HIGHLY CONCENTRATED DRUG PARTICLES, FORMULATION, SUSPENSION, AND USES THEREOF

• Main Authors: RYAN D MERCER, ALESSI THOMAS R, CATHERINE M ROHLOFF, BING YANG
• Format: Patent
• Language: English; Japanese
• Published: 06.07.2017
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

PROBLEM TO BE SOLVED: To provide a novel highly concentrated drug particle formulation.SOLUTION: According to the present invention, a drug accounts for about 25 wt % to about 80 wt % of a particle formulation. The particle formulations of the present invention comprise, for example, macromolecules, such as proteins and/or small molecules (such as steroid hormones). The particle formulation typically further includes one or more additional component, for example, one or more stabilizer (e.g., carbohydrates, antioxidants, amino acids, and buffers). Such concentrated particle formulations can be combined with a suspension vehicle to form suspension formulations. The suspension formulation comprises: (i) a non-aqueous, single-phase vehicle, comprising one or more polymer and one or more solvent, the vehicle exhibiting viscous fluid characteristics; and (ii) a highly concentrated drug particle formulation. Devices for delivering the suspension formulations and methods of use are also described. The present invention provides means for needed improvements in drug formulation and delivery to improve patient compliance and expand drug availability.SELECTED DRAWING: None 【課題】新規な高濃度薬物粒子製剤の提供。【解決手段】薬物は粒子製剤の約２５ｗｔ％〜約８０ｗｔ％を占める。本発明の粒子製剤は例えば、マクロ分子、例えばタンパク質及び／又は小分子（例えばステロイド・ホルモン）を含む。粒子製剤は典型的にはさらに、１又は複数の追加成分、例えば１又は複数の安定剤（例えば炭水化物、抗酸化剤、アミノ酸、及び緩衝剤）を含む。このような高濃度粒子製剤を懸濁ビヒクルと組み合わせることにより、懸濁製剤を形成することができる。懸濁製剤は、（ｉ）１又は複数のポリマー及び１又は複数の溶媒を含む、粘性流体特性を呈する非水性単一相ビヒクルと、（ｉｉ）高濃度薬物粒子製剤とを含んでいる。懸濁製剤の送達装置及び使用方法も記載されている。本発明は患者コンプライアンスを改善し、薬物利用可能性を広げるために、薬物製剤及び送達における必要な改善手段を提供する。【選択図】なし