Intranasal Administration of Milnacipran in Rats: Evaluation of the Transport of Drugs to the Systemic Circulation and Central Nervous System and the Pharmacological Effect
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概要
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Recently, transnasal drug delivery has attracted a great deal of attention as an administration route to deliver drugs directly to the central nervous systems (CNS) and drug targeting of the CNS is expected to increase. In the present study, we investigated the possibility of using a transnasal delivery system for milnacipran, a serotonin–noradrenaline reuptake inhibitor (SNRI), by evaluating the transport to the systemic circulation and cerebrospinal fluid (CSF) and the pharmacological effect after intranasal (i.n.) administration. Moreover, the effect of chitosan as a bioadhesive material on the transport to the systemic circulation and CSF and the pharmacological effect after i.n. administration were evaluated. As a result, i.n. administration of milnacipran was found to produce a higher direct delivery to the CNS as well as to the systemic circulation, suggesting that this is a promising route of administration and an alternative to peroral (p.o.) administration. Furthermore, the i.n. co-administration with chitosan led to increased plasma and CSF concentrations and an enhanced pharmacological effect, evaluated by means of the forced swimming test. The results suggested that chitosan produced a long residence time of milnacipran in the nasal cavity due to its bioadhesive effect, leading to the enhanced transport of milnacipran from the systemic circulation to the CNS via the blood–brain barrier by an increase in systemic absorption as well as direct transport to the CNS, resulting in a higher antidepressant effect compared to that with p.o. administration.
- 公益社団法人 日本薬学会の論文
著者
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Morimoto Yasunori
Faculty of Pharmaceutical Sciences, Josai University
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Uchida Masaki
Faculty Of Pharmaceutical Sciences Josai University
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KOBAYASHI Jun
Faculty of Medicine, Department of Parasitology, University of Ryukyus
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Morimoto Yasunori
Faculty Of Pharmaceutical Sciences Josai University
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NATSUME Hideshi
Faculty of Pharmaceutical Sciences, Josai University
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Uchida Masaatsu
Departments Of Pharmacology Meiji Pharmaceutical University
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Uchida Mihoko
Department Of Biochemistry Faculty Of Pharmaceutical Sciences Hoshi University
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Uchida M
Otsuka Pharmaceutical Co. Ltd. Tokushima Jpn
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Natsume Hideshi
Faculty Of Pharmaceutical Sciences Josai University:research Institute Of Tts Technology
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Katoh Takuya
Faculty of Pharmaceutical Sciences, Josai University
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Mori Mutsuhiro
Scientific Affairs Department, Pharmaceuticals Sales Division, Asahi Kasei Pharma Corporation
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Maeno Takuya
Department of Pharmacy, Kosei Chuo General Hospital
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Ohtake Kazuo
Faculty of Pharmaceutical Sciences, Josai University
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Kobayashi Jun
Faculty Of Agriculture Yamaguchi University
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Uchida Masaki
Faculty of Pharmaceutical Sciences, Josai University
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