ArticlePharmaceutical research2013
Supersolubilization and amorphization of a model basic drug, haloperidol, by interaction with weak acids.
Article in Pharmaceutical research, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 48 citations in OpenAlex.
- Amorphization of Albendazole Using Organic Acid-based Solid Dispersions for Improved Dissolution: A Solvent-free Approach.AAPS PharmSciTech · 2025Article
- Impact of the Coformer Carbon-Chain Length on the Properties of Haloperidol Pharmaceutical Salts.Crystal growth & design · 2025Article
- Effects of Different Weak Small Organic Acids on Clofazimine Solubility in Aqueous Media.Pharmaceutics · 2024Article
- Drug Dissolution in Oral Drug Absorption: Workshop Report.The AAPS journal · 2023Article
- Release Enhancement by Plasticizer Inclusion for Amorphous Solid Dispersions Containing High TPharmaceutical research · 2023Article
- Challenges, current status and emerging strategies in the development of rapidly dissolving FDM 3D-printed tablets: An overview and commentary.ADMET & DMPK · 2023Review
- Chemical Stability Study of HMolecules (Basel, Switzerland) · 2022Article
- Citric Acid: A Multifunctional Pharmaceutical Excipient.Pharmaceutics · 2022Review
- Enhanced pharmacokinetic performance of dapoxetine hydrochloride via the formulation of instantly-dissolving buccal films with acidic pH modifier and hydrophilic cyclodextrin: Factorial analysis,Journal of advanced research · 2020Article
- Development of Fast-Dissolving Amorphous Solid Dispersion of Itraconazole by Melt Extrusion of its Mixture with Weak Organic Carboxylic Acid and Polymer.Pharmaceutical research · 2018Article
- Effect of ionization of drug on drug solubilization in SMEDDS prepared using Capmul MCM and caprylic acid.Asian journal of pharmaceutical sciences · 2017Article
- Characterization of Solid Dispersion of Itraconazole Prepared by Solubilization in Concentrated Aqueous Solutions of Weak Organic Acids and Drying.Pharmaceutical research · 2016Article
- Biodegradable Elastomers with Antioxidant and Retinoid-like Properties.ACS biomaterials science & engineering · 2016Article
- Hydroxypropyl-β-cyclodextrin functionalized calcium carbonate microparticles as a potential carrier for enhancing oral delivery of water-insoluble drugs.International journal of nanomedicine · 2015Article
Corrections and comments
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Authors and funding
7 authors at 3 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
purposeTo present a novel approach of greatly enhancing aqueous solubility of a model weakly basic drug, haloperidol, by using weak acids that would not form salts with the drug and to attain physically stable form of amorphous drug by drying such aqueous solutions.
methodAqueous solubility of haloperidol in presence of increasing concentrations of four different weak organic acids (malic, tartaric, citric, fumaric) were determined. Several concentrated aqueous solutions with differing drug-to-acid molar ratios were dried in vacuum oven, and dried materials were characterized by DSC, powder XRD, dissolution testing, and stability study.
resultAcids were selected such that they would not form salts with haloperidol. Haloperidol solubility increased greatly with increased concentrations of malic, tartaric and citric acids, reaching >300 mg/g of solution. In contrast to the haloperidol HCl aqueous solubility of 4 mg/g, this may be called supersolubilization. Fumaric acid did not cause such solubilization as it had low water solubility. Dried solids formed dispersions of amorphous haloperidol in acids that were either amorphous or partially crystalline. Amorphous haloperidol was physically stable and had better dissolution rate than HCl salt.
conclusionA novel method of drug solubilization in aqueous media by acid-base interaction is presented. Physically stable amorphous systems of drugs may also be prepared by using this organic solvent-free approach.
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