Mebendazolium mesylate anhydride salt: rational design based on supramolecular assembly, synthesis, and solid-state characterization.

The design mebendazole (MBZ) multicomponent systems is important to obtain new materials that incorporate the API (active pharmaceutical ingredient) with better thermal stability, avoiding the interconversion of desmotropes. Interestingly, the presence of water molecules in the mebendazolium mesylate monohydrate prevents the formation of the (8) supramolecular synthon, found in all mebendazolium salts with polyatomic counterions. Here, we designed a new mebendazolium mesylate anhydrous salt based on statistical scrutiny of all mebendazole crystal structures identified in the literature and an exhaustive analysis of the conformational and geometrical requirements for the supramolecular assembly.

Crystalline and amorphous famotidine malate as pathways to prevent polymorphic transformation with improved dissolution.

Famotidine (FMT) is an orally administered histamine H2-receptor blocker with limited bioavailability since it exhibits low solubility and low permeability. In addition, the recent withdrawal of ranitidine from the market, makes famotidine an interesting candidate to obtain solid forms with improved pharmacokinetic performance. In this work, crystal engineering concepts and the co-amorphous formation strategy were applied to obtain two novel solids.

Strategies for Improving the CO Adsorption Process of CPO-27-Mg through Thermal Treatment and Urea Functionalization.

In this work, the influence of degassing temperature and urea functionalization were investigated as ways to improve the CO adsorption performance of CPO-27-Mg. Through post-synthesis modification treatments, four samples with different degrees of urea functionalization were obtained, incorporating 10, 25, 50, and 100% of urea concerning the metal sites of the MOF. Alternatively, the influence of the degassing temperature of the non-functionalized MOF between 70 and 340 °C was also evaluated.

ROS-generating rare-earth coordination networks for photodynamic inactivation of .

Water-ethanol suspensions of 2D coordination network (CN) based on rare earth elements and mixed ligands were evaluated as reactive oxygen species (ROS) generators under UV light irradiation, in contact with a biomimetic substrate (tryptophan) or an O2(1Δg) quencher (1,3-diphenylisobenzofuran; 1,3-DPBF). A combination of bottom-up and top-down strategies was implemented in order to obtain nano-sized CN particles and the subsequent colloidal suspensions were also tested towards photodynamic inactivation of Candida albicans (C. albicans).

Synthesis, physicochemical characterisation and biological activity of anandamide/ɛ-polycaprolactone nanoparticles obtained by electrospraying.

Drug encapsulation in nanocarriers such as polymeric nanoparticles (Nps) may help to overcome the limitations associated with cannabinoids. In this study, the authors' work aimed to highlight the use of electrospraying techniques for the development of carrier Nps of anandamide (AEA), an endocannabinoid with attractive pharmacological effects but underestimated due to its unfavourable physicochemical and pharmacokinetic properties added to its undesirable effects at the level of the central nervous system. The authors characterised physicochemically and evaluated in vitro biological activity of anandamide/ɛ-polycaprolactone nanoparticles (Nps-AEA/PCL) obtained by electrospraying in epithelial cells of the human proximal tubule (HK2), to prove the utility of this method and to validate the biological effect of Nps-AEA/PCL.

Strong photoluminescence and sensing performance of nanosized CaLnNaWO (Ln = Sm,Eu) compounds obtained by the dry "top-down" grinding method.

Two lanthanide doped nanosystems CaLnNaWO (Ln = Eu, Sm), denoted as Eu@CWO and Sm@CWO, were prepared by a "top-down" approach in three simple steps: activation, miniaturization by high-energy milling, and further calcination. The solids were thoroughly characterized by X-ray powder diffraction (XRPD) and Scanning-electron microscopy (SEM). Also, analyses of the structure of the compounds and the impact of milling on the crystallite shape and size were carried out through Rietveld refinements.

Rational Design of a Famotidine-Ibuprofen Coamorphous System: An Experimental and Theoretical Study.

Famotidine (FMT) and ibuprofen (IBU) were used as model drugs to obtain coamorphous systems, where the guanidine moiety of the antacid and the carboxylic group of the nonsteroidal anti-inflammatory drug could potentially participate in H-bonds leading to a given structural motif. The systems were prepared in 3:7, 1:1, and 7:3 FMT and IBU molar ratios, respectively. The latter two became amorphous after 180 min of comilling.

Preparation and Physical Characterization of a Diclofenac-Ranitidine Co-precipitate for Improving the Dissolution of Diclofenac.

Mixing aqueous solutions of sodium diclofenac (DIC-Na) and ranitidine hydrochloride (RAN·HCl) afforded an off-white solid (DIC-RAN) that was investigated from the microscopic, thermal, diffractometric, spectroscopic, and functional (chemometrics-assisted dissolution) points of view. The solid has a 2:1 (DIC:RAN) molar ratio according to (1)H nuclear magnetic resonance spectroscopy. It is thermally stable, displaying a broad endothermic signal centered at 105°C in the thermogram, and its characteristic reflections in the powder X-ray diffractogram remained unchanged after a 3-month aging period.

