ArticleAAPS PharmSciTech2016
pH-Dependent Solubility and Dissolution Behavior of Carvedilol--Case Example of a Weakly Basic BCS Class II Drug.
Article in AAPS PharmSciTech, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 48 papers.
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Who cites it
48 citing papers in PubMed.
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- Dissolution Enhancement by Binding Agents: A Potential Shortcut to Improving Bioavailability?The AAPS journal · 2026Article
- Design, optimization and characterization of mucoadhesive buccal film as a novel delivery system for doxazosin mesylate.Saudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2026Article
- Sugar-Based Eutectic Systems Combined with Cyclodextrins for Enhanced Solubility of Carvedilol.Molecules (Basel, Switzerland) · 2026Article
- Optimizing Particle Size of pH Modifiers Enhances Dissolution of Weakly Basic Drugs.AAPS PharmSciTech · 2026Article
- Effect of Spinacia oleracea on In Vitro Disintegration and Dissolution of Clopidogrel Bisulfate Tablets.Pharmacology research & perspectives · 2026Article
- Quality by design approach for optimization, in-vitro and in-vivo evaluation of compression-spheronized itopride hydrochloride loaded gastroretentive pellets for the treatment of gastroesophageal reflux disease.Naunyn-Schmiedeberg's archives of pharmacology · 2026Article
- Carvedilol Pharmaceutical Cocrystals: Preparation, Advanced Characterization and Dissolution Behavior.AAPS PharmSciTech · 2026Article
- Fabrication of Second-Generation Acalabrutinib Nanocrystals by Employing the Nano-Edge Method for Improving the Physico-Chemical Properties and Forecasting their In-Silico Pharmacokinetic Behaviour.AAPS PharmSciTech · 2026Article
- The Advancement of In Vitro Lipolysis: Two-Step Flow-Through Method for the Evaluation of Lipid-Based Drug Delivery Systems.Pharmaceutics · 2025Article
- Mucin Mimics and Impacts the Function of Polymeric Inhibitors in Stabilizing Drug Supersaturation.Molecular pharmaceutics · 2025Article
- Impact of Simulated Gastrointestinal Fluid: Viscosity, Surface Tension, and pH on the Dissolution and Rheology Assessment of Viscosity of Two Commercial Candesartan Cilexetil Products.Turkish journal of pharmaceutical sciences · 2025Article
- Oral delivery of the non-β-blocking R-carvedilol enantiomer for skin cancer chemoprevention in SKH-1 mice.AAPS open · 2025Article
- Design of colon-targeted drug delivery of dexamethasone: Formulation and in vitro characterization of solid dispersions.Heliyon · 2024Article
- A child-friendly anti-infective gummy formulation: Design, physicochemical, micromechanical, and taste sensory evaluation.Drug delivery and translational research · 2024Article
- Polymeric Amorphous Solid Dispersions of Dasatinib: Formulation and Ecotoxicological Assessment.Pharmaceutics · 2024Article
- Development of a UPLC-MS/MS method for quantifying KPT-335 (Verdinexor) in feline plasma for a study of PK.Frontiers in veterinary science · 2024Article
- Development of a Carvedilol Oral Liquid Formulation for Paediatric Use.Pharmaceutics · 2023Article
- Flexible New Dosage Forms Containing Carvedilol for the Treatment of Patients with Cardiovascular Disorders: Development, Stability, Palatability, and Microbiological Studies.AAPS PharmSciTech · 2023Article
- Dabrafenib-Panobinostat Salt: Improving the Dissolution Rate and Inhibition of BRAF Melanoma Cells.ACS omega · 2023Article
Corrections and comments
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Authors and funding
8 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The objective of this study was to investigate the pH-dependent solubility and dissolution of weakly basic Biopharmaceutical Classification Systems (BCS) class II drugs, characterized by low solubility and high permeability, using carvedilol, a weak base with a pK a value of 7.8, as a model drug. A series of solubility and in vitro dissolution studies was carried out using media that simulate the gastric and intestinal fluids and cover the physiological pH range of the GI from 1.2 to 7.8. The effect of ionic strength, buffer capacity, and buffer species of the dissolution media on the solubility and dissolution behavior of carvedilol was also investigated. The study revealed that carvedilol exhibited a typical weak base pH-dependent solubility profile with a high solubility at low pH (545.1-2591.4 μg/mL within the pH range 1.2-5.0) and low solubility at high pH (5.8-51.9 μg/mL within the pH range 6.5-7.8). The dissolution behavior of carvedilol was consistent with the solubility results, where carvedilol release was complete (95.8-98.2% released within 60 min) in media simulating the gastric fluid (pH 1.2-5.0) and relatively low (15.9-86.2% released within 240 min) in media simulating the intestinal fluid (pH 6.5-7.8). It was found that the buffer species of the dissolution media may influence the solubility and consequently the percentage of carvedilol released by forming carvedilol salts of varying solubilities. Carvedilol solubility and dissolution decreased with increasing ionic strength, while lowering the buffer capacity resulted in a decrease in carvedilol solubility and dissolution rate.
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