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 co

Oral 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

Polyvinal 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.

With the aim of developing potential antimicrobials, a series of new 5-fluoroisatin derivatives incorporated with different secondary amines (piperidine, morpholine, pyrrolidine, dimethylamine, and diphenylamine) for monomer, and (piperazine) in case of dimer Mannich bases, separately in presence of formaldehyde to obtain Mannich bases of 5-fluoroisatin derivatives, which then each Mannich derivatives reacts with phenylhydrazine to form Schiff bases as final products. The resulting compounds were characterized by two spectroscopic analyses; (Fourier- transform infrared) FT-IR and proton nuclear magnetic resonance spectroscopy (¹H-NMR). In addition, the in vitro antibacterial and antifungal activities were tested against some human pathogen

Objective: Carbamazepine is typically used for the treatment of seizure disorders and neuropathic pain. One of the major problems with this drug is its low solubility in water; therefore the objective of this study was to enhance the solubility of carbamazepine by complexation with cyclodextrin to be formulated as effervescent and dispersible granules.Methods: Solvent evaporation method was used to prepare, binary (Carbamazepine/β-cyclodextrin) complex and ternary (Carbamazepine/β-cyclodextrin/hydroxypropyl methyl cellulose (HPMC E5). The more soluble complex will be further formulated as unit dose effervescent and dispersible granules. The complexes were evaluated for their solubility, drug content, percentage practical yield and

Zerumbone is a well-known compound having anti-cancer, anti-ulcer, anti-inflammatory and anti-hyperglycemic effects. During its use for the disease treatment, the membrane of erythrocyte can be affected by consumption of this bioactive compound. The current study was the first report of investigation of the hemolytic activities on human erythrocytes and cytotoxic profile of zerumbone. The toxicity of zerumbone on human erythrocytes was determined by in vitro hemolytic assay. Brine shrimp lethality assay was used to evaluate the cytotoxic effect of zerumbone at concentrations 10, 100 and 1000 μg/mL. The human erythrocyte test showed no significant toxicity at low concentrations, whereas hemolytic effect was amplified up to 17.5 % at

S Khalifa E, AM Sabeeh A, AN Adil A, AW Ghassan H…, 2007

A series of benzohydrazide derivatives attached to coumarin moiety at position 6 and 7 have been synthesized. The reaction of coumarin derivatives (coumarin I and II) with p-nitrophenyl hydrazine yield Schiff bases (compound1a and IIa_).These Schiff bases were refluxed with benzoyl chloride to give benzohydrazide derivatives of coumarin substituted at its 6 or 7 nucleus position (Ia₁ and IIa₁).The reaction and the purity of the products were checked by thin layer chromatography (TLC). The structures of the final compounds  and  their intermediates were confirmed by their melting points, infra red spectroscopy, and elemental microanalysis(CHN).

Compounds (Ia1 and IIa1) were evaluated for&n