A phase i study evaluating tolerability, pharmacokinetics, and preliminary efficacy of l-menthol in upper gastrointestinal endoscopy

N. Hiki, M. Kaminishi, T. Hasunuma, M. Nakamura, S. Nomura, N. Yahagi, H. Tajiri, H. Suzuki

Research output: Contribution to journalArticle

21 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)221-228
Number of pages8
JournalClinical Pharmacology and Therapeutics
Volume90
Issue number2
DOIs
Publication statusPublished - 2011 Aug 1

ASJC Scopus subject areas

  • Pharmacology
  • Pharmacology (medical)

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