ArticlePharmaceutical research2022
pH-Dependent supersaturation from amorphous solid dispersions of weakly basic drugs.
Article in Pharmaceutical research, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- Colloidal Stability of Amorphous Nanoparticles in Solution: Impact of Stabilizer.Pharmaceutical research · 2026Article
- Hot-melt extruded ibuprofen ternary solid dispersions using in-line UV-Vis: Impact of an ionizable polymer on thermodynamics and dissolution.International journal of pharmaceutics: X · 2026Article
- Mechanistic Insights into Amorphous Solid Dispersions: Bridging Theory and Practice in Drug Delivery.Pharmaceutical research · 2025Review
- Trends in amorphous solid dispersion drug products approved by the U.S. Food and Drug Administration between 2012 and 2023.International journal of pharmaceutics: X · 2024Article
- Navigating the Solution to Drug Formulation Problems at Research and Development Stages by Amorphous Solid Dispersion Technology.Recent advances in drug delivery and formulation · 2024Review
- Enteric coating of tablets containing an amorphous solid dispersion of an enteric polymer and a weakly basic drug: A strategy to enhance in vitro release.International journal of pharmaceutics · 2023Article
- Fed- and Fasted-State Performance of Pretomanid Amorphous Solid Dispersions Formulated with an Enteric Polymer.Molecular pharmaceutics · 2023Article
- Impact of Gastric pH Variations on the Release of Amorphous Solid Dispersion Formulations Containing a Weakly Basic Drug and Enteric Polymers.Molecular pharmaceutics · 2023Article
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Authors and funding
7 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeIn amorphous solid dispersions (ASDs), the chemical potential of a drug can be reduced due to mixing with the polymer in the solid matrix, and this can lead to reduced drug release when the polymer is insoluble in the dissolution media. If both the drug and the polymer composing an ASD are ionizable, drug release from the ASD becomes pH-dependent. The goal of this study was to gain insights into the pH-dependent solubility suppression from ASD formulations.
methodsThe maximum release of clotrimazole, a weakly basic drug, from ASDs formulated with insoluble and pH-responsive polymers, was determined as a function of solution pH. Drug-polymer interactions in ASDs were probed using melting point depression, moisture sorption, and solid-state Nuclear Magnetic Resonance spectroscopy (SSNMR) measurements.
resultsThe extent of solubility suppression was dependent on polymer type and drug loading. The strength of drug-polymer interactions was found to correlate well with the degree of solubility suppression. For the same ASD, the degree of solubility suppression was nearly constant across the solution pH range studied, suggesting that polymer-drug interactions in residual ASD solids was independent of solution pH. The total drug release agrees with the Henderson-Hasselbalch relationship if the suppressed amorphous solubility of the free drug is independent of solution pH.
conclusionsThe mechanism of solubility suppression at different solution pHs appeared to be drug-polymer interactions in the solid-state, where the concentration of the free drug remains the same at variable pHs and the total drug concentration follows the Henderson-Hasselbalch relationship.
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