LIMITED-TIME RELEASE TYPE GRANULES, AND APPLICATION OF THE SAME

• Main Authors: OKUDA YUTAKA, HONJO TATSUYA, SATO MASAKI, KOBAYASHI YOSHIYUKI, SAEKI ISAMU
• Format: Patent
• Language: English; Japanese
• Published: 15.01.2024
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

To provide limited-time release type granules that have high productivity and versatility, highly suppress elution of active ingredient to form a lag time, and can quickly elute active ingredients after passing the lag time.SOLUTION: Granules are formed and prepared by a core part containing active ingredients and a coating layer covering the core part. The content mass of a water-swellable substance in the core part is less than 15 mass%. The coating layer includes (meth)acrylic polymer having ammonio methacrylate unit, and does not substantially include a water-swellable substance and a salting-out insolubilization promoter. In the granules, the elution rate of active ingredient at pH1.2 in an elution test paddle method is 85% or more for 60 minutes.SELECTED DRAWING: None 【課題】生産性および汎用性が高く、有効成分の溶出を高度に抑制してラグ時間を形成し、ラグ時間経過後は速やかに有効成分を溶出できる時限放出型顆粒を提供する。【解決手段】有効成分を含む核部と、この核部を被覆するコーティング層とで形成して、顆粒を調製する。前記核部中の水膨潤性物質の含有質量は１５質量％未満である。前記コーティング層は、アンモニオメタクリレート単位を有する（メタ）アクリル系重合体を含み、かつ水膨潤性物質および塩析型不溶化促進剤を実質的に含まない。前記顆粒は、溶出試験パドル法において、ｐＨ１．２での有効成分の溶出率が６０分で８５％以上である。【選択図】なし