Solubility of pharmaceuticals in water and alcohols

Pobudkowska, Aneta; Domańska, Urszula; Jurkowska, Barbara A.; Dymczuk, Katarzyna

doi:10.1016/j.fluid.2015.02.018

Cited by 14 publications

(7 citation statements)

References 35 publications

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“…23 Again, each value was considered to be significantly higher compared to previous studies. Pobudkowska [26][27][28] In the studies without a given temperature or ionic strength; the temperature was 298.5 K and the ionic strength 0.020M. 19…”

Section: Bates-schwarzenbach Methodsmentioning

confidence: 99%

Recent Advancements in Spectrophotometric pKa Determinations: A Review

Berkhout

2019

IJPER

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The pKa value is a key feature in Absorption, Distribution, Metabolism and Excretion (ADME) of drugs, thus knowing this value is critical in drug development. In this review, pKa values determined in the past decade, using UV-Vis spectrometry, are discussed. To determine the pKa, four methods were applied; Henderson-Hasselbach, Albert-Serjeant, Bates-Schwarzenbach and Spectrometric titrations. This review will show the value of this aged but well-established technique in the past decade, due to its simplicity, accuracy, cost efficiency and reproducibility.

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Section: Bates-schwarzenbach Methodsmentioning

confidence: 99%

Recent Advancements in Spectrophotometric pKa Determinations: A Review

Berkhout

2019

IJPER

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“…Solid–liquid equilibria (SLE) of the studied systems were performed at 0.1 MPa and at a temperature range from 279.98 to 417.05 K, using a dynamic method. − The solutions containing the ionic liquids and TB drugs (presented in Table ) were weighted with an accuracy of 10 –4 g and placed into a Pyrex glass cell which was capped with a Teflon valve at the end of a capillary-thin (inner diameter of 0.1 mm) neck. The cell was placed in a temperature-controlled bath with water (293–333 K) with 10% methanol (267–293 K) or silicon (333–416 K).…”

Section: Experimental Proceduresmentioning

confidence: 99%

Solubility Data as a Response for a Challenge for Formulation Chemists: Imidazolium-Based Ionic Liquids and Antitubercular Antibiotic Medicines

et al. 2016

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The evolution of technology is directed to reduce industrial waste from chemical processes to zero. In the past decade interest in ionic liquids (ILs) has grown, and they have been recognized as potential substitutes for volatile organic solvents used in certain chemical processes, including those in the pharmaceutical industry. Following this increasing interest and because ILs can have a great potential for the pharmaceutical industry, we tested the solubility of two antitubercular medicines, pyrazinecarboxamide and isoniazid, in imidazolium ionic liquids, namely [C4mim][BF4], [C4mim][PF6], [C4mim][OTf], and [C8mim][OTf], in the range of 279.98 to 417.05 K. Both drugs exhibited an improved solubility in [C4mim][BF4] than in the other studied ILs. The solutes had an enhanced solubility in more hydrophilic ILs, such as [C4mim][BF4] and [C4mim][PF6]. The solubility decreased in ILs containing the hydrophobic anion trifluoromethanesulfonate and with the increasing alkyl chain length in the cation. The solid–liquid phase equilibria of all investigated systems were described using six different correlation equations. The satisfactory results which revealed a good description with an acceptable standard deviation temperature range were collected for isoniazid or pyrazinecarboxamide in [C4mim][PF6], [C4mim][OTf] and [C8mim][OTf]. Comparison to solubility in NTf2 and [C10mim][OTf] was provided.

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“…The models have been used to determine the solubility of e.g. flurbiprofen [8], octopamine HCl [9], synephrine [10], lobeline HCl [12], methyl xanthines [13], protein kinase CK2 inhibitors [14] or derivatives of anthranilic acid [15]. According to local concentration theory, the average concentrations of the substances described at the molecular level are differentiated.…”

Section: Modellingmentioning

confidence: 99%

Physicochemical Properties and Solubility of Hydrochloride Mucolytic Agents

2021

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Two widely used active pharmaceutical ingredients (API), ambroxol hydrochloride (AMB·HCl) and bromhexine hydrochloride (BMH·HCl), belong to the expectorant and mucokinetic group of drugs. Their applications are found in the treatment of the upper respiratory tract and bronchopulmonary diseases. The compounds have similar chemical structures, but are different enough to distinguish their physicochemical properties. To understand better the bioavailability of the drugs a series of experiments was performed to establish significant parameters. With differential scanning calorimetry (DSC) the temperature and the enthalpy of fusion were determined with no observed polymorphic transformations. The phase diagrams for binary systems {active agent (1) + solvent (2)} were determined with three solvents: 1-octanol, water and ethanol, to describe phase equilibria by correlation with the local composition models: Wilson, UNIQUAC and NRTL. Finally, the Bates–Schwarzenbach method was used to establish the ionization constants of AMB·HCl and BMH·HCl at two temperatures: room temperature 298.2 K and human body temperature 310.2 K. Our study can give an insight into further drug delivery system design and help to create more effective drug application forms.

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Solubility of pharmaceuticals in water and alcohols

Cited by 14 publications

References 35 publications

Recent Advancements in Spectrophotometric pKa Determinations: A Review

Recent Advancements in Spectrophotometric pKa Determinations: A Review

Solubility Data as a Response for a Challenge for Formulation Chemists: Imidazolium-Based Ionic Liquids and Antitubercular Antibiotic Medicines

Physicochemical Properties and Solubility of Hydrochloride Mucolytic Agents

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