and granulated, and directly compressed with mannitol, calcium hydrogen phosphate, micropowder silica gel and magnesium stearate .

[0032] Examples 6-10 investigated the types and dosages of fillers and lubricants for each component. The formulation process is shown in Table 2, and the unit of the components in the table is g.

[0033] Table 2

[0034]

[0035] Preparation:

[0036] Potassium citrate, sorbitol and brepiprazole were heated and melted in a hot-melt extruder, and then the melt was extruded into pellets, mixed with the corresponding excipients in each example, and then directly compressed into tablets.

[0037] It can be seen that different fillers are sele...

Embodiment 11

[0039] In the published patent CN107397730A embodiment 2-1, 2-2, 2-3 and embodiment 1, embodiment 2, embodiment 3 in the present invention, in vitro dissolution curve investigation, such as figure 1 ,table 3.

[0040] In vitro dissolution test conditions: Dissolution test method (paddle method, 50rpm), using disodium hydrogen phosphate-citric acid buffer solution (900ml) with a pH value of 4.5 as the test liquid.

[0041] table 3

[0042]

[0043] It can be seen that the present invention heats and melts potassium citrate, sorbitol and brepiprazole in a hot-melt extruder, then extrudes the molten material to granulate, mixes it with the corresponding auxiliary materials in each embodiment, and directly compresses it into tablets , the 5min dissolution rate of the prepared tablet is higher than the dissolution rate of the currently published patents and dosage forms reported in the literature. Therefore, the bripiprazole is made into a solid dispersion, which greatly improv...

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Abstract

The present invention discloses a preparation method of brexpiprazole tablets and belongs to the field of pharmaceutical preparations. The brexpiprazole tablets are prepared by directly tabletting brexpiprazole solid dispersion particles and auxiliary materials, and the brexpiprazole solid dispersion particles are prepared by the following method: heating and melting potassium citrate, sorbitol and brexpiprazole in a hot melt extruder, and extruding and granulating the melt materials, wherein a weight ratio of brexpiprazole to potassium citrate is 1:(0.5-2) and a weight ratio of the brexpiprazole to the sorbitol is 1:(1-5). An in-vitro dissolution rate of the brexpiprazole is increased.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a brepiprazole tablet and a preparation method thereof. Background technique [0002] Bripiprazole, chemical name: 7-[4-(4-benzo[B]thiophen-4-yl-1-piperazine)butoxy]-2(1H)-quinolinone, CAS number: 913611 -97-9, molecular formula: C 25 h 27 N 3 o 2 S, molecular weight: 433.57, its chemical structural formula is as follows: [0003] [0004] Bripiprazole is white or off-white crystal or crystalline powder, soluble in N-methylpyrrolidone, slightly soluble in N,N-dimethylacetamide, insoluble in methanol, very insoluble in ethanol (99.5), almost insoluble in water. Poor solubility of brepiprazole is a key factor affecting clinical efficacy. [0005] Bripiprazole, clinically used for schizophrenia and severe depression, is the first dopamine D2, 5-HT1A receptor agonist and 5-HT2A receptor antagonist jointly developed by Denmark's Lundbeck Pharmaceuticals and Japan's O...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/20A61K47/12A61K47/26A61K31/496A61P25/18A61P25/24
CPCA61K9/2095A61K9/2013A61K9/2018A61K31/496A61P25/18A61P25/24
Inventor 刘莎莎胡海波殷学治李晓庆
Owner 浙江诺得药业有限公司
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