ArticleDrug design, development and therapy2015
Soluplus®/TPGS-based solid dispersions prepared by hot-melt extrusion equipped with twin-screw systems for enhancing oral bioavailability of valsartan.
Article in Drug design, development and therapy, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed.
- Combining High-Throughput Screening and Machine Learning to Predict the Formation of Both Binary and Ternary Amorphous Solid Dispersion Formulations for Early Drug Discovery and Development.Pharmaceutical research · 2025Article
- Design of Experiment Approach for Enhancing the Dissolution Profile and Robustness of Loratadine Tablet Using D-α-Tocopheryl Polyethylene Glycol 1000 Succinate.Pharmaceutics · 2025Article
- Genistein transfersome-embedded topical delivery system for skin melanoma treatment:Drug delivery · 2024Article
- Self-micellizing solid dispersion of thymoquinone with enhanced biopharmaceutical and nephroprotective effects.Drug delivery · 2024Article
- Quality by design-based development and optimization of fourth-generation ternary solid dispersion of standardized Piper longum extract for melanoma therapy.Drug delivery and translational research · 2023Article
- Amorphous Pterostilbene Delivery Systems Preparation-Innovative Approach to Preparation Optimization.Pharmaceutics · 2023Article
- Increasing Cellular Uptake and Permeation of Curcumin Using a Novel Polymer-Surfactant Formulation.Biomolecules · 2022Article
- Pharmaceutical amorphous solid dispersion: A review of manufacturing strategies.Acta pharmaceutica Sinica. B · 2021Review
- Article
- The Development and Validation of a Novel "Dual Cocktail" Probe for Cytochrome P450s and Transporter Functions to Evaluate Pharmacokinetic Drug-Drug and Herb-Drug Interactions.Pharmaceutics · 2020Article
- Enhancement of dissolution of atorvastatin through preparation of polymeric solid dispersions using supercritical fluid technology.Research in pharmaceutical sciences · 2020Article
- Design and Characterization of Cyclosporine A-Loaded Nanofibers for Enhanced Drug Dissolution.ACS omega · 2020Article
- An update on the contribution of hot-melt extrusion technology to novel drug delivery in the twenty-first century: part I.Expert opinion on drug delivery · 2019Review
- Curcumin-loaded self-nanomicellizing solid dispersion system: part I: development, optimization, characterization, and oral bioavailability.Drug delivery and translational research · 2018Article
- Hot Melt Extrusion: Highlighting Physicochemical Factors to Be Investigated While Designing and Optimizing a Hot Melt Extrusion Process.Pharmaceutics · 2018Review
- A Repurposed Drug for Brain Cancer: Enhanced Atovaquone Amorphous Solid Dispersion by Combining a Spontaneously Emulsifying Component with a Polymer Carrier.Pharmaceutics · 2018Article
- Application of Soluplus to Improve the Flowability and Dissolution of Baicalein Phospholipid Complex.Molecules (Basel, Switzerland) · 2017Article
- Challenges and Strategies in Thermal Processing of Amorphous Solid Dispersions: A Review.AAPS PharmSciTech · 2016Review
- Development of megestrol acetate solid dispersion nanoparticles for enhanced oral delivery by using a supercritical antisolvent process.Drug design, development and therapy · 2015Article
Corrections and comments
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Authors and funding
6 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
backgroundSoluplus(®) (SP) and D-alpha-tocopherol polyethylene glycol 1000 succinate (TPGS)-based solid dispersion (SD) formulations were developed by hot-melt extrusion (HME) to improve oral bioavailability of valsartan (VST).
methodsHME process with twin-screw configuration for generating a high shear stress was used to prepare VST SD formulations. The thermodynamic state of the drug and its dispersion in the polymers were evaluated by solid-state studies, including Fourier-transform infrared, X-ray diffraction, and differential scanning calorimetry. Drug release from the SD formulations was assessed at pH values of 1.2, 4.0, and 6.8. Pharmacokinetic study was performed in rats to estimate the oral absorption of VST.
resultsHME with a high shear rate produced by the twin-screw system was successfully applied to prepare VST-loaded SD formulations. Drug amorphization and its molecular dispersion in the polymer matrix were verified by several solid-state studies. Drug release from SD formulations was improved, compared to the pure drug, particularly at pH 6.8. Oral absorption of drug in rats was also enhanced in SP and TPGS-based SD groups compared to that in the pure drug group.
conclusionSP and TPGS-based SDs, prepared by the HME process, could be used to improve aqueous solubility, dissolution, and oral absorption of poorly water-soluble drugs.
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