抄録
Peppermint oil has been shown to relax gastrointestinal smooth muscle. In this randomized, placebo-controlled study, an L-menthol preparation, NPO-11, was assessed for tolerability and pharmacokinetics (PK) during gastrointestinal endoscopy. Single doses of NPO-11, as high as 320mg, were well tolerated. NPO-11 was rapidly absorbed, with peak concentrations reached within 1h after administration. Approximately 70% of the administered L-menthol and its metabolites were excreted in the urine, and this amount fluctuated with no change in the dose. The principal metabolite identified in plasma and urine was menthol glucuronide. The other metabolites include mono-or di-hydroxylated menthol derivatives, most of which are excreted, in part, as glucuronic acid conjugates. The pharmacokinetic data indicated that when NPO-11 is sprayed directly onto the gastric mucosa, it is rapidly metabolized to glucuronic acid conjugates that are excreted in urine. The findings from this study provide new data on the safety and PK of NPO-11 and support further trials.
| 元の言語 | English |
|---|---|
| ページ（範囲） | 221-228 |
| ページ数 | 8 |
| ジャーナル | Clinical Pharmacology and Therapeutics |
| 巻 | 90 |
| 発行部数 | 2 |
| DOI | |
| 出版物ステータス | Published - 2011 8 |
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ASJC Scopus subject areas
- Pharmacology
- Pharmacology (medical)
これを引用
A phase i study evaluating tolerability, pharmacokinetics, and preliminary efficacy of l-menthol in upper gastrointestinal endoscopy. / Hiki, N.; Kaminishi, M.; Hasunuma, T.; Nakamura, M.; Nomura, S.; Yahagi, Naohisa; Tajiri, H.; Suzuki, H.
：: Clinical Pharmacology and Therapeutics, 巻 90, 番号 2, 08.2011, p. 221-228.研究成果: Article
}
TY - JOUR
T1 - A phase i study evaluating tolerability, pharmacokinetics, and preliminary efficacy of l-menthol in upper gastrointestinal endoscopy
AU - Hiki, N.
AU - Kaminishi, M.
AU - Hasunuma, T.
AU - Nakamura, M.
AU - Nomura, S.
AU - Yahagi, Naohisa
AU - Tajiri, H.
AU - Suzuki, H.
PY - 2011/8
Y1 - 2011/8
N2 - Peppermint oil has been shown to relax gastrointestinal smooth muscle. In this randomized, placebo-controlled study, an L-menthol preparation, NPO-11, was assessed for tolerability and pharmacokinetics (PK) during gastrointestinal endoscopy. Single doses of NPO-11, as high as 320mg, were well tolerated. NPO-11 was rapidly absorbed, with peak concentrations reached within 1h after administration. Approximately 70% of the administered L-menthol and its metabolites were excreted in the urine, and this amount fluctuated with no change in the dose. The principal metabolite identified in plasma and urine was menthol glucuronide. The other metabolites include mono-or di-hydroxylated menthol derivatives, most of which are excreted, in part, as glucuronic acid conjugates. The pharmacokinetic data indicated that when NPO-11 is sprayed directly onto the gastric mucosa, it is rapidly metabolized to glucuronic acid conjugates that are excreted in urine. The findings from this study provide new data on the safety and PK of NPO-11 and support further trials.
AB - Peppermint oil has been shown to relax gastrointestinal smooth muscle. In this randomized, placebo-controlled study, an L-menthol preparation, NPO-11, was assessed for tolerability and pharmacokinetics (PK) during gastrointestinal endoscopy. Single doses of NPO-11, as high as 320mg, were well tolerated. NPO-11 was rapidly absorbed, with peak concentrations reached within 1h after administration. Approximately 70% of the administered L-menthol and its metabolites were excreted in the urine, and this amount fluctuated with no change in the dose. The principal metabolite identified in plasma and urine was menthol glucuronide. The other metabolites include mono-or di-hydroxylated menthol derivatives, most of which are excreted, in part, as glucuronic acid conjugates. The pharmacokinetic data indicated that when NPO-11 is sprayed directly onto the gastric mucosa, it is rapidly metabolized to glucuronic acid conjugates that are excreted in urine. The findings from this study provide new data on the safety and PK of NPO-11 and support further trials.
UR - http://www.scopus.com/inward/record.url?scp=79960611229&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=79960611229&partnerID=8YFLogxK
U2 - 10.1038/clpt.2011.110
DO - 10.1038/clpt.2011.110
M3 - Article
C2 - 21544078
AN - SCOPUS:79960611229
VL - 90
SP - 221
EP - 228
JO - Clinical Pharmacology and Therapeutics
JF - Clinical Pharmacology and Therapeutics
SN - 0009-9236
IS - 2
ER -