Trial reportPharmaceutical research2010
Predicting intestinal precipitation--a case example for a basic BCS class II drug.
Trial report in Pharmaceutical research, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 28 papers.
What it found
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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
28 citing papers in PubMed.
- Optimizing Particle Size of pH Modifiers Enhances Dissolution of Weakly Basic Drugs.AAPS PharmSciTech · 2026Article
- Article
- Development and optimization of a novel spectroscopic method to monitor crystallization behavior of BCS-II drug.Turkish journal of chemistry · 2026Article
- Towards sustainable lipidomics: computational screening and experimental validation of chloroform-free alternatives for lipid extraction.Analytical and bioanalytical chemistry · 2025Article
- Development of in vitro-in vivo correlation for establishing patient-centric quality standards of dissolution for lamotrigine extended-release tablets.European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V · 2025Article
- Self-emulsifying Drug Delivery Systems: Concept to Applications, Regulatory Issues, Recent Patents, Current Challenges and Future Directions.Current pharmaceutical biotechnology · 2025Review
- Parameterization of Physiologically Based Biopharmaceutics Models: Workshop Summary Report.Molecular pharmaceutics · 2024Review
- Pharmacokinetics evaluation of newly formulated beads alginate/gum acacia loaded ketoconazole in rabbit plasma by oral administration.ADMET & DMPK · 2024Article
- A Combined In-Vitro and GastroPlus® Modeling to Study the Effect of Intestinal Precipitation on Cinnarizine Plasma Profile in a Fasted State.AAPS PharmSciTech · 2023Article
- Physiologically Based Biopharmaceutics Model for Selumetinib Food Effect Investigation and Capsule Dissolution Safe Space - Part I: Adults.Pharmaceutical research · 2023Article
- The Impact of Water-Soluble Chitosan on the Inhibition of Crystal Nucleation of Alpha-Mangostin from Supersaturated Solutions.Polymers · 2022Article
- An IQ Consortium Perspective on Connecting Dissolution Methods to In Vivo Performance: Analysis of an Industrial Database and Case Studies to Propose a Workflow.The AAPS journal · 2022Article
- An Insight into Eudragit S100 Preserving Mechanism of Cinnarizine Supersaturation.AAPS PharmSciTech · 2022Article
- Role of Permeability on the Biopredictive Dissolution of Amorphous Solid Dispersions.AAPS PharmSciTech · 2021Review
- Use of Physiologically Based Pharmacokinetic Modeling for Predicting Drug-Food Interactions: Recommendations for Improving Predictive Performance of Low Confidence Food Effect Models.The AAPS journal · 2021Article
- The Effects of Dose Volume and Excipient Dose on Luminal Concentration and Oral Drug Absorption.The AAPS journal · 2020Review
- Current Status of Supersaturable Self-Emulsifying Drug Delivery Systems.Pharmaceutics · 2020Review
- Crystallization from Supersaturated Solutions: Role of Lecithin and Composite Simulated Intestinal Fluid.Pharmaceutical research · 2018Article
- Incorporation of lipolysis in monolayer permeability studies of lipid-based oral drug delivery systems.Drug delivery and translational research · 2018Article
- Predictive Performance of Physiologically Based Pharmacokinetic Models for the Effect of Food on Oral Drug Absorption: Current Status.CPT: pharmacometrics & systems pharmacology · 2018Review
Corrections and comments
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo investigate the prediction accuracy of in vitro and in vitro/in silico methods for in vivo intestinal precipitation of basic BCS class II drugs in humans.
methodsPrecipitation rate of a model drug substance, AZD0865 (pKa = 6.1; log K(D) = 4.2), was investigated in vitro using simulated intestinal media, and calculations of the crystallization rates were made with a theoretical model. Human intestinal precipitation was estimated by analysis of pharmacokinetic data from clinical studies at different doses.
resultsAll in vitro models predicted rapid drug precipitation, where the intestinal concentration of dissolved AZD0865 at the highest dose tested was expected to decrease to half after less than 20 min. However, there was no indication of precipitation in vivo in humans as there was a dose proportional increase in drug plasma exposure. The theoretical model predicted no significant precipitation within the range of expected in vivo intestinal concentrations.
conclusionsThis study indicated that simple in vitro methods of in vivo precipitation of orally administered bases overpredict the intestinal crystalline precipitation in vivo in humans. Hydrodynamic conditions were identified as one important factor that needs to be better addressed in future in vivo predictive methods.
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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.