Evaluation of Poorly Soluble Drugs’ Dissolution Rate by Laser Scattering in Different Water Isotopologues

Abstract

The most important task in the design of dosage forms is to modify the pharmaceutical substances structure in order to increase solubilization, targeted delivery, controlled rate of drug administration, and its bioavailability. Screening—laboratory (in vitro) or computer (in silico)—as a procedure for selecting a prototype for the design of a drug molecule, involves several years of research and significant costs. Among a large number of solvents and diluents (alcohol, ether, oils, glycerol, Vaseline) used in the pharmaceutical industry for the manufacture of drugs water finds the greatest application. This is because all biological reactions (reactions in living systems) take place in water and distribution of the fluid in the body and the substances found within is critical for the maintenance of intracellular and extracellular functions. Modern studies in the field of the stable isotopic compositions of natural water and its structure and properties make it possible to use isotopic transformations of the water to improve the pharmacokinetic properties of medicinal substances without previous structural modification. It is known that by replacing any of the atoms in the reacting substance molecule with its isotope, it is possible to record changes in the reactivity, which are expressed as a change in the reaction rate constant, i.e., in the manifestation of the kinetic isotope effect (KIE). The article presents the results of studies on the effect of the kinetic isotope effect of a solvent—water—on increasing the solubility and dissolution rate constants of poorly soluble drugs using laser diffraction spectroscopy. The results of the studies can be successfully implemented in pharmaceutical practice to overcome the poor solubility of medicinal substances of classes II and IV, according to the biopharmaceutical classification system (BCS), in water for pharmaceutical purposes by performing its preliminary and safe isotopic modification.

Optimization of Delivery and Bioavailability of Encapsulated Caffeic Acid

“…Given that most medicinal substances have poor solubility, researchers are looking for different solutions to this problem [42,43]. One of the most important factors is the ability of the solid form, administered orally, to dissolve in physiological body fluids and the therapeutic effect of the absorbed active substance [25,44]. Arivarasu et al described in their study that orally administered caffeic acid is an effective agent in reducing the intestinal effects of Cisplatin and may be useful in reducing the gastrointestinal toxicity of this drug [45].…”

Influence of Mechanical Loading on the Process of Tribochemical Action on Physicochemical and Biopharmaceutical Properties of Substances, Using Lacosamide as an Example: From Micronisation to Mechanical Activation

“…The SLS (LALLS) method was also used to study the kinetics of dissolution of the studied Lcs samples in water according to a previously developed method [ 36 ]. To do this, a sample of Lcs substance powder of about 0.03 g was placed in a cell with 3 mL of water.…”

Precipitation of aqueous transition metals in particulate matter during the dithiothreitol (DTT) oxidative potential assay

“…The particle number concentration was continuously measured using laser particle light scattering (Mastersizer 3000, Malvern Panalytical). [70][71][72][73][74][75][76] Monodispersed polystyrene latex (PSL) microspheres (0.5 mm) with 2.5 weight% dispersion in water were used to calibrate the instrument, laser obscuration (the parameter measured by the instrument) and particle number concentration (r 2 of 0.99, Fig. S2 †).…”