LONG-LASTING FORMULATION CONTAINING RIVASTIGMINE, AND METHOD FOR PRODUCING THE SAME

To provide sustained-release microspheres for rivastigmine-containing injection formulations that have stable drug release for a long time without initial rapid release although the drug content of rivastigmine in the microspheres is high, and have excellent administration capability and a uniform particle size distribution; to provide a sustained-release injection formulation for preventing or treating Alzheimer's disease containing the microspheres; and to provide a method for producing the microspheres.SOLUTION: The present invention relates to a sustained-release microsphere for injection formulation containing an active ingredient selected from the group consisting of rivastigmine and pharmaceutically acceptable poorly soluble salts thereof, and a biodegradable polymer; to a long-lasting injection formulation containing the same for preventing or treating Alzheimer's disease; and to a method for producing the microsphere, the long-lasting injection formulation containing rivastigmine sustained-release microspheres in which initial rapid drug release is effectively controlled even although there is a high content of the drug, and can thus maximize therapeutic effects by reducing gastrointestinal tract-associated side effects, which often occur in patients who receive conventional orally administered drugs, and increasing medication compliance.SELECTED DRAWING: Figure 3b 【課題】微粒球内リバスチグミンの含有量が高いながらも、初期の急激な放出なしに長期間の安定した薬物放出特性を有し、優れた投与能と均一な粒度分布を有する、リバスチグミン含有注射製剤用徐放性微粒球、微粒球を含むアルツハイマー病の予防・治療用徐放性注射製剤、および微粒球の製造方法の提供。【解決手段】本発明は、リバスチグミンおよびその薬学的に許容可能な難溶性塩からなる群より選ばれる有効成分および生分解性高分子を含む注射製剤用徐放性微粒球、それを含むアルツハイマー病の予防・治療用長期持続型注射製剤および前記微粒球の製造方法に関し、高い含有量でありながらも初期の急激な薬物放出が効果的に調節されるリバスチグミン徐放性微粒球を含む長期持続型注射製剤に関し、従来の経口投与剤でしばしば現れる胃腸管系の副作用を減らし、服薬コンプライアンスを高めて治療効果を極大化できる。【選択図】図３ｂ