The purpose of this research work is to synthesize conjugates of some NSAIDs with sulfamethoxazole as possible mutual prodrugs to overcome the local gastric irritation of NSAID with free carboxyl group by formation of ester linkage that supposed to remain intact in stomach and may hydrolyze in intestine chemically or enzymatically; in addition to that attempting to target the synthesized derivative to the colon by formation of azo group that undergo reduction only by colonic bacterial azo reductaze enzyme to liberate the parent compound to act locally (treatment of inflammation and infections in colon)
Theligand4-[5-(2-hydoxy-phenyl)- [1,3,4- thiadiazole-2- ylimino methyl]-1,5-dimethyl -2-phenyl-1,2-dihydro-pyrazol-3-one [HL1] is prepared and characterized. It is reacted with poly(vinyl chloride) (PVC) in THF to form the PVC-L compounds ,PVC-L interacted with ions of transition metals to form PVC-L-MII complexes .All prepared compounds are characterized by FTIR spectroscopy, u.v-visible spectroscopy, C.H.N.S. analysis and some of them by 1HNMR
This study involves the synthesis of a new class of silicon polymers, designated as P1-P7, derived from dichlorodimethylsilane (DCDMS) in combination with various organic compounds (Schiff bases prepared from different amines and appropriate aldehydes or ketones) [I-V] through condensation polymerization. The structures of all monomers and polymers were characterization by FTIR and 1HNMR spectroscopy (for some polymers). The results of thermogravimetric analysis (TGA) and differential scanning calorimetry DSC test show stable thermal behaviour. Polymers with a higher concentration of aromatic rings in their repeating structural units exhibited a higher temperature for weight loss, indicating increased thermal stability. Thermal meas
... Show MoreAlginate is one of the natural biopolymers that is widely used for drug formulations, combination of alginate with other polymers, such as gum acacia, pectin, and carrageenan can increase mechanical strength, therefore, can reduce leakage of the encapsulated active pharmaceutical ingredient from the polymer matrix. Interaction of alginate and these polymers can occur via intermolecular hydrogen bonds causing synergism, which is determined from the viscosity of polymer mixture.
Alginate was combined with gum acacia/pectin/carrageenan in different blending ratios (100:0, 75:25, 50:50, 25:75, and 0:100) with and without addition of CaCl2. The synergism effect is obtained from the design of experimental (DoE), and calculati
... Show MoreThe drug promethazine hydrochloride (PRZH) forms with rhodium (II) a colored chelate (?max = 472 nm) complex at (pH = 2.1) which is extractable with benzyl alcohol as organic solvent. Under the appropriate experimental conditions a calibration plot was set up from which some analytical parameter were derived and deduced by regression. Standard addition procedure was also adopted. It has been estimated that the concentration of the drug PRZH to be 24.89 mg per unit and 24.19 mg per unit for both calibrations. Under optimal conditions, the developed method has been achieved the following characteristics: LDR (30 – 150 µg ml-1 ) PRZH , RSD % ( 0.6 – 2.47 ) , sandell sensitivity( 0.0844 µg. cm -2 ) , LOD ( 1.66 µgml-1 ) , recovery
... Show MoreBackground: The treatment of schizophrenia typically involves the use of olanzapine (OLZ), a typical antipsychotic drug that has poor oral bioavailability due to its low solubility and first-pass effect. Objective: To prepare and optimize OLZ as nanoparticles for transdermal delivery to avoid problems with oral administration. Methods: The nanoprecipitation technique was applied for the preparation of eight OLZ nanoparticles by using different polymers with various ratios. Nanoparticles were evaluated using different methods, including particle size, polydispersity index (PDI), entrapment efficiency (EE%), zeta potential and an in vitro release study. The morphology was evaluated by a field emission scanning electron microscope (F
... 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 MoreOn the basis of known coumarin-based prodrug system, a novel coumarin-based mutual prodrug of 5-fluorouracil and dichloroacetic acid was designed, synthesized and evaluated as a promising oral chemotherapeutic agent basing on in vitro stability study in HCl buffer (pH 1.2) and in phosphate buffer (pH 7.4), as well as in vitro release study in human serum. The chemical structure of prodrug was confirmed by analyzing its FTIR, 1H NMR, 13C NMR and MS-ESI spectra. The results of in vitro kinetic study indicated that the prodrug was significantly stable in HCl and in phosphate buffers, and was hydrolyzed in human serum followed pseudo first order kinetics.
Keywords: Coumarin-bas
... Show MoreBacterial infections pose an ongoing challenge due to resistance developed by infectious bacteria. So much research targeting designing new antibacterials is published annually. Our goal is to synthesize compounds that have given antibacterial activity according to molecular docking against the chosen target protein and that have acceptable ADMET properties that can be synthesized and used in the future. New 2-(5-methoxy-1-(4-chlorobenzene)-2-methyl-1H-indol-3-yl)acetohydrazide derivatives’ antibacterial efficacy against two common strains of Gram-negative and Gram-positive microorganisms has been developed, produced, and investigated. Sophisticated, modern analytical methods, including ATR-FTIR and 1H NMR spectroscopy, were used
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