Solvatomorphism of Moxidectin.

The solvatomorphism of the anthelmintic drug moxidectin is investigated, and a new solvatomorph with nitromethane is reported. Moreover, the hitherto unknown crystal structures of the solvatomorphs with ethanol and 2-propanol are reported and discussed. The thermal characterization of these solvatomorphs through variable-temperature powder X-ray diffraction analysis (VT-PXRD) is also described, providing new insights into the crystallochemistry of this active pharmaceutical ingredient.

Pulmonary embolism with migrating thrombus through patent foramen ovale: A case for a mixed pharmacological and percutaneous management.

A 61-year-old man, admitted to our hospital for bilateral pulmonary embolism, complicated by right renal ischemia and multiple splenic infarcts due to a mobile thrombus entrapped in a patent foramen ovale, has been successfully treated with apixaban 5 mg twice daily followed by transcatheter patent foramen ovale closure. < Apixaban could be a therapeutic alternative to thrombolysis and surgery in patients with warfarin-resistant thrombus straddling in the patent foramen ovale (PFO). Furthermore, apixaban could be a simple and useful option to manage patients undergoing transcatheter PFO closure.

Designing the Optimal Formulation for Biopharmaceuticals: A New Approach Combining Molecular Dynamics and Experiments.

Biopharmaceuticals are often stored in a lyophilized form. However, stresses due to both the freezing and the drying steps of the lyophilization process can be harmful to protein stability, and appropriate excipients must be added to minimize detrimental effects. In this work, molecular dynamics was used to provide insight into the mechanisms of protein stabilization by different osmolytes, using lactate dehydrogenase as model protein.

Targeting Transient Receptor Potential Vanilloid 1 (TRPV1) Channel Softly: The Discovery of Passerini Adducts as a Topical Treatment for Inflammatory Skin Disorders.

Despite being an old molecule, capsaicin is still a hot topic in the scientific community, and the development of new capsaicinoids is a promising pharmacological approach in the management of skin disorders related to inflammation and pruritus. Here we report the synthesis and the evaluation of capsaicin soft drugs that undergo deactivation by the hydrolyzing activity of skin esterases. The implanting of an ester group in the lipophilic moiety of capsaicinoids by the Passerini multicomponent reaction affords both agonists and antagonists that retain transient receptor potential vanilloid 1 channel (TRPV1) modulating activity and, at the same time, are susceptible to hydrolysis.

Evaluation of salivary surface tension in a cohort of young healthy adults.

Objective: To determine salivary pH, flow rate (FR) and surface tension (γs) in a cohort of 30 healthy young adults. To acquire cohort biological independent variables (age, gender, weight, height, medications, smoking, pathologies, and allergies) and to correlate them with pH, FR and γs obtained values. Evaluate the possible variation of the γs values during the time after the withdrawal and the influence of the operational abilities of the experimenting operators.

Improvement of a mixture experiment model relating the component proportions to the size of nanonized itraconazole particles in extemporary suspensions.

A paper by Foglio Bonda et al. published previously in this journal (2016, Vol. 83, pp.

Apixaban-Induced Resolution of A Massive Left Atrial and Appendage Thrombosis in a Very Elderly Patient.

A 86-year-old woman with first diagnosed atrial fibrillation (AF) underwent mitral valve annuloplasty 10 years before was admitted to our Unit due to congestive heart failure. Trans-thoracic echocardiogram (TTE) revealed a large fluctuant echogenic mass in the posterior wall of the left atrium. Trans-esophageal echo (TEE) showed the origin of the mass within the left atrial appendage.

Salivary flow rate and pH in patients with oral pathologies.

Objective: Determine salivary pH and flow rate (FR) in a sample of 164 patients who came to Oral Pathology ambulatory, 84 suffering from oral lesions and 80 without oral lesions. Another aim was to evaluate factors that influence salivary flow rate.

Patients And Methods: Subjects underwent clinical examination and completed an anamnestic questionnaire in order to obtain useful information that was used to classify participants in different groups.

Microencapsulated bitter compounds (from reduce daily energy intakes in humans.

Mounting evidence showed that bitter-tasting compounds modulate eating behaviour through bitter taste receptors in the gastrointestinal tract. This study aimed at evaluating the influence of microencapsulated bitter compounds on human appetite and energy intakes. A microencapsulated bitter ingredient (EBI) with a core of bitter root extract and a coating of ethylcellulose-stearate was developed and included in a vanilla microencapsulated bitter ingredient-enriched pudding (EBIP).

Formulation and Coating of Alginate and Alginate-Hydroxypropylcellulose Pellets Containing Ranolazine.

The formulation and the coating composition of biopolymeric pellets containing ranolazine were studied to improve their technological and biopharmaceutical properties. Eudragit L100 (EU L100) and Eudragit L30 D-55-coated alginate and alginate-hydroxypropylcellulose (HPC) pellets were prepared by ionotropic gelation using 3 concentrations of HPC (0.50%, 0.

Calcium Alginate and Calcium Alginate-Chitosan Beads Containing Celecoxib Solubilized in a Self-Emulsifying Phase.

In this work alginate and alginate-chitosan beads containing celecoxib solubilized into a self-emulsifying phase were developed in order to obtain a drug delivery system for oral administration, able to delay the drug release in acidic environment and to promote it in the intestinal compartment. The rationale of this work was linked to the desire to improve celecoxib therapeutic effectiveness reducing its gastric adverse effects and to favor its use in the prophylaxis of colon cancer and as adjuvant in the therapy of familial polyposis. The systems were prepared by ionotropic gelation using needles with different diameters (400 and 600 μm).

Preparation of multiparticulate systems for oral delivery of a micronized or nanosized poorly soluble drug.

The purpose of the present work was to prepare multiparticulate drug delivery systems for oral administration of a poorly soluble drug such as itraconazole. Multiparticulate systems were prepared by extrusion/spheronization technique using a mix of crospovidone, low viscosity hypromellose, microcrystalline cellulose, micronized drug and water. In order to improve the release performance of the multiparticulate systems, the micronized drug was suspended in water with polysorbate 20 and nanonized by a high-pressure homogenization.

Nanonized itraconazole powders for extemporary oral suspensions: Role of formulation components studied by a mixture design.

Itraconazole (ITZ) nanocrystal-containing powders were prepared through the combined use of high pressure homogenization (HPH) and spray drying (SD). These powders were intended as base materials for the preparation of extemporary oral suspensions of the drug. The role and the effect of stabilizers on the size of re-dispersed particles were studied using a mixture design and a Scheffé model relating the dried nanosuspension composition to the mean particle diameters.

Self-emulsifying excipient platform for improving technological properties of alginate-hydroxypropylcellulose pellets.

In this work, alginate, alginate-pectin and alginate-hydroxypropylcellulose pellets were produced by ionotropic gelation and characterized. Ibuprofen was selected as model drug; it was suspended in the polymeric solution in crystalline form or dissolved in a self-emulsifying phase and then dispersed into the polymeric solution. The self-emulsifying excipient platform composed of Labrasol (PEG-8 caprylic/capric glycerides) and d-α-tocopherol polyethylene glycol 1000 succinate (TPGS), able to solubilize the drug was used to improve the technological and biopharmaceutical properties of the alginate pellets.

Determination of breath alcohol value after using mouthwashes containing ethanol in healthy young adults.

Objective: To evaluate breath alcohol value and blood alcohol concentration after using mouthwashes containing ethanol in a panel of healthy young adults. To determine zeroing time of these values and if subjects' body mass index or gender influenced it. Breathalyzer test is a practice performed to detect alcohol-impaired-drivers that can be penalized.

Kinematic viscosity of unstimulated whole saliva in healthy young adults.

Objective: To analyze kinematic viscosity and pH of unstimulated whole saliva, evaluate possible variations after sampling, identify any gender differences and detect possible correlations between them.

Subjects And Methods: The sample consisted of sixty-four healthy young adults (37 females and 27 males, mean age 25.2 years).

Polymorphism and kinetic behavior of binary mixtures of triglycerides.

The work is aimed at investigating the polymorphism and the phase transition kinetics of binary lipid mixtures with potential application in controlled drug delivery. The lipid systems, constituted of glyceryl tristearate (GTS) added with different amounts (1.0-7.

