Development of a mianserin suppository for patients with delirium and depression who cannot take it orally

Research Project

Project/Area Number	16K18958
Research Category	Grant-in-Aid for Young Scientists (B)
Allocation Type	Multi-year Fund
Research Field	Medical pharmacy
Research Institution	Showa University
Principal Investigator	Nawata Shuichi 昭和大学, 薬学部, 講師 (10744386)
Project Period (FY)	2016-04-01 – 2020-03-31
Project Status	Completed (Fiscal Year 2019)
Budget Amount *help	¥2,340,000 (Direct Cost: ¥1,800,000、Indirect Cost: ¥540,000) Fiscal Year 2018: ¥130,000 (Direct Cost: ¥100,000、Indirect Cost: ¥30,000) Fiscal Year 2017: ¥650,000 (Direct Cost: ¥500,000、Indirect Cost: ¥150,000) Fiscal Year 2016: ¥1,560,000 (Direct Cost: ¥1,200,000、Indirect Cost: ¥360,000)
Keywords	せん妄 / 抑うつ / 経口摂取困難 / ミアンセリン / 坐剤 / 薬物動態 / 高齢者 / ミアンセリン坐剤 / 薬物動態試験 / 臨床薬物動態 / 在宅医療
Outline of Final Research Achievements	There is a limited number of drugs available for patients with depression and delirium that are difficult to administer orally. Therefore, we developed a mianserin suppositories that is expected to be effective for both symptoms. Based on the pharmacokinetics of the suppositories in healthy adult males, we concluded that the suppository has the potential for clinical application. Therefore, in the present study, we further investigated the pharmacokinetics of the suppository in the elderly, who are often used in practice. The pharmacokinetics were studied in three healthy elderly adult males. The results showed that a single 20 mg dose had a slow increase in blood concentration. Based on these results, it was concluded that the efficacy and safety of the drug should be ensured by starting at 20 mg, and increasing the dose as the clinical effect of the drug is monitored. It was suggested that it could be done.
Academic Significance and Societal Importance of the Research Achievements	経口投与が困難な患者に対して、服用していた錠剤を粉砕して基剤と混合し、坐剤として投与する方法は、従来より行われてきた。しかし、坐剤として投与した際の薬物動態の検討が行われるケースは少ない。また、吸収促進を目的に医薬品以外の基剤が使用されるケースも多く、日常臨床への応用が困難なケースが多く見受けられる。今回、我々は、ミアンセリン錠を粉砕して医薬品の基剤と混合しただけの坐剤において、若年成人と高齢成人での薬物動態の違いを明らかにした。特に高齢成人での坐剤の薬物動態に関する研究報告は、ほとんどなく、今後の坐剤開発においても有益な情報を社会に発信できたと考えらる。