ArticlePharmaceutical research2012
Solution behavior of PVP-VA and HPMC-AS-based amorphous solid dispersions and their bioavailability implications.
Article in Pharmaceutical research, 2012. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 21 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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
21 citing papers in PubMed, 101 citations in OpenAlex.
- Mechanism-based classification of in vitro-in vivo correlation failures and model-informed strategies for drug product development.Archives of pharmacal research · 2026Review
- Article
- Modification of Peptide and Permeation Enhancer In Vitro Release Rates by Dispersion with a Gel-Forming Polymer.Pharmaceutical research · 2025Article
- Biofunctional Excipients: Their Emerging Role in Overcoming the Inherent Poor Biopharmaceutical Characteristics of Drugs.Pharmaceutics · 2025Review
- Review
- Dissolution-permeation of hot-melt extruded amorphous solid dispersion comprising an experimental grade of HPMCAS.ADMET & DMPK · 2023Article
- Applicability of an Experimental Grade of Hydroxypropyl Methylcellulose Acetate Succinate as a Carrier for Formation of Solid Dispersion with Indomethacin.Pharmaceutics · 2021Article
- Soluplus-Mediated Diosgenin Amorphous Solid Dispersion with High Solubility and High Stability: Development, Characterization and Oral Bioavailability.Drug design, development and therapy · 2020Article
- Effect of Polymer Hydrophobicity on the Stability of Amorphous Solid Dispersions and Supersaturated Solutions of a Hydrophobic Pharmaceutical.Molecular pharmaceutics · 2019Article
- Investigating the molecular dissolution process of binary solid dispersions by molecular dynamics simulations.Asian journal of pharmaceutical sciences · 2018Article
- Dissolution and uniformity of content of tablets developed with extract of Ximenia americana L.PloS one · 2018Article
- Design and Solidification of Fast-Releasing Clofazimine Nanoparticles for Treatment of Cryptosporidiosis.Molecular pharmaceutics · 2017Article
- Biorelevant test for supersaturable formulation.Asian journal of pharmaceutical sciences · 2017Review
- Opioid Addiction: Social Problems Associated and Implications of Both Current and Possible Future Treatments, including Polymeric Therapeutics for Giving Up the Habit of Opioid Consumption.BioMed research international · 2017Review
- Initial Drug Dissolution from Amorphous Solid Dispersions Controlled by Polymer Dissolution and Drug-Polymer Interaction.Pharmaceutical research · 2016Article
- Evaluation of the Microcentrifuge Dissolution Method as a Tool for Spray-Dried Dispersion.The AAPS journal · 2016Article
- Freeze Dried Quetiapine-Nicotinamide Binary Solid Dispersions: A New Strategy for Improving Physicochemical Properties and Ex Vivo Diffusion.Journal of pharmaceutics · 2016Article
- Solid-state characterization of Felodipine-Soluplus amorphous solid dispersions.Drug development and industrial pharmacy · 2016Article
- The effect of polymeric excipients on the physical properties and performance of amorphous dispersions: Part I, free volume and glass transition.Pharmaceutical research · 2015Article
- Fundamental aspects of solid dispersion technology for poorly soluble drugs.Acta pharmaceutica Sinica. B · 2014Review
Corrections and comments
PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.
Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo identify the mechanism behind the unexpected bio-performance of two amorphous solid dispersions: BMS-A/PVP-VA and BMS-A/HPMC-AS.
methodsSolubility of crystalline BMS-A in PVP-VA and HPMC-AS was measured by DSC. Drug-polymer interaction parameters were obtained by Flory-Huggins model fitting. Drug dissolution kinetics of spray-dried dispersions were studied under sink and non-sink conditions. BMS-A supersaturation was studied in the presence of pre-dissolved PVP-VA and HPMC-AS. Potency and crystallinity of undissolved solid dispersions were determined by HPLC and DSC. Polymer dissolution kinetics were obtained by mass balance calculation. Bioavailability of solid dispersions was assessed in dogs.
resultsIn solid state, both polymers are miscible with BMS-A, while PVP-VA solublizes the drug better. BMS-A dissolves similarly from both solid dispersions in vitro regardless of dissolution method, while the HPMC-AS dispersion performed much better in vivo. At the same concentration, HPMC-AS is more effective in prolonging BMS-A supersaturation; this effect was negated by the slow dissolution rate of HPMC-AS. Further study revealed that fast PVP-VA dissolution resulted in elevated drug loading in undissolved dispersions and facilitated drug recrystallization before complete release. In contrast, the hydrophobicity and slower HPMC-AS dissolution prevented BMS-A recrystallization within the HPMC-AS matrix for >24 h.
conclusionsThe lower bioavailability of PVP-VA dispersion was attributed to BMS-A recrystallization within the undissolved dispersion, due to hydrophilicity and fast PVP-VA dissolution rate. Polymer selection for solid dispersion development has significant impact on in vivo performance besides physical stability.
Indexed as
Identifiers
What OpenQuestion holds
Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.