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5 MGLU5 PHARMACEUTICAL COMPOSITIONS OF METABOTROPIC GLUTAMATE 5 RECEPTOR MGLU5 ANTAGONISTS

机译:5代谢谷氨酸的MGLU5药物成分5受体MGLU5拮抗剂

摘要

The present invention relates to a pharmaceutical composition of a metabotropic glutamate 5 receptor (mGlu5) antagonist or a pharmacologically acceptable salt thereof. The composition contains a therapeutically active compound, a nonionic polymer and an ionic polymer, a binder and a filler in the form of matrix pellets, matrix tablets or coated pellets. The composition provides a pH-independent in vitro release profile of 70% NMT within 1 hour, 85% NMT within 4 hours, and 80% NLT within 8 hours. Such compositions are useful for the treatment of CNS disorders such as, for example, treatment-resistant depression (TRD) and fragile X chromosome syndrome.
机译:本发明涉及代谢型谷氨酸5受体(mGlu5)拮抗剂或其药理学上可接受的盐的药物组合物。该组合物包含治疗活性化合物,非离子聚合物和离子聚合物,以基质丸粒,基质片剂或包衣丸粒形式的粘合剂和填充剂。该组合物在1小时内提供70%NMT,在4小时内提供85%NMT,在8小时内提供80%NLT的非pH依赖性体外释放曲线。这样的组合物可用于治疗CNS疾病,例如抗治疗性抑郁症(TRD)和脆弱的X染色体综合征。

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