Eureka AIR delivers breakthrough ideas for toughest innovation challenges, trusted by R&D personnel around the world.

Brexpiprazole orally disintegrating tablets

A technology for oral disintegrating tablets and epipiprazole, which is applied in the field of epipiprazole oral disintegrating tablets, can solve the problems of difficulty in covering up the irritation of epipiprazole, the preparation is easily broken, and is uncomfortable for transportation, and achieves enhanced medication administration. The effect of compliance, improved bioavailability, improved taste

Inactive Publication Date: 2016-03-23
BEIJING KANG LISHENG PHARMA TECH DEV
View PDF3 Cites 12 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this technology is relatively cumbersome, and the prepared preparation is easily broken, which is not suitable for transportation, and it cannot be wet when taking it, which increases the requirements for patients and is not conducive to the compliance of schizophrenia patients.
[0008] At the same time, after a large number of experiments, it was found that adding a flavoring agent was difficult to cover the stimulation of ebiprazole, so the traditional simple method was not suitable for preparing ebiprazole orally disintegrating tablets

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Brexpiprazole orally disintegrating tablets
  • Brexpiprazole orally disintegrating tablets
  • Brexpiprazole orally disintegrating tablets

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Epipiprazole Orally Disintegrating Tablets is formulated with the following components, and the dosage is 1000 tablets:

[0021]

[0022]

[0023] Its preparation method comprises the following steps:

[0024] The epipiprazole and the prescription amount of lactose are micronized until the particle size of the raw material is less than 10 μm;

[0025] The micronized raw material and lactose co-powder and the prescription amount of Udraki are mixed evenly;

[0026] 3) The diluent, disintegrant and lubricant are gradually added by an equal amount incremental method, after repeated sieving and mixing, alcohol water is used as a wetting agent, granulated, and dried after external pressure tablet to obtain the oral disintegration of epipiprazole. Unpack.

[0027] 4) Detect the dissolution curve of the prepared orally disintegrating tablet, and it should reach more than 85% in 30 minutes.

[0028] test results

[0029] Mouthfeel: Slightly bitter, but acceptable.

...

Embodiment 2

[0036] Epipiprazole Orally Disintegrating Tablets is formulated with the following components, and the dosage is 1000 tablets:

[0037]

[0038]

[0039] Its preparation method comprises the following steps:

[0040] 1) Micronize epipiprazole and the recipe amount of lactose to the particle size of the raw material <10 μm;

[0041] 2) The micronized raw material and lactose co-powder and the recipe amount are utech, and mix them evenly;

[0042] 3) The diluent, disintegrant and lubricant are gradually added by an equal amount incremental method, after repeated sieving and mixing, alcohol water is used as a wetting agent, granulated, and dried after external pressure tablet to obtain the oral disintegration of epipiprazole. Unpack.

[0043] 4) Detect the dissolution curve of the prepared orally disintegrating tablet, and it should reach more than 85% in 30 minutes.

[0044] test results

[0045] Mouthfeel: No bitterness and numbness, slightly sweet and slightly cool. ...

Embodiment 3

[0052] Epipiprazole Orally Disintegrating Tablets is formulated with the following components, and the dosage is 1000 tablets:

[0053]

[0054]

[0055] Its preparation method comprises the following steps:

[0056] 1) Micronize epipiprazole and the recipe amount of lactose to the particle size of the raw material <10 μm;

[0057] 2) The micronized raw material and lactose co-powder and the recipe amount are utech, and mix them evenly;

[0058] 3) The diluent, disintegrant and lubricant are gradually added by an equal amount incremental method, after repeated sieving and mixing, alcohol water is used as a wetting agent, granulated, and dried after external pressure tablet to obtain the oral disintegration of epipiprazole. Unpack.

[0059] 4) Detect the dissolution curve of the prepared orally disintegrating tablet, and it should reach more than 85% in 30 minutes.

[0060] test results

[0061] Mouthfeel: No bitterness, coolness.

[0062] Compressibility: good

[0...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
Wavelengthaaaaaaaaaa
Login to View More

Abstract

The invention discloses brexpiprazole orally disintegrating tablets and a preparation method of the brexpiprazole orally disintegrating tablets. Bexpiprazole serves as a medicine activity component, and powder co-grinding is conducted on brexpiprazole and lactose so that the dissolution of brexpiprazole and lactose can be improved; eudragit serves as a bitter taste masking agent, a co-ground object is mixed with other auxiliaries to form granules, and finally the tablets are formed through pressing. Due to the fact that brexpiprazole is almost undissolved in water, the dissolution of brexpiprazole can be promoted by preparing the orally disintegrating tablets, and bioavailability is improved; eudragit is used for masking the bitter taste, the bitter and numb taste of brexpiprazole is effectively masked, and the medicine taking compliance of a patient is enhanced.

Description

technical field [0001] The invention relates to a pharmaceutical preparation in the category of oral rapid release, in particular to an orally disintegrating tablet of epipiprazole. Background technique [0002] Epipiprazole Tablets, as 5-HT1A receptor and dopamine D2 receptor agonist, 5-HT2A receptor antagonist, are clinically used for the treatment of major depression and schizophrenia. For the treatment of major depressive disorder, the initial dose is 0.5 mg / day or 1 mg / day, and then increased to the target dose of 2 mg once a day, with a maximum recommended dose of 3 mg / day; for the treatment of schizophrenia, the initial dose It is 1 mg / day, the recommended target dose is 2 mg to 4 mg once daily, and the maximum recommended dose is 4 mg / day. Epipiprazole has broad activity at multiple monoamine systems, with reduced partial agonist activity at dopamine D2 receptors, and reduced activity at specific 5-HT receptors (eg, 5-HT1A, 5-HT2A, 5-HT7). The improved affinity has...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
IPC IPC(8): A61K9/20A61K31/496A61K47/32A61K47/38A61P25/24A61P25/18
CPCA61K31/496A61K9/0056A61K9/2027A61K9/2059
Inventor 程刚
Owner BEIJING KANG LISHENG PHARMA TECH DEV
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com