Formulation and characterization study of itraconazole-loaded microparticles.

The aim of the work was to realize itraconazole-loaded formulations in form of microparticles using a fast, simple and solvent free production procedure. The selected excipients were able to enhance wettability of the final product, to increase drug dissolution rate and to maintain drug in solution thanks to the formation of an emulsified system after contact with the gastrointestinal fluids. Itraconazole formulations contained a structuring lipid, a solubilizing agent and a surface active substance and were prepared by a hot melt method (MMS, melting-milling-sieving).

Daily and annually variation of unstimulated whole saliva flow rate and pH and their relation with body profile in healthy young adults.

Aim: To analyse pH and flow rate (FR) of unstimulated whole saliva (UWS), detecting their possible correlations both among themselves and with body profile; in addition to identify daily, annually and gender differences.

Materials And Methods: Eighty-one (47 ♀; 34 ♂) healthy young adults (mean age 22.7±4.

A novel dense CO(2) supercritical fluid technology for the development of microparticulate delivery systems containing ketoprofen.

VarioSol® is an innovative, solvent-free technology able to produce microparticles exploiting near-critical CO(2) properties as spraying and cooling agent. The aim of the present work was to evaluate the feasibility to produce in a single processing step by VarioSol® technology, oral ketoprofen-loaded microparticles with gastro-protective properties. The obtained products were powders composed of regular in shape and small in diameter microparticles, characterized by high drug content (40%) and good flow properties.

Quinidine for Pharmacological Cardioversion of Long-lasting Atrial Fibrillation.

In the daily clinical practice, patients with atrial fibrillation (AF) lasting more than 48h (or not datable at all) are not uncommon. In long-lasting AF changes in electrophysiological features (electrical remodeling) can occur, resulting in a loss of sensibility to most antiarrhythmic drugs. There is strong evidence that the main mechanism involved in electrical remodeling is a global shortening in refractory period.

Carboplatin-induced Kounis syndrome.

A 50-year-old man in chemotherapy for an advanced lung adenocarcinoma presented with chest pain and cutaneous rash during carboplatin infusion with electrocardiographic (ECG) evidence of an inferior lesion wave. The administration of steroids and nitrates promptly resulted in clinical and ECG normalization, without enzymatic dismission. This reaction was considered compatible with allergic coronary vasospasm (also known as Kounis syndrome), a rare but possible complication of chemotherapy.

Thermogravimetric investigation of the hydration behaviour of hydrophilic matrices.

This article proposes thermogravimetric analysis (TGA) as a useful method to investigate the hydration behaviour of hydrophilic matrix tablets containing hydroxypropylmethylcellulose (HPMC), sodium carboxymethylcellulose (NaCMC) or a mixture of these two polymers and four drugs with different solubility. The hydration behaviour of matrix systems was studied as a function of the formulation composition and of the dissolution medium pH. TGA results suggest that the hydration of matrices containing HPMC is pH-independent and not affected by the characteristics of the loaded drug; this confirms HPMC as a good polymer to formulate controlled drug delivery systems.

Difficulties in the production of identical drug products from a pharmaceutical technology viewpoint.

Generic products reduce healthcare expenditure and create market competition, and it is broadly assumed that these drugs are identical to the original branded reference drug product. In practice, despite legislation demanding demonstration of pharmaceutical equivalence and bioequivalence, thereby ensuring the safety and efficacy of the product, generic products can differ significantly from the reference drug and amongst themselves, particularly in terms of pharmacokinetic properties. These differences most often relate to pharmaceutical technical differences in production of the active principle ingredient (e.

Empirical kinetic model of propafenone release from Hot Air Coating microparticles.

Lipid microparticles, containing 30% and 50% (w/w) propafenone hydrochloride as the active molecule and cetearyl alcohol and Pluronic F68 as excipients, were prepared by Hot Air Coating (HAC). The aim of the work was to identify the kinetics and the mechanism of the drug release process from these microparticulate systems. The application of the Weibull model to the release data from each single fraction of microparticles suggests that a diffusive mechanism governs drug release from microparticles.