Mefenamic acid (MA) is one of the non-steroidal anti-inflammatory drugs, it is widely used probably due to having both anti-inflammatory and analgesic activity, the main side effects of mefenamic acid include gastrointestinal tract (GIT) disturbance mainly diarrhea, peptic ulceration, and gastric bleeding. The analgesic effects of NSAIDs are probably linked to COX-2 inhibition, while COX-1 inhibition is the major cause of this classic adverse effects. Introduction of thiazolidinone may lead to the increase in the bulkiness leads to the preferential inhibition of COX-2 rather than COX-1 enzyme. The study aimed to synthesize derivatives of mefenamic acid with more potency and to decrease the drug's potential side effects, new series of 4-thiazolidinone derivatives of mefenamic acid were synthesized IVa-g. The synthetic procedures for target compounds and their intermediates are designed to be as follows: acylation of secondary amine of mefenamic acid by chloroacetylchloride to produce compound (I), then reaction between compound (I) and hydrazine hydrate to form hydrazine derivative of mefenamic acid (compound II). After that, Schiff base formation by addition of seven benzaldehyde derivatives and finally, cyclization in presence of thioglycolic acid to form 4-thiazolidinone heterocyclic ring. The characterization of the titled compounds has been established on the basis of their spectral FTIR, 1HNMR data, and by measurements of their physical properties. In vivo acute anti-inflammatory effect of the synthesized compounds was evaluated in rats using egg-white induced edema model of inflammation. The tested compounds and the reference drug produced significant reduction of paw edema with respect to the effect of dimethyl sulfoxide 10%v/v (control group). Compound IVe showed more potent effect than mefenamic acid at 240-300 min, while at time 300 min, compounds IVa and IVd exhibit more potent anti-inflammatory effect than mefenamic acid (50mg/kg, i.p.) as they reduced paw edema significantly more than mefenamic acid at mentioned intervals (p<0.05) . On the other hand compound IVc exhibited lower anti-inflammatory effect.
The preferred route of drug administration is the oral route, but drugs with narrow absorption window in the gastrointestinal tract are still challenging. The ability to extend and monitor the gastric emptying time is a valuable tool for processes remaining in the stomach longer than other traditional dosage forms.
The purpose of this study was to formulate and evaluate gastroretentive superporous hydrogel (SPH) of carvedilol with view to improve its solubility and increase gastric residence time in order to get sustained release formulas via utilization of various kinds and concentrations of hydrophilic polymers then after, incorporate the best prepared formula into capsules.
Sixteenth formulae of SPH h
... Show MoreThis study aims to encapsulate atenolol within floating alginate-ethylcellulose beads as an oral controlled-release delivery system using aqueous colloidal polymer dispersion (ACPD) method.To optimize drug entrapment efficiency and dissolution behavior of the prepared beads, different parameters of drug: polymer ratio, polymer mixture ratio, and gelling agent concentration were involved.The prepared beads were investigated with respect to their buoyancy, encapsulation efficiency, and dissolution behavior in the media: 0.1 N HCl (pH 1.2), acetate buffer (pH 4.6) and phosphate buffer (pH 6.8). The release kinetics and mechanism of the drug from the prepared beads was investigated.All prepare
... Show MoreMeloxicam (MLX) is non-steroidal anti -inflammatory, poorly water soluble, highly permeable drug and the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal tract. Solid dispersion (SD) is an effective technique for enhancing the solubility and dissolution rate of such drug.
The present study aims to enhance the solubility and the dissolution rate of MLX by SD technique by solvent evaporation method using sodium alginate (SA), hyaluronic acid (HA), collagen and xyloglucan (XG) as gastro-protective hydrophilic natural polymers.
Twelve formulas were prepared in different drug: polymer ratios and evaluated for their, percentage yield, drug content, water so
... Show MoreAbstract
The aim of this study was to prepare rebamipide ocular inserts in order to extend its release on the ocular surface for dry eye treatment. Solubility study was applied to the drug with or without l-arginine using different solvents. Solvent casting technique was used to prepare the inserts; l-arginine was used to solubilize the drug, hydroxypropyl methylcellulose grades (E5 and K15M) and poly ethylene glycol 200 were used as excipients. The inserts were evaluated for their physical and mechanical properties, moisture loss% and absorption %, surface pH, and in-vitro drug release. The use l-arginine exhibited an enhancement of rebamipide solubility in both deionized water and phosphate buffer (pH 7.4) by a
... Show MoreNonalcoholic fatty liver disease (NAFLD) is a common liver disease that ranges from simple steatosis to nonalcoholic steatohepatitis (NASH). So far, the underlying mechanism remains poorly understood. Here, we show that hepatic carboxylesterase 2 (CES2) is markedly reduced in NASH patients, diabetic
Specific microorganisms can produce bacterial nanocellulose (BNC), with acetic acid bacteria (AAB) being the most active producer. The family Acetobacteraceae includes the obligate aerobic, motile acetic acid bacteria. The BNC has attracted a lot of interest across a wide range of industries, including pharmaceuticals, due to its flexible characteristics, properties, and advantages. The present study was conducted to purify and characterize BNC produced from AAB isolated from apple vinegar. Bacterial nanocellulose was synthesized using a natural date palm liquid medium at pH 6 at 30°C for 8–10 days. The bacterial cellulose produced was then purified using a technique involving 0.1 M sodium hydroxide. To ascertain the surface mor
... Show MoreUsing an environmentally friendly chemical process, a novel nanocomposite consisting of reduced graphene oxide (rGO) and silver(I) oxide (Ag2O) nanoparticles was successfully synthesized in this work, and its optical properties along with photoelectric performance were investigated. Ag2O is a narrow-bandgap p-type semiconductor with strong visible light response but exhibits poor carrier separation and structural instability during exposure to radiation. In order to overcome shortcomings encountered with Ag2O, rGO was used as a conductive support to produce rGO@Ag2O nanocomposites with improved electronic interactions. Various characterization tests, including energy-dispersive X-ray spectroscopy (EDXS), field emission scanning electron mic
... Show MoreBy using vacuum evaporation, thin films of the (CdS)0.75-(PbS)0.25 alloy have been deposited to form a nanocrystalline composite. Investigations were made into the morphology, electrical, optical and I-V characteristics of (CdS)0.75-(PbS)0.25 films asdeposited and after annealing at various temperatures. According to AFM measurements, the values of grain sizes rise as annealing temperatures rise, showing that the films' crystallinity has been increased through heat treatment. In addition, heat treatment results in an increase in surface roughness values, suggesting rougher films that could be employed in more applications. The prepared films have direct energy band gaps, and these band gaps increase with the increase in the degrees
... Show MoreDue to the advantages over other metallic materials, such as superior corrosion resistance, excellent biocompatibility, and favorable mechanical properties, titanium, its alloys and related composites, are frequently utilized in biomedical applications, particularly in orthopedics and dentistry. This work focuses on developing novel titanium-titanium diboride (TiB2; ceramic material) composites for dental implants where TiB2 additions were estimated to be 9 wt.%. In a steel mold, Ti-TiB2 composites were fabricated using a powder metallurgy technique and sintered for five hours at 1200 °C. Microstructural and chemical properties were analyzed by energy dispersive X-ray spectroscopy (EDX), scanning electron microscopy (SEM), and X-ra
... Show More