The discovery of novel therapeutic molecules is always difficult, and there are a variety of methodologies that use the most diverse and innovative medicinal chemistry approaches. One such approach is the deuteration technique: Deuteration is the process of substituting deuterium for hydrogen in a molecule. When compared to the drug molecule, its deuterated analogues may retain the features of the original molecule and, in some cases, improve its pharmacological activity, with fewer side effects and lower toxicity. Metronidazole is a commonly used antibiotic to treat anaerobic bacterial infections, protozoal and microaerophilic bacterial infections. Metronidazole has a half-life of 6.5 ± 2.9 hours. A number of studies have recently been conducted on the selective substitution of hydrogen with deuterium. which increases the bond strength, increasing the biological half-life and, consequently, the drug's metabolic stability also increases. In an attempt to address metronidazole's drawbacks and clinical resistance, deuterated metronidazole was synthesised, characterised, and tested for antibacterial, antifungal, and anti-tubercular activities. The metronidazole and its deuterated compound showed equipotent antifungal activity and aerobic antibacterial activity. Also, when compared with the non-deuterated compound, deuterated metronidazole exhibited better anaerobic antibacterial and anti-tubercular activity.
Background: Bilastine (BLA) is a second-generation H1 antihistamine used to treat allergic rhinoconjunctivitis. Because of its limited solubility, it falls under class II of the Biopharmaceutics Classification System (BSC). The solid dispersion (SD) approach significantly improves the solubility and dissolution rate of insoluble medicines. Objective: To improve BLA solubility and dissolution rate by formulating a solid dispersion in the form of effervescent granules. Methods: To create BLA SDs, polyvinylpyrrolidone (PVP K30) and poloxamer 188 (PLX188) were mixed in various ratios (1:5, 1:10, and 1:15) using the kneading technique. All formulations were evaluated based on percent yield, drug content, and saturation solubility. The fo
... Show MoreOral jelly is a semisolid preparation that could resolve problem associated withdosage form’s swallowing, especially in pediatric and elderly ones. This work aimedto prepare oral flurbiprofen (FBP) jelly to improve patient compliance. Heating andcongealing method was used to prepare FBP jelly using three different polymers (pectin,sodium carboxymethyl cellulose, and hydroxypropyl methylcellulose). The effect ofdifferent concentrations of pectin and sucrose on jelly properties was studied. Theresults revealed that both pectin and sodium carboxymethyl cellulose polymers gaveacceptable jelly appearance and consistency. It was also observed that the increase ofpectin or sucrose concentration had a significant impact on jelly viscosity. All pe
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The effective surface area of drug particle is increased by a reduction in the particle size. Since dissolution takes place at the surface of the solute, the larger the surface area, the further rapid is the rate of drug dissolution. Ketoprofen is class II type drug according to (Biopharmaceutics Classification System BCS) with low solubility and high permeability. The aim of this investigation was to increase the solubility and hence the dissolution rate by the preparation of ketoprofen nanosuspension using solvent evaporation method. Materials like PVP K30, poloxamer 188, HPMC E5, HPMC E15, HPMC E50, Tween 80 were used as stabilizers in perpetration of differ
... Show MoreThe present work provides to treat real oily saline wastewater released from drilling oil sites by the use of electrocoagulation technique. Aluminum tubes were utilized as electrodes in a concentric manner to minimize the concentrations of 113400 mg TDS/L, 65623 mg TSS/L, and the ions of 477 mg HCO3/L, 102000 mg Cl/L and 5600 mg Ca/L presented in real oily wastewater under the effect of the operational parameters (the applied current and reaction time) by making use of the central composite rotatable design. The final concentrations of TDS, TSS, HCO3, Cl, and Ca that obtained were 93555 ppm (17.50%), 11011 ppm (83.22%), 189ppm (60.38%), 80000ppm (22%), and 4200 ppm (25%), respectively, under the optimum values of the operational parameters
... Show MoreClotrimazole (CLO) is an antimycotic imidazole derivative applied locally for the treatment of vaginal yeast infections. In this study, CLO was formulated as vaginal mucoadhesive hydrogel, using different types of mucoadhesive polymers to ensure prolonged contact between active ingredient and vaginal mucosa.
Physicochemical properties of the prepared formulas were evaluated as a visual inspection, pH, swelling index, spreadability, and mucoadhesive characteristics, in addition to an in-vitro drug release. The influence of type and concentration of polymers as CMC-Na (1.5, 2.5, and 3.5%w/w), carbopol 940( 0.25, 0.5, and 1 %w/w) and poloxamer 407 (15, 25, 30%w/w) on CLO release from the prepared gels were also invest
... Show MoreOndansetron HCl (OND) is a potent antiemetic drug used for control of nausea and vomiting associated with cancer chemotherapy. It exhibits only 60 – 70 % of oral bioavailability due to first pass metabolism and has a relative short half-life of 3-5 hours. Poor bioavailability not only leads to the frequent dosing but also shows very poor patient adherence. Hence, in the present study an approach has been made to develop OND nanoparticles using eudragit® RS100 and eudragit® RL100 polymer to control release of OND for transdermal delivery and to improve patient compliance.
Six formulas of OND nanoparticles were prepared using nanoprecipitation technique. The particles sizes and zeta potential were measured
... Show MoreIn this article, Pb2Ba1.7Sr0.3Ca2Cu3O10+δ superconductor material was synthesized using conventional solid-state reaction method. X-ray diffraction (XRD) analysis demonstrated one dominant phase 2223 and some impurities in the product powder. The strongest peaks in the XRD pattern were successfully indexed assuming a pseudo-tetragonal cell with lattice constants of a = 3.732, b = 3.733 and c = 14.75 Å for a Pb-Based compound. The crystallite size and lattice strain between the layers of the studied compound were estimated using several methods, namely the Scherrer, Williamson-Hall (W.H), sizestrain plot (SSP) and Halder Wagner (H.W) approach. The values of crystallite size, calculated by Scherrer, W.H, SSP and H.W methods, were 89.454077
... Show MoreThis study discussed the effects of doping with silver (Ag) on the optical and structural properties of
CdO nanoparticles at different concentrations 0, 1, 2, 3, 4, 5 wt% prepared by the precipitation method. The
materials were annealed at 550˚C for 1 h. The structural, topographical, and optical properties were
diagnosed by X-ray diffraction analysis, atomic force instrument, and visible and ultraviolet spectrometers.
The results show that the average diameter of the grains depends on the percentage of added silver to the
material, as the diameter decreased from 88.8 to 59.7 nm, and it was found that the roughness increased from
5.56 to 26.5. When studying the optical properties, it was noted that th