ArticleBiomolecules & therapeutics2015
Preclinical Pharmacokinetic Evaluation of β-Lapachone: Characteristics of Oral Bioavailability and First-Pass Metabolism in Rats.
Article in Biomolecules & therapeutics, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 12 papers.
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Who cites it
12 citing papers in PubMed, 28 citations in OpenAlex.
- Pharmacokinetic and safety evaluation of MB12066, an NQO1 substrate.Drug design, development and therapy · 2017Trial
- IR783-Stabilized Nanodrugs Enhance Anticancer Immune Response by Synergizing Oxidation Therapy and Epigenetic Modulation.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
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- Naphth[1,2-Molecules (Basel, Switzerland) · 2023Article
- Isopropyl Gallate, a Gallic Acid Derivative: In Silico and In Vitro Investigation of Its Effects onPharmaceutics · 2022Article
- The possibility of low isomerization of β-lapachone in the human body.Translational and clinical pharmacology · 2021Article
- Rapid Interference-free Analysis of β-Lapachone in Clinical Samples Using Liquid Chromatography-Mass Spectrometry for a Pharmacokinetic Study in Humans.Analytical sciences : the international journal of the Japan Society for Analytical Chemistry · 2021Article
- Anticancer Potential of Resveratrol, β-Lapachone and Their Analogues.Molecules (Basel, Switzerland) · 2020Review
- Mechanically Robust Gastroretentive Drug-Delivery Systems Capable of Controlling Dissolution Behaviors of Coground β-Lapachone.Pharmaceutics · 2019Article
- Activation of NQO-1 mediates the augmented contractions of isolated arteries due to biased activity of soluble guanylyl cyclase in their smooth muscle.Naunyn-Schmiedeberg's archives of pharmacology · 2018Article
- Enhancing Oral Absorption of β-Lapachone: Progress Till Date.European journal of drug metabolism and pharmacokinetics · 2017Review
- Intestinal Permeability of β-Lapachone and Its Cyclodextrin Complexes and Physical Mixtures.European journal of drug metabolism and pharmacokinetics · 2016Article
Corrections and comments
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Authors and funding
8 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
β-Lapachone has drawn increasing attention as an anti-inflammatory and anti-cancer drug. However, its oral bioavailability has not been yet assessed, which might be useful to develop efficient dosage forms possibly required for non-clinical and clinical studies and future market. The aim of the present study was thus to investigate pharmacokinetic properties of β-lapachone as well as its first-pass metabolism in the liver, and small and large intestines after oral administration to measure the absolute bioavailability in rats. A sensitive HPLC method was developed to evaluate levels of β-lapachone in plasma and organ homogenates. The drug degradation profiles were examined in plasma to assess the stability of the drug and in liver and intestinal homogenates to evaluate first-pass metabolism. Pharmacokinetic profiles were obtained after oral and intravenous administration of β-lapachone at doses of 40 mg/kg and 1.5 mg/kg, respectively. The measured oral bioavailability of β-lapachone was 15.5%. The considerable degradation of β-lapachone was seen in the organ homogenates but the drug was quite stable in plasma. In conclusion, we suggest that the fairly low oral bioavailability of β-lapachone may be resulted from the first-pass metabolic degradation of β-lapachone in the liver, small and large intestinal tracts and its low aqueous solubility.
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