Etodolac is choice of drug for pain and inflammation but has major side effects of gastric ulcers that are due to free carboxylic group. Etodolac belongs to the chemical class of non-selective COX-inhibitor but preferentially COX-2 inhibitor. Here the ester linked mutual prodrugs of etodolac with phytophenols like vanillin, carvacrol, umbelliferone, guaiacol, sesamol and syringaldehyde were synthesized. All the prodrugs were characterized by IR-spectroscopy, 1H-NMR, 13C-NMR and mass spectrometry. Among the synthesized prodrugs, the Eto-van, Eto-umbe, Eto-sesa and Eto-syr showed improved analgesic and anti-inflammatory activity compared to etodolac. All the synthesized prodrugs showed less ulcerogenic side effects compared to etodolac.
“Orodispersible Tablet†a tablet that is to be placed in oral cavity where it disperses rapidly by saliva with no need for water before swallowing. Zaltoprofen (ZLP) is one of NSAIDs which is used in the treatment of rheumatoid arthritis and osteoarthritis as well as to relieve inflammation and pain after surgery, injury and tooth extraction. The present study was aimed to prepare rapidly dissolved lyophilized Zaltoprofen tablet with different pharmaceutical excipients and studying the factors affecting pharmaceutical properties like (solubility, disintegration time DT, dissolution, etc.) of tablets. The lyophilized disintegrating tablets (LDTs) were prepared using Zydis technique by lyophilization an aqueous
... Show MoreNystatin is the drug of choice for treatment of cutaneous fungal infections with main disadvantage that is the need for multiple applications to achieve complete eradication which may reduce patient compliance. Microparticles offer a solution for such issue as they are one of sustained release preparations that achieve slow release of drug over an extended period of time. The objectives of this study were to fabricate nystatin-loaded chitosan microparticles with the ultimate goal of prolonging drug release and to analyze the influence of polymer concentration on various properties of microparticles. Microparticles were prepared by chemical cross-linking method using glutaraldehyde as cross-linking agent. Five formulas, namely N1C1, N1C2,
... Show MoreBackground: Bilastine is a non-sedating, second-generation antihistamine used to treat urticaria and allergic conjunctivitis. Objective: to formulate and test bilastine as a mucoadhesive ophthalmic in situ gel in order to extend its presence at site for longer time and help treat conjunctivitis and allergic rhinitis. Methods: We prepared formulations using different concentrations of poloxamers (Poloxamer 407 (P407) and Poloxamer 188 (P188)) in combination with hydroxypropyl methyl cellulose (HPMC). The prepared formulas were evaluated for their physicochemical properties, sol-gel transition temperature, viscosity, mucoadhesive strength, drug release, and kinetic modeling. Results: The prepared in situ gels were clear and transparen
... Show MoreA series of Schiff base-bearing salicylaldehyde moiety compounds (1-4) had been designed, synthesized, subjected to insilico ADMET prediction, molecular docking, characterization by FT-IR, and CHNS analysis techniques, and finally to their Anti-inflammatory profile using cyclooxygenase fluorescence inhibitor screening assay methods along with standard drugs, celecoxib, and diclofenac. The ADMET studies were used to predict which compounds would be suitable for oral administration, as well as absorption sites, bioavailability, TPSA, and drug likeness. According to the results of ADME data, all of the produced chemicals can be absorbed through the GIT and have passed Lipinski’s rule of five. Through molecular docking with PyRx 0.8, these
... Show MoreThe diverse urban spaces of the streets is an important part of the city's physicist configuration and a link between architectural and civilizational communication through time starting from the historic towns down to the contemporary cities, within the proposals of the future cities. From general observations and literature review a research problem is crystallized as some directions not arbitrary rational when expansion and the growth of cities, and other measures wrong or the existence of some incorrect actions and processes related to the cities planning as a categorizing the goals and priorities in city plan.The streets were constitute a high proportion of the total area of cities, where up to over 30% in major cities. These
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The topological parameters of the metal-metal and metal-ligand bonding interactions in a trinuclear tetrahydrido cluster [(Cp*Co) (CpRu)2 (μ3-H) (μ-H)3]1 (Cp* = η5 -C5Me4Et), (Cp = η5 -C5Me5), was explored by using the Quantum Theory of Atoms-in-Molecules (QTAIM). The properties of bond critical points such as the bond delocalization indices δ (A, B), the electron density ρ(r), the local kinetic energy density G(r), the Laplacian of the electron density ∇2ρ(r), the local energy density H(r), the local potential energy density V(r) and ellipticity ε(r) are compared with data from earlier organometallic system studies. A comparison of the topological processes of different atom-atom interactions has become possible than
... Show MoreNine new compounds of 2-amino-5-chlorobenzothiazole derivatives were synthesized. These new compounds were formed through the reaction of 2-amino-5-chlorobenzothiazole 1 with ethyl chloroacetate and KOH, which gave an ester derivative 2, followed by refluxing compound 2 with hydrazine hydrate to afford hydrazide derivative 3. The reaction of compound 3 with CS2 and KOH gave 1,3,4-oxadiazole-2-thiol derivative 4, and then the reaction of compound 2 with thiosemicarbazide to produce compound 5 then treated it with 4%NaOH led to ring closure to provide 1,2,4-triazole-3-thiol derivative
... Show MoreThe energy density state are the powerful factor for evaluate the validity of a material in any application. This research focused on examining the electrical properties of the Se6Te4- xSbx glass semiconductor with x=1, 2 and 3, using the thermal evaporation technique. D.C electrical conductivity was used by determine the current, voltage and temperatures, where the electrical conductivity was studied as a function of temperature and the mechanical electrical conduction were determined in the different conduction regions (the extended and localized area and at the Fermi level). In addition, the density of the energy states in these regions is calculated using the mathematical equations. The constants of energy density states are det
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