Solid preparation of cariprazine for oral administration

A technology of cariprazine and modified-release cariprazine, which is applied in the direction of non-active ingredient medical preparations, medical preparations containing active ingredients, pill delivery, etc., and can solve the problem of drug insolubility in neutral or alkaline environments And other issues

Inactive Publication Date: 2020-02-07
RICHTER GEDEON NYRT
View PDF9 Cites 5 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, a drug that is soluble in an acidic environment may actually be insoluble in a neutral or alkaline environment

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
  • Solid preparation of cariprazine for oral administration
  • Solid preparation of cariprazine for oral administration
  • Solid preparation of cariprazine for oral administration

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0214] Embodiment 1: floating sheet (F1)

[0215] F1 floating tablets were prepared by fluidized granulation, in which cariprazine was mixed with microcrystalline cellulose and alginic acid in a fluidized bed apparatus; the mixture was then sprayed with aqueous citric acid. The dried granules were covered with glyceryl distearate by heating the granules. In the final step, the granules are mixed with the external phase (hypromellose, sodium bicarbonate, colloidal anhydrous silicon dioxide, magnesium stearate) and compressed into tablets using rotary tablet press equipment.

[0216] The composition contains gas forming agents and release modifiers to increase residence time in the stomach throughout the 8 hour dissolution time course.

[0217]

[0218] Table 4: Qualitative and quantitative composition of F1 floating flakes

[0219] F1 floating tablets exhibit an in vitro release profile in which, on average, no more than about 15-35% of the total cariprazine is released ...

Embodiment 2

[0223] Embodiment 2: floating sheet (F2)

[0224] F2 floating tablets were prepared by fluidized granulation, in which cariprazine was mixed with microcrystalline cellulose and alginic acid in a fluidized bed apparatus; the mixture was then sprayed with an aqueous solution of citric acid. The dried granules were covered with glyceryl distearate by heating the granules. In the final step, the granules are mixed with the external phase (lactose monohydrate, hypromellose, sodium bicarbonate, colloidal anhydrous silicon dioxide, magnesium stearate) and compressed into tablets using rotary tablet press equipment agent.

[0225] The composition contains gas forming agents and release modifiers to increase residence time in the stomach throughout the 8 hour dissolution time course.

[0226]

[0227] Table 6: Qualitative and quantitative composition of F2 floating flakes

[0228] F2 floating tablets exhibit an in vitro release profile in which, on average, no more than about 2...

Embodiment 3

[0232] Example 3: Capsules (F3) Containing Bioadhesive Beads

[0233] The F3 capsule composition was prepared by the following steps: mixing cariprazine with microcrystalline cellulose and polyacrylic acid polymer in a high shear mixer; after granulating with liquid, extruding the granulated mixture to form a suitable Cylindrical aggregates, which are then rounded into round pellets. Before encapsulation, the pellets are dried in fluid bed equipment; the pellets are sieved to target size and lubricated with talc and calcium stearate. The resulting pellets are filled into hard gelatin capsules.

[0234]

[0235] Table 8: Qualitative and quantitative composition of F3 bioadhesive beads for capsules

[0236] F3 capsules exhibit an in vitro release profile in which, on average, no more than about 55-65% of the total cariprazine is released within 1 hour and no more than the total cariprazine is released within 3 hours after placement in a standard dissolution testing appara...

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

No PUM Login to view more

Abstract

The invention relates oral phamiaceuticai compositions for the modified release delivery of cariprazine (trans-N-{4-[2-[4-(2,3-dichlorophenyl)-piperazin-l-yl]-ethyl]-cyclohexyl}-N',N'- dimethylurea) or pharmaceutically acceptable salts thereof for less than daily dosing. The invention also relates to the use of said compositions in the treatment and / or prevention of pathological conditions which require the modulation of dopamine receptors. The invention also relates to the process for the preparation of said modified release pharmaceutical compositions.

Description

[0001] field of invention [0002] The present invention provides modified release delivery of cariprazine (trans-N-{4-[2-[4-(2,3-dichlorophenyl)- Oral pharmaceutical composition and method of piperazin-1-yl]-ethyl]-cyclohexyl}-N',N'-dimethylurea) or a pharmaceutically acceptable salt thereof. [0003] Background of the invention [0004] Cariprazine is a partial dopamine D3-preferential D3 / D2 receptor agonist. WO 2005 / 012266 A1 discloses cariprazine and pharmaceutically acceptable salts thereof. This document also discloses pharmaceutical compositions comprising cariprazine hydrochloride or other pharmaceutically acceptable salts, and their use in the treatment and / or prevention of pathological conditions requiring modulation of dopamine receptors, said pathological conditions Examples include psychosis (such as schizophrenia, schizoaffective disorder, etc.), substance abuse (such as alcohol, cocaine, nicotine, opioids, etc.), schizophrenia with cognitive impairment (includi...

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
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K9/20A61K9/28A61K31/496A61P25/28A61P25/18
CPCA61K9/0065A61K9/1635A61K9/1652A61K9/2009A61K9/2018A61K9/2027A61K9/2054A61K9/2846A61K9/2866A61K31/495A61P25/18A61P25/28C07D295/03C07D295/033A61K9/2077A61K9/4808A61P25/00A61K9/0053A61K47/38
Inventor M·康塔E·萨巴T·B·达罗克兹Z·玛格斯R·拉兹基纳拉伯斯
Owner RICHTER GEDEON NYRT
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
Try Eureka
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap