PROLONGED RELEASE FORMULATIONS COMPRISING 2-OXO-1-PYRROLIDINE DERIVATIVE

• Main Authors: FANARA DOMENICO, FREDERIC EECKMAN, MONIQUE BERWAER
• Format: Patent
• Language: English; Japanese
• Published: 06.08.2015
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

PROBLEM TO BE SOLVED: To provide an oral pharmaceutical composition of a 2-oxo-1-pyrrolidine derivative represented by the formula (I) which is effective in epilepsy treatment, and to provide a production method thereof and a method for therapeutic use.SOLUTION: The invention relates to a prolonged release formulation consisting of granulates containing Brivaracetam or Seletracetam as active ingredients in an internal core and coated with a release control layer, and to the use thereof. In the pharmaceutical composition, the release control layer contains an ammonio alkyl methacrylate ethyl acrylate copolymer, an ethyl acrylate methyl methacrylate copolymer, or an ethylcellulose, or a cellulose acetate having an acetyl group of a level contained in the range of 32%-44%, or at least one kind of copolymers which are their mixtures. 【課題】てんかん治療に有効である式（Ｉ）で表される２−オキソ−１−ピロリジン誘導体の経口医薬組成物並びにその製造方法及び治療的使用方法の提供。【解決手段】活性成分としてブリバラセタム又はセレトラセタムを内部コア中に含み、放出制御層で被覆されている粒状物からなる持続放出製剤及び該使用。前記放出制御層が、アンモニオアルキルメタクリレートエチルアクリレートコポリマー、若しくはエチルアクリレートメチルメタクリレートコポリマー、若しくはエチルセルロース、若しくは３２％〜４４％の範囲に含まれるレベルのアセチル基を有するセルロースアセテート、又はそれらの混合物である少なくとも１種のポリマーを含む医薬組成物。【選択図】なし