ArticleActa pharmacologica Sinica2015
Intestinal absorption characteristics of imperialine: in vitro and in situ assessments.
Article in Acta pharmacologica Sinica, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.
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11 citing papers in PubMed, 22 citations in OpenAlex.
- Revealing key antioxidant compounds and mechanisms in Fritillaria Bulbus by metabolomics and network pharmacology.NPJ science of food · 2025Article
- Integrated UPLC-MS/MS and UPLC-Q-TOF-MS/MS analysis to reveal pharmacokinetics, tissue distribution, metabolism, and excretion of sipeimine in rats.Frontiers in pharmacology · 2025Article
- Promoting oral absorption of Panax notoginseng saponins via thiolated trimethyl chitosan and wheat germ agglutinin-modified nanoformulation.Drug delivery and translational research · 2024Article
- A distinction between Fritillaria Cirrhosa Bulbus and Fritillaria Pallidiflora Bulbus via LC-MS/MS in conjunction with principal component analysis and hierarchical cluster analysis.Scientific reports · 2023Article
- Comparison of intestinal absorption characteristics between rhubarb traditional Chinese medicine preparation and activity ingredients usingChinese herbal medicines · 2023Article
- Bulbus Fritillariae Cirrhosae as a Respiratory Medicine: Is There a Potential Drug in the Treatment of COVID-19?Frontiers in pharmacology · 2021Review
- The Absorption Characteristics of Nonvolatile Components in a Water Extraction FromFrontiers in pharmacology · 2020Article
- A Systematic Review on Traditional Uses, Sources, Phytochemistry, Pharmacology, Pharmacokinetics, and Toxicity of Fritillariae Cirrhosae Bulbus.Evidence-based complementary and alternative medicine : eCAM · 2020Review
- Pharmacokinetic Study of Delavinone in Mice after Intravenous and Oral Administration by UPLC-MS/MS.BioMed research international · 2019Article
- Characterization, Molecular Docking, and In Vitro Dissolution Studies of Solid Dispersions of 20(S)-Protopanaxadiol.Molecules (Basel, Switzerland) · 2017Article
- Developments in Methods for Measuring the Intestinal Absorption of Nanoparticle-Bound Drugs.International journal of molecular sciences · 2016Review
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Authors and funding
6 authors at 2 institutions in 1 country.
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No grant is acknowledged in the PubMed record.
Abstract
aimImperialine is an effective compound in the traditional Chinese medicine chuanbeimu (Bulbus Fritillariae Cirrhosae) that has been used as antitussive/expectorant in a clinical setting. In this study we investigated the absorption characteristics of imperialine in intestinal segments based on an evaluation of its physicochemical properties.
methodsCaco-2 cells were used to examine uptake and transport of imperialine in vitro, and a rat in situ intestinal perfusion model was used to characterize the absorption of imperialine. The amount of imperialine in the samples was quantified using LC-MS/MS.
resultsThe aqueous solubility and oil/water partition coefficient of imperialine were determined. This compound demonstrated a relatively weak alkalinity with a pKa of 8.467±0.028. In Caco-2 cells, the uptake of imperialine was increased with increasing pH in medium, but not affected by temperature. The apparent absorptive and secretive coefficient was (8.39±0.12)×10(-6) cm/s and (7.78±0.09)×10(-6) cm/s, respectively. Furthermore, neither the P-glycoprotein inhibitor verapamil nor Niemann-Pick C1-Like 1 transporter inhibitor ezetimibe affected the absorption and secretion of imperialine in vitro. The in situ intestinal perfusion study showed that the absorption parameters of imperialine varied in 4 intestinal segments (duodenum, jejunum, ileum and colon) with the highest ones in the colon, where a greater number of non-ionized form of imperialine was present.
conclusionThe intestinal absorptive characteristics of imperialine are closely related to its physicochemical properties. The passive membrane diffusion dominates the intestinal absorption of imperialine.
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