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.
The 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 MoreThe main purpose of the paper is to identify the controllability of an existing production system; yogurt production line in Abu Ghraib Dairy Factory which has several machines of food processing and packing that has been studied. Through the starting of analysis, instability in production has been found in the factory. The analysis is built depending on experimental observation and data collection for different processing time of the machines, and statistical analysis has been conducted to model the production system. Arena Software is applied for simulating and analyzing the current state of the production system, and results are expanded to improve the system production and efficiency. Research method is applied to contribute in knowi
... 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 MoreBackground: 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 MoreThe aim of present study was to develop gel formulation of microsponges of poorly soluble drug meloxicam (MLX) in order to enhance the release and dissolution of MLX which is the limitation for preparation in topical forms. Also skin delivery is an alternative administration for MLX that can minimize gastrointestinal (GI) side effects and improve patient compliance. The microsponges of MLX were prepared by quasi-emulsion solvent diffusion method. The effects of drug:polymer ratio, stirring time and Eudragit polymer type on the physical characteristics of microsponges were investigated and characterized for production yield, loading efficiency, particle size, surface morphology, and in vitro drug release from microsponges. The selec
... 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
... Show MorePolyvinal alcohol was Cynoethylated , complex compound with Iodin in presence of Cu++ ions were preparated and their ultra violet (U.V) and infra red( IR) spectra were investigated. The prepared derivative and complexes were evaluated as antibacterial and antifungal agents following the standard dilution method. MIC(minimum inhibitory concentration) for each polymer using ten types of gram + ve and gram _ ve bacteria were determinated in addition to three types of fungi. The results obtainded showed that MIC, s were around 0.0011 × 103 molar for different polymetric derivatives tried.