The effect of chloride ion (Cl-) on dissolution rates of hydrochloride, mesylate (methanesulfonate) and phosphate salt forms of a model drug, haloperidol, was investigated. The dissolution rates of the salts in 0.01 M HCl from rotating disks followed the order of mesylate>phosphate>hydrochloride. With additional chloride ion, a decrease in dissolution rate of the hydrochloride salt was observed due to the common ion effect. Dissolution rates of mesylate and phosphate salts also decreased due to their conversion to the HCl salt form on the surfaces of dissolving disks, however, the dissolution rates of mesylate and phosphate salts under identical chloride ion concentrations were still higher than that of the HCl salt. In powder dissolution studies, it was observed that kinetics of nonhydrochloride-to-hydrochloride salt conversion play a major role in dissolution; the mesylate dissolved completely (<5 min) before its dissolution rate could be impeded by its conversion to the hydrochloride salt form. Therefore, despite the potential for conversion to a hydrochloride salt form, certain nonhydrochloride salt forms may still be preferred for dosage form development due to kinetic advantages during dissolution, such as higher apparent...Continue Reading
Effect of diffusion layer pH and solubility on the dissolution rate of pharmaceutical bases and their hydrochloride salts. I: Phenazopyridine
Preformulation investigation. I. Relation of salt forms and biological activity of an experimental antihypertensive
Investigation of solubility and dissolution of a free base and two different salt forms as a function of pH
Miniaturized rotating disk intrinsic dissolution rate measurement: effects of buffer capacity in comparisons to traditional wood's apparatus
Multivariate data analysis of factors affecting the in vitro dissolution rate and the apparent solubility for a model basic drug substance in aqueous media
Solution-mediated phase transformation of haloperidol mesylate in the presence of sodium lauryl sulfate
Optimization of salting-out taste-masking system for micro-beads containing drugs with high solubility
Solution-mediated phase transformation: significance during dissolution and implications for bioavailability
In Vivo Predictive Dissolution: Comparing the Effect of Bicarbonate and Phosphate Buffer on the Dissolution of Weak Acids and Weak Bases
Surfactant-mediated dissolution of metformin hydrochloride tablets: wetting effects versus ion pairs diffusivity
Solution-mediated phase transformation of salts during dissolution: investigation using haloperidol as a model drug
Characterization of Solid Dispersion of Itraconazole Prepared by Solubilization in Concentrated Aqueous Solutions of Weak Organic Acids and Drying
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Continuous Preparation of 1:1 Haloperidol-Maleic Acid Salt by a Novel Solvent-Free Method Using a Twin Screw Melt Extruder
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Ionizable Drug Self-Associations and the Solubility Dependence on pH: Detection of Aggregates in Saturated Solutions Using Mass Spectrometry (ESI-Q-TOF-MS/MS).
Modifying the diffusion layer of soluble salts of poorly soluble basic drugs to improve dissolution performance
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