ArticleAAPS PharmSciTech2012
Understanding the oral mucosal absorption and resulting clinical pharmacokinetics of asenapine.
Article in AAPS PharmSciTech, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 30 papers, 1 of them a synthesis that pooled it.
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The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.
Who cites it
30 citing papers in PubMed, 1 synthesis or guideline pooled it.
- Therapeutic Impact of Ascorbic Acid on Oral and Periodontal Tissues: A Systematic Literature Review.Medicina (Kaunas, Lithuania) · 2024Pooled it
- Pilot clinical trial of neoadjuvant toll-like receptor 7 agonist (Imiquimod) immunotherapy in early-stage oral squamous cell carcinoma.Frontiers in immunology · 2025Trial
- Reduced Use of Antibiotics and Nasal Decongestants During Treatment with a Mouthwash Containing Delmopinol.Oral health & preventive dentistry · 2023Trial
- Trial
- The effect of food on the high clearance drug asenapine after sublingual administration to healthy male volunteers.European journal of clinical pharmacology · 2015Trial
- Pharmacokinetics of a novel sublingual spray formulation of the antimalarial drug artemether in healthy adults.Antimicrobial agents and chemotherapy · 2015Trial
- Trip killers: Addressing a critical knowledge gap in psychedelic research.Journal of psychopharmacology (Oxford, England) · 2026Review
- In Vitro Oral Cavity Permeability Assessment to Enable Simulation of Drug Absorption.Pharmaceutics · 2025Article
- Evaluation of Drug Permeation Enhancement by Using In Vitro and Ex Vivo Models.Pharmaceuticals (Basel, Switzerland) · 2025Review
- Polyphenolic compounds in combating MDR periodontal pathogens: current research and future directions.Frontiers in pharmacology · 2025Review
- Evaluation of Monolayer and Bilayer Buccal Films Containing Metoclopramide.Pharmaceutics · 2024Article
- The Bioavailability of CHF6563, an Ethanol-Free, Sublingual Neonatal Buprenorphine Formulation: A Bridging Study Conducted in Adults.The journal of pediatric pharmacology and therapeutics : JPPT : the official journal of PPAG · 2024Article
- Eradication of proliferative verrucous leukoplakia with toll-like receptor 7 agonist (topical imiquimod): a case report.Frontiers in oncology · 2024Article
- The Extraordinary Case of a Woman with a 30-Year-Long Diffuse Leishmaniasis Cured with One Single Ampoule of Intranasal Pentavalent Antimoniate.Pathogens (Basel, Switzerland) · 2023Article
- Harnessing Clinical Trial and Real-World Data Towards an Understanding of Sex Effects on Drug Pharmacokinetics, Pharmacodynamics and Efficacy.Frontiers in pharmacology · 2022Review
- Chewing Gums as a Drug Delivery Approach for Oral Health.International journal of dentistry · 2022Review
- A novel amorphous solid dispersion based on drug-polymer complexation.Drug delivery and translational research · 2021Article
- Pharmacokinetic Model Analysis of Supralingual, Oral and Intravenous Deliveries of Mycophenolic Acid.Pharmaceutics · 2021Article
- Evaluation of clinical, histological, TNF-α, and collagen expressions on oral ulcer in rats after treatment withF1000Research · 2021Article
- Assessing Effects of BHV-0223 40 mg Zydis Sublingual Formulation and Riluzole 50 mg Oral Tablet on Liver Function Test Parameters Utilizing DILIsym.Toxicological sciences : an official journal of the Society of Toxicology · 2020Article
Corrections and comments
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Authors and funding
2 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Absorption of drugs from the oral cavity into the mucosal tissues is typically a fast event. Dissolved drugs partition into the mucosal membranes and within minutes will reach equilibrium with drug in solution in the oral cavity. However, this does not always equate to rapid drug appearance in the systemic circulation. This has been attributed to slow partitioning out of the mucosal tissues and into the systemic circulation. Based on information from literature, physicochemical properties of asenapine, and clinical data, we conclude that for sublingually administered asenapine, the exposure is primarily a function of rapid partitioning into the mucosal membranes. This is followed by slow partitioning out of the mucosal tissues and into the systemic circulation, leading to a T (max) value of about 1 h. The bioavailability of asenapine at doses below the saturation solubility in the mouth does not change and is controlled primarily by mass transport equilibrium. At doses above the saturation solubility, the bioavailability becomes more dependent not only on the distribution equilibrium but also on contact time in the mouth because additional variables (e.g. dissolution rate of the drug) need to be accounted for. These explanations are consistent with oral cavity absorption models from the literature and can be used to accurately describe the clinical data for asenapine.
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