申请人:ADARE PHARMACEUTICALS, INC.
公开号:US10568832B2
公开(公告)日:2020-02-25
There is provided a method for preparing an orally disintegrating tablet (ODT) composition comprising microparticles of one or more taste-masked active pharmaceutical ingredient(s), rapidly-dispersing microgranules, and other optional, pharmaceutically acceptable excipients wherein the ODT disintegrates on contact with saliva in the buccal cavity in about 60 seconds forming a smooth, easy-to-swallow suspension. Furthermore, the microparticles (crystals, granules, beads or pellets containing the active) applied with a taste-masking membrane comprising a combination of water-insoluble and gastrosoluble polymers release not less than about 60% of the dose is in the stomach in about 30 minutes, thus maximizing the probability of achieving bioequivalence to the reference IR product having rapid onset of action (short Tmax). A process for preparing such compositions for oral administration using conventional fluid-bed equipment and rotary tablet press is also disclosed.
本发明提供了一种制备口腔崩解片(ODT)组合物的方法,该组合物包含一种或多种掩味活性药物成分的微颗粒、快速分散微粒和其他任选的、药学上可接受的赋形剂,其中口腔崩解片在颊腔中与唾液接触后约 60 秒内崩解,形成平滑、易于吞咽的悬浮液。此外,微颗粒(晶体、颗粒、珠子或含有活性物质的小丸)上涂有掩味膜,掩味膜由水不溶性聚合物和胃溶性聚合物组合而成,在约 30 分钟内可释放出不少于 60% 的胃内剂量,从而最大限度地提高了与快速起效(短 Tmax)的参考红外产品实现生物等效性的可能性。此外,还公开了一种使用传统流化床设备和旋转式压片机制备此类口服组合物的工艺。