METHOD FOR IMPROVING PHARMACEUTICAL PROPERTIES OF MICROPARTICLES COMPRISING DIKETOPIPERAZINE AND ACTIVE AGENT

• Main Authors: MARSHALL GRANT, BRYAN R WILSON
• Format: Patent
• Language: English; Japanese
• Published: 17.03.2016
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

PROBLEM TO BE SOLVED: To provide improved particles and/or an improved dry powder which have more efficient delivery and better stability of an active agent.SOLUTION: A method of producing a dry powder comprises the steps of: (a) providing a solution of diketopiperazine; (b) forming particles of diketopiperazine; and (c) removing a solvent by spray drying to obtain the dry powder. The powder has improved aerodynamic performance, and allows an active agent to be more stable and more efficiently delivered than lyophilized diketopiperazine-insulin formulations. The dry powder has utility as pharmaceutical formulations for pulmonary delivery.SELECTED DRAWING: Figure 1 【課題】活性薬剤のより効率的な送達及びより良い安定性を有する改善された粒子及び/又は改善された乾燥粉末の提供【解決手段】（a）ジケトピペラジンの溶液を提供し、（ｂ）ジケトピペラジンの粒子を形成し、及び（ｃ）噴霧乾燥により溶媒を取り除いて得た乾燥粉末。前記粉末は、改善された空気力学的性能を有し、凍結乾燥されたジケトピペラジン−インシュリン製剤と比較して、活性薬剤がより安定であり、そして効率的に送達される。肺送達のための医薬製剤としての有用性がある、乾燥粉末の製造方法。【選択図】図１