Title |
The pharmacokinetics of mianserin suppositories for rectal administration in dogs and healthy volunteers: a pilot study
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Published in |
Journal of Pharmaceutical Health Care and Sciences, May 2016
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DOI | 10.1186/s40780-016-0046-7 |
Pubmed ID | |
Authors |
Shuichi Nawata, Noriko Kohyama, Naoki Uchida, Satoshi Numazawa, Masayuki Ohbayashi, Yasuna Kobayashi, Masanori Iwata, Takanori Nakajima, Hiroshi Saito, Akira Izuka, Toshinori Yamamoto |
Abstract |
We formulated mianserin suppositories for the treatment of delirium and evaluated their pharmacokinetics by measuring plasma drug concentrations in dogs and healthy human volunteers. Mianserin suppositories were prepared by a melting technique using Tetramide® tablets and Witepsol H-15 as the suppository base. Pharmacokinetics of this 30-mg mianserin preparation were evaluated in three beagle dogs and three healthy adult males, in line with ethics committee approval. Plasma mianserin levels were determined using gas chromatography-mass spectrometry. In dogs, the maximum plasma mianserin concentration (Cmax) was 1.3 ± 0.4 ng/mL, the time to Cmax (tmax) was 5.5 ± 4.3 h, and the area under the plasma concentration-time curve from 0 to 24 h (AUC0-24) was 18.9 ± 1.9 h・ng/mL. In humans, the Cmax was 14.6 ± 6.3 ng/mL, the tmax was 8 h, and the AUC0-24 was 266 ± 103 h・ng/mL. The current study characterized the pharmacokinetics of mianserin suppositories in dogs and humans. As compared to oral administration, the suppositories produced a lower Cmax and a delayed tmax, although AUC0-24 values were comparable. It will be necessary to identify an appropriate dose that produces an adequate plasma mianserin concentration for effective and safe clinical use. UMIN000013853. |
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Demographic breakdown
Readers by professional status | Count | As % |
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Unspecified | 1 | 13% |
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Unknown | 2 | 25% |
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Unspecified | 1 | 13% |
Neuroscience | 1 | 13% |
Immunology and Microbiology | 1 | 13% |
Unknown | 3 | 38% |