Looking for the interactions between omeprazole and amoxicillin in a disordered phase. An experimental and theoretical study.

In this paper, co-grinding mixtures of omeprazole-amoxicillin trihydrate (CGM samples) and omeprazole-anhydrous amoxicillin (CGMa samples) at 3:7, 1:1 and 7:3 molar ratios, respectively, were studied with the aim of obtaining a co-amorphous system and determining the potential intermolecular interactions. These systems were fully characterized by differential scanning calorimetry (DSC), FT-infrared spectroscopy (FTIR), X-ray powder diffraction (PXRD), scanning electron microscopy (SEM) and solid state Nuclear Magnetic Resonance (ssNMR). The co-grinding process was not useful to get a co-amorphous system but it led to obtaining the 1:1 CGMa disordered phase.

Physicochemical characterization of 2-hydroxybenzophenone with β-cyclodextrin in solution and solid state.

The characterization of the inclusion complex between 2-hydroxybenzophenone (2OHBP) and β-cyclodextrin (βCD) in the solid state was performed using Fourier transform infrared spectroscopy (FTIR), powder X-ray diffractometry (PXRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA), and transmission electron microscopy (TEM). The apparent formation constant of the complex was determined by phase solubility diagrams and liquid chromatography (HPLC) at different temperatures. The formation of the inclusion complex induced slight shifts in the FTIR spectrum while by PXRD a new crystalline phase was observed.

Solid-state supramolecular synthesis based on the N-H…O heterosynthon: an approach to solve the polymorphism problem in famotidine.

Famotidine (FMT), a histamine H2 -receptor antagonist, is a drug commonly used in treatments of gastroesophageal diseases that presents solid-state polymorphism (A and B forms), the marketed form being the metastable polymorph B. A new stable salt was obtained by combination of FMT and maleic acid as coformer. FMT maleate (FMT-MLT) was prepared either by solvent evaporation or comilling methods.

Mebendazole mesylate monohydrate: a new route to improve the solubility of mebendazole polymorphs.

Mebendazole mesylate monohydrate, a new stable salt of mebendazole (MBZ), has been synthesized and fully characterized. It was obtained from recrystallization of MBZ forms A, B, or C in diverse solvents with the addition of methyl sulfonic acid solution. The crystal packing is first organized as a two-dimensional array consisting of rows of alternating MBZ molecules linked to columns of mesylate ions by hydrogen bonds.

Structure-directing and template roles of aromatic molecules in the self-assembly formation process of 3D holmium-succinate MOFs.

Two new holmium-succinate frameworks have been synthesized by hydrolysis in situ of the succinylsalicylic acid under different hydrothermal conditions. Compound 1, [Ho(2)(C(4)H(4)O(4))(3)(H(2)O)(2)]·0.33(C(7)H(6)O(3)), P ̅i space group, has a novel structure composed by 1D-SBUs consisting of [HoO(9)] chains of polyhedra linked by the succinate ligands giving a 3D framework.

Thermodynamic and kinetic control on the formation of two novel metal-organic frameworks based on the Er(III) ion and the asymmetric dimethylsuccinate ligand.

Two new layered polymeric frameworks have been synthesized under different hydrothermal conditions and characterized by single-crystal X-ray diffraction, thermal analysis, and variable temperature-Fourier Transform Infrared Spectroscopy (VT-FTIR). The compound I, with formula [Er(2)(dms)(3)(H(2)O)(4)], has a triclinic cell with parameters a = 5.8506 A, b = 9.

Reversible breaking and forming of metal-ligand coordination bonds: temperature-triggered single-crystal to single-crystal transformation in a metal-organic framework.

Yb(C(4)H(4)O(4))(1.5)] undergoes a temperature-triggered single-crystal to single-crystal transformation. Thermal X-ray single-crystal studies showed a reversibly orchestrated rearrangement of the atoms generated by the breaking/formation of coordination bonds, in which the stoichiometry of the compound remains unchanged.

Intermolecular contacts influencing the conformational and geometric features of the pharmaceutically preferred mebendazole polymorph C.

Mebendazole (MBZ) is a common benzimidazole anthelmintic that exists in three different polymorphic forms, A, B, and C. Polymorph C is the pharmaceutically preferred form due to its adequated aqueous solubility. No single crystal structure determinations depicting the nature of the crystal packing and molecular conformation and geometry have been performed on this compound.

Adsorption of citric acid from dilute aqueous solutions by hydroxyapatite.

The role of citric acid in the demineralization of dental enamel, which is mainly constituted by hydroxyapatite, is important for periodontal regeneration and in the conditioning of enamel or dentin for bonding restorative resins. The adsorption of citric acid from aqueous solutions onto synthetic hydroxyapatite at 278, 288, 298, and 308 K and pH 4.8 has been studied by means of UV spectroscopy.