Cariprazine trihydrate compound

A technology of cariprazine trihydrate and trihydrate, applied in the field of medicine, can solve the problems of high impurity content, moisture absorption and weight gain, difficulty in purifying cariprazine and the like

Inactive Publication Date: 2017-05-24
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In the actual production process, the applicant found that there were problems such as difficult purification, high impurity content and certain moisture absorption and weight gain in the preparation process of cariprazine

Method used

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  • Cariprazine trihydrate compound
  • Cariprazine trihydrate compound
  • Cariprazine trihydrate compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] In a 100L reactor, add 6 kg of cariprazine trihydrate to a mixture of 10 times (weight-volume ratio) tetrahydrofuran-ethyl acetate-water=4.3:0.8:5, heat to 70°C and keep warm 30 minutes, strain while hot. The filtrate was kept at 47°C for 1 hour; then naturally cooled to 35°C and held for 10 hours, the precipitated crystals were filtered and dried naturally at room temperature to obtain 6.02 kg of white crystals with a purity of 99.92%, and the solvent residue test met the requirements. The moisture measured by the Karl Fischer method is 0.89%.

[0034] Microparticles or microspheres are prepared by combining the compounds of the invention with a pharmaceutically acceptable solid or liquid carrier, and optionally with pharmaceutically acceptable adjuvants and vehicles, using standard and conventional techniques. The composition is used for preparing oral preparations and injections. It is given by way of example only and in no way is it intended to limit the scope of ...

Embodiment 2

[0036] Tablets containing cariprazine trihydrate: 25% by weight of cariprazine trihydrate, appropriate amount of lactose, 30% microcrystalline cellulose, 18% pregelatinized starch, and 8% low-substituted hydroxypropyl cellulose , 1% sodium lauryl sulfate, 0.8% magnesium stearate, appropriate amount of polyvinyl pyrrolidone.

[0037] Process: Preparation of tablet cores: mix the main ingredients and auxiliary materials evenly according to the determined prescription, granulate, ventilate and dry the granules below 40°C, sieve the granules with l6 mesh, add magnesium stearate and remaining starch, and press into tablets. Instantly.

[0038] Isolation layer coating: Add talcum powder to 5% polyvinylpyrrolidone (PVP) absolute ethanol solution, stir evenly, and prepare a 20% suspension as the isolation layer coating solution. Coating is carried out in a fluidized bed, and the process conditions are as follows: spray pressure 0.3 MPa, liquid inlet speed 5mL / min, inlet temperature 3...

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PUM

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Abstract

The invention belongs to the technical field of medicines and particularly relates to a cariprazine trihydrate compound. The obtained cariprazine trihydrate compound contains three crystallization waters and has the advantages as follows: the purity is high, the stability is good and moisture-absorption weight gain is not remarkable under the high-humidity condition.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to cariprazine trihydrate and a preparation method thereof, and also relates to the application of the hydrate composition in treating schizophrenia. Background technique [0002] Schizophrenia is a lifelong disabling mental disorder of which the reported worldwide incidence is about 1%. The disorder usually manifests during adolescence or young adulthood; the main symptoms fall into three categories: positive symptoms, such as delusions and hallucinations; negative symptoms, such as an inability to drive and social withdrawal; and cognitive symptoms, such as attention and memory There is a problem. They lead to social and occupational sexual dysfunction, with inescapable implications for the victimized individual's place of existence within the family and wider society. In addition to psychotic symptoms, patients with schizophrenia are at greater risk for medical com...

Claims

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Application Information

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IPC IPC(8): C07D295/135A61K31/495A61P25/18
CPCC07D295/135
Inventor 严洁王志凤
Owner TIANJIN HANKANG PHARMA BIOTECH
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