Perampanel sesquihydrate compound

A technology of sesquihydrate and hydrate, which is applied in the field of medicine, can solve the problems of hygroscopic weight gain, difficult purification, high impurity content, etc.

Inactive Publication Date: 2015-05-27
TIANJIN HANKANG PHARMA BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] Perampanel has great advantages in terms of effectiveness and safety, but in the actual production process, the applicant found that there are diffic

Method used

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  • Perampanel sesquihydrate compound
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  • Perampanel sesquihydrate compound

Examples

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Embodiment 1

[0040] Microparticles or microspheres are prepared by combining the compounds of the present 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 the invention in any way.

[0041] Example 2

Embodiment 2

[0043] Prescription: Perampanel sesquihydrate 10.7g, microcrystalline cellulose 12g, pregelatinized starch 16g, sodium starch glycolate 5g, lactose 210g, PEG-4000 25g, magnesium stearate 6g, 30 grams of povidone K30, 33 grams of croscarmellose sodium, appropriate amount of distilled water, made into 10,000 tablets.

[0044] Process:

[0045] Preparation of tablet core: according to the determined prescription, the main ingredient and auxiliary materials are mixed uniformly, granulated, and the granules are ventilated and dried below 40°C, granulated with a 16 mesh sieve, added magnesium stearate and remaining starch, and compressed into tablets to obtain final product .

[0046]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...

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Abstract

The invention belongs to the technical field of medicines and particularly relates to a perampanel sesquihydrate and a preparation method thereof. The perampanel sesquihydrate contains one and a half crystal water. The perampanel sesquihydrate has the advantages that the purity is high; the stability is good, and the moisture absorption and the weight increment are not obvious even at a high humidity condition; by virtue of the perampanel sesquihydrate, the inhibiting effect to the activity of AMPA receptor glutamic acid is increased by about 20%. The invention further relates to application of a composition of the perampanel sesquihydrate in the treatment of neuropsychiatric diseases.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to perampanel sesquihydrate and a preparation method thereof, and also relates to the application of using the hydrate composition to treat diseases in the neuropsychiatric field. Background technique [0002] Epilepsy is a recurrent chronic syndrome caused by abnormal discharge of neurons. It is a common disease with a global prevalence of about 5‰ to 10‰. There are about 20 to 70 new cases per 10,000 people every year. Except for some patients who can be treated for the cause through surgery and other methods, most patients need to take antiepileptic drugs (Antiepileptic Drugs, AEDs) for a long time. Although there are currently more than 20 AEDs approved for marketing in the world, about one-third of the patients with AEDs monotherapy or combination therapy still show drug resistance, which is refractory epilepsy. Therefore, drug developers have been working hard to ...

Claims

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Application Information

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IPC IPC(8): C07D213/57C07D213/127A61K31/444A61P25/08
CPCC07D213/64
Inventor 严洁李轩
Owner TIANJIN HANKANG PHARMA BIOTECH
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