Development of the ciprofloxacin powder formulation for inhalation based on a new drug transport mechanism

2020 Fiscal Year Final Research Report

• Project/Area Number: 19K16460
• Research Category: Grant-in-Aid for Early-Career Scientists
• Allocation Type: Multi-year Fund
• Review Section: Basic Section 47060:Clinical pharmacy-related
• Research Institution: Doshisha Women's College of Liberal Arts
• Principal Investigator: Kimura Shunsuke 同志社女子大学, 薬学部, 助手 (70792274)
• Project Period (FY): 2019-04-01 – 2021-03-31
• Keywords: 非晶質製剤 / 経肺投与 / 肺炎 / 抗菌薬

Outline of Final Research Achievements

To improve the drug content of lung, the new ciprofloxacin (CPFX) powder inhalation system based on a solubility-independent drug membrane transport mechanism was developed. The amorphous formulations of CPFX were prepared by ball milling with amino acids as the co-former. The cumulative membrane transport amount from the amorphous formulations was higher than the crystalline formulation, especially for CPFX/ASP was the highest among them. Similarly, in vivo pharmacokinetic studies, it was showed that the intratracheal administration of CPFX/ASP enabled the higher CPFX content of lung in a short time than any other formulation. In addition, the pulmonary drug content relative to the plasma level was also higher than that of the CPFX solution. The findings suggest that the new powder inhalation system using the amorphous formulation is superior in improving the CPFX content of lung.

Free Research Field

薬物動態学

Academic Significance and Societal Importance of the Research Achievements

従来の肺炎に対する薬物療法では、肺への薬物到達効率の低さが問題であり、治療効率の低下だけではなく、副作用リスクの増大も懸念された。その点、本研究で開発された新規粉末吸入製剤の有用性が高いことは明らかである。特に、本製剤システムは、これまで吸入製剤化の課題であった溶解性や膜透過性について考慮する必要がないことが大きな利点である。さらに、肺炎に限らず、吸入製剤の選択肢が限られる他の呼吸器疾患に対しても応用可能であり、吸入製剤開発における画期的なアプローチとなり得る。