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Prolonged Release Formulations Comprising an 2-Oxo-1-Pyrrolidine Derivate

A drug, alkyl technology, applied in the field of extended release formulations containing 2-oxo-1-pyrrolidine derivatives, which can solve problems such as increased total surface area

Inactive Publication Date: 2014-10-08
UCB SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0016] However, because brivaracetam and setraracetam are extremely water soluble (their solubility exceeds 500 mg / ml), slow release to this extent is not obvious, especially with non-monolithic form, since the total surface area thus increases significantly

Method used

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  • Prolonged Release Formulations Comprising an 2-Oxo-1-Pyrrolidine Derivate
  • Prolonged Release Formulations Comprising an 2-Oxo-1-Pyrrolidine Derivate
  • Prolonged Release Formulations Comprising an 2-Oxo-1-Pyrrolidine Derivate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0146] Example 1. Seletracetam Sustained Release Formulation

[0147] Seletracetam granules were prepared according to the composition specified in Table 1.

[0148] Table 1. Core Composition of Seletracetam Granules

[0149]

[0150]

[0151] The resulting active core had an average particle size of 770 μm. in trademark Hydroxypropylmethylcellulose sold under 606 was used as a binder. Grade 606 is preferred.

[0152] Microcrystalline cellulose was used as diluent.

[0153] Talc is an anti-sticking agent.

[0154] Ethyl acrylate-methyl methacrylate copolymer in trademark Sold under NE 30D. It is used as a controlled release polymer.

[0155] Desmethicones sold under the trademark Simethicone are used as defoamers.

[0156] Anhydrous colloidal silica on the mark 200 under sale. It acts as a detackifier and glidant.

[0157] The obtained granules showed the sustained-release properties of seletracetam and met the in vitro dissolution requirements.

[0158] ...

Embodiment 2

[0161] Example 2: All experiments were carried out according to the guidelines of the local animal experiment ethics committee.

[0162] Seizure-like responses in hippocampal slices: Levetiracetam attenuates both high-K+ / low-Ca2+ concentrations-evoked and bicuculline-induced epileptiform responses in rat hippocampal slices. The effect of brivaracetam on high-K+ / low-Ca2+ concentrations or bicuculline-induced epileptiform responses was examined in hippocampal transverse sections prepared from Sprague-Dawley rats according to previously reported standard methods. By changing the normal perfusate (K+3mM; Ca2+2.4mM) of artificial cerebrospinal fluid (ACSF) to high-K+ / low-Ca2+ fluid (HKLCF) (K+7.5mM; Ca2+0.5mM) or to contain 5M formazan ACSF to bicuculline (BMI) induces epileptiform responses.

[0163] Extracellular field potentials (FPs) in the CA3 region of the slices were recorded using 2M NaCl-perfused glass microelectrodes. Evoked FPs were recorded at 10-min intervals in resp...

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Abstract

The invention relates to a pharmaceutical composition comprising Brivaracetam or Seletracetam as active ingredient. The invention relates specifically to a prolonged release formulation made of granules containing the active ingredient in their inner core.

Description

[0001] This application is a divisional application of a Chinese invention patent application with a filing date of November 17, 2009, an application number of 200980145588.7, and an invention title of "Extended Release Preparation Containing 2-oxo-1-pyrrolidine Derivatives". technical field [0002] The present invention relates to oral pharmaceutical compositions of 2-oxo-1-pyrrolidine derivatives, their preparation methods and their therapeutic applications. Background technique [0003] International Patent Application Publication No. WO01 / 62726 discloses 2-oxo-1-pyrrolidine derivatives and methods for their preparation. The application specifically discloses the compound (2S)-2-[(4R)-2-oxo-4-propyl-pyrrolidin-1-yl]butyramide, whose known international nonproprietary name is Brixil Tan. [0004] International Patent Application Publication No. WO2005 / 121082 describes the preparation of 2-oxo-1-pyrrolidine derivatives and discloses in particular that (2S)-2-[(4S)-4-(2,2-...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K9/16A61K31/4015A61P25/08A61P25/16A61P25/14A61P25/06A61P25/18A61P29/00A61P25/00
CPCA61K9/5026A61K9/50A61P25/00A61P25/06A61P25/08A61P25/14A61P25/16A61P25/18A61P29/00A61K9/4891A61K31/4015
Inventor D·法纳拉F·艾克曼M·贝尔韦尔
Owner UCB SA