Aim: To develop dabigatran etexilate (DE)-loaded self-nanoemulsifying drug delivery systems (SNEDDS) for the prevention of stroke and thromboembolism.
Materials & Methods: SNEDDS were optimized by ternary phase diagrams and then further solidified into dispersible tablets. In vitro dissolution was analyzed by a phase distribution study. In situ absorption and in vivo pharmacokinetic studies were tested in male Sprague-Dawley rats.
Results: The phase distribution study showed that more than 60% of DE was retained in the oil phase. Dissolution rate was dramatically enhanced without significant precipitation (<30%) in simulated intestinal fluid. Optimized SNEDDS had 531.80% relative bioavailability compared with Pradaxa(®) capsules (a commercial DE product).
Conclusion: The developed SNEDDS are promising materials for improving the dissolution and oral bioavailability of BCS class IIb drugs.
Download full-text PDF |
Source |
|---|---|
| http://dx.doi.org/10.2217/nnm-2016-0138 | DOI Listing |
Publication Analysis
Top Keywords
Similar Publications
Systematic Analysis of the Design, Methodology and Patient Population Characteristics of the Pediatric Direct Oral Anticoagulant (DOAC) Trials of Venous Thromboembolism Treatment.
J Thromb Haemost
January 2025
Department of Paediatrics, Medical University of Vienna, Vienna, Austria.
Introduction: The pediatric direct oral anticoagulation (DOAC) trials provide an opportunity to evaluate and characterize challenges in their design and execution to inform future antithrombotic trials.
Objective: To perform a systematic review of pediatric DOAC trials for the treatment of venous thromboembolism to critically appraise their methodology and understand the feasibility and challenges.
Methods: Systematic search of MEDLINE, EMBASE, the Cochrane Library and ClinicalTrials.
Characteristics of Gastrointestinal Bleeding While Taking Direct Oral Anticoagulants in Patients with Nonvalvular Atrial Fibrillation and Differences Among Drugs-A Single-Center Retrospective Cohort Study.
J Clin Med
December 2024
Department of Medicine, Teikyo University School of Medicine, Tokyo 173-8605, Japan.
: Direct oral anticoagulants (DOACs) are frequently used to prevent embolism in atrial fibrillation. Gastrointestinal bleeding is frequent, but its drug-specific characteristics remain unclear. This study examined the frequency and characteristics of gastrointestinal bleeding in patients with nonvalvular atrial fibrillation for different DOACs.
View Article and Find Full Text PDFMicrodose Cocktail Study Reveals the Activity and Key Influencing Factors of OATP1B, P-Gp, BCRP, and CYP3A in End-Stage Renal Disease Patients.
Clin Pharmacol Ther
January 2025
Drug Clinical Trial Center, Peking University Third Hospital, Beijing, China.
OATP1B, P-gp, BCRP, and CYP3A are the most contributing drug-metabolizing enzymes or transporters (DMETs) for commonly prescribed medication. Their activities may change in end-stage renal disease (ESRD) patients with large inter-individual variabilities (IIVs), leading to altered substrate drug exposure and ultimately elevated safety risk. However, the changing extent and indictive influencing factors are not quantified so far.
View Article and Find Full Text PDFImportance of infarct topography in determination of stroke mechanism and recurrence risk: a post-hoc analysis of the dabigatran acute treatment of stroke trial.
BMJ Open
January 2025
School of Clinical Medicine, Faculty of Medicine and Health, University of New South Wales, Sydney, New South Wales, Australia
Objective: To evaluate the relationship between infarct pattern, inferred stroke mechanism and risk of recurrence in patients with ischaemic stroke. The question is clinically relevant to optimise secondary stroke prevention investigations and treatment.
Design: We conducted a retrospective analysis of the dabigatran treatment of acute stroke II (DATAS II) trial (ClinicalTrials.
Real-Time Imaging of Platelet-Initiated Plasma Clot Formation and Lysis Unveils Distinct Impacts of Anticoagulants.
Thromb Haemost
January 2025
Department of Medical Physiology, Hamamatsu University School of Medicine, Hamamatsu, Japan.
Background: Fibrinolysis is spatiotemporally well-regulated and greatly influenced by activated platelets and coagulation activity. Our previous real-time imaging analyses revealed that clotting commences on activated platelet surfaces, resulting in uneven-density fibrin structures, and that fibrinolysis initiates in dense fibrin regions and extends to the periphery. Despite the widespread clinical use of direct oral anticoagulants (DOACs), their impact on thrombin-dependent activation of thrombin-activatable fibrinolysis inhibitor (TAFI) and fibrinolysis remains unclear.
View Article and Find Full Text PDFWant AI Summaries of new PubMed Abstracts delivered to your In-box?
Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!