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Formulation and Evaluation of Bilayer Tablets Containing Immediate Release Aspirin Layer and Floating Clopidogrel Layer
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Aspirin and clopidogrel are considered the most important oral platelets aggregation inhibitors. So it is widely used for treatment and prophylaxis of cardiovascular and peripheral vascular diseases related to platelets aggregation .In this study aspirin and clopidogrel were formulated together as floating bilayer tablet system. Three different formulas of 75 mg aspirin were prepared by wet granulation method as immediate release layer; different disintegrants used to achieve rapid disintegration. Formula with crosscarmellose as disintegrant achieve rapid disintegration was selected for preparation of bilayer tablet.

Different formulas of 75 mg clopidogrel were prepared as sustained release floating layer by wet granulation (effervescent ) method ;the physical and floating properties for compressed clopidogrel matrix were studied in addition to study the effect of polymer  concentration(HPMC) ,and its combination with ethyl cellulose and carbapol ,effect of different diluents and effect of increasing sodium bicarbonate amount on the release from compressed matrix .

Formula prepared with HPMC and EC in a ratio of 1:1 was capable to retard the release of clopidogrel for 6 hours in addition to its good floating behavior and therefore selected to prepare bilayer tablets in combination with selected aspirin layer.

The prepared bilayer tablets were further subjected to evaluation of their physical, floating properties and release behavior. Finally the kinetic study reflects acceptable shelf life for aspirin and clopidogrel.

Key words: Aspirin, Clopidogrel, Bilayer tablet, Floating tablet.

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Publication Date
Tue Mar 30 2021
Journal Name
Baghdad Science Journal
Synthesis, Characterization and Biological Activity Evaluation of Some Pyrazoles, Thiazoles and Oxazoles Derived from 2-Mercaptoaniline
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    Synthesis of 2-mercaptobenzothiazole (A1) is performed from the reaction of  o-aminothiophenol and carbon disulfide CS2 in ethanol under basic condition. Compound (A1)  is reacted with chloro acetyl chloride to give compound (A2). Hydrazide acid compound (A3) is obtained from the reaction of compound (A2) with  hydrazine hydrate in ethanol under reflux in the presence of glacial acetic acid .The reaction of hydrazide acid compound (A3) with ethyl acetoacetate gives pyrazole compound (A4). The new hydrazone  compound (A5) was prepared from the reaction of compound (A3) with  benzaldehyde. Reaction of compound

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Publication Date
Wed Mar 25 2020
Journal Name
International Journal Of Drug Delivery Technology
Synthesis, Characterization and Antimicrobial Evaluation of New Azo Compounds Derived from Sulfonamides and Isatin Schiff Base
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The present study deals with the synthesis of four different azo-azomethine derivatives; this is done by two steps; the first step is diazotization of sulfonamides (sulfanilamide, sulfacetamide, sulfamethoxazole, and sulfadiazine) separately, followed by the second step; the coupling reaction of diazotized compounds with isatin bis-Schiff base named 3-((4-nitrobenzylidene) hydrazono)indolin-2-one. The later one (bis-Schiff base) was synthesized by the reaction of 3-hydrazono-indolin-2-one with p-nitrobenzaldehyde. The chemical structures of newly synthesized compounds were approved on the basis of their FTIR, 1H-NMR, and CHNS elemental analysis data results. The synthesized azo compounds were tested in vitro for their antimicrobial potentia

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Publication Date
Mon Nov 01 2021
Journal Name
Journal Of Ecological Engineering
Calibration and evaluation of aquacrop for maize (Zea Mays L.) under different irrigation and cultivation methods
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rop simulation models play a pivotal role in evaluating irrigation management strategies to improve water use in agriculture. The aim of this study is to verify the validity of the Aquacrop model of maize under the surface and sprinkler irrigation systems, and a cultivation system, borders and furrows, and for two varieties of Maze (Fajr and Drakma) At two different sites in Iraq, Babylon and Al-Qadisiyah governorates. An experiment was conducted to evaluate the performance of the Aquacrop model in simulating canopy cover (CC), biomass (B), dry yield, harvest index (HI), and water productivity (WP). The results of RMSE, R2, MAE, d, NSE, CC, Pe indicated good results and high compatibility between measured and simulated values. The highest a

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Publication Date
Fri Apr 23 2021
Journal Name
International Journal Of Environmental Analytical Chemistry
Removal of levofloxacin and ciprofloxacin from aqueous solutions and an economic evaluation using the electrocoagulation process‏
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For this research, the utilisation of electrocoagulation (EC) toremove theciprofloxacin (CIP) and levofloxacin (LVX) from aqueous solutions was examined. The effective removal efficiencies are 93.47% for CIP and 88.00% for LVX, under optimum conditions. The adsorption isotherm models with suitable mechanisms were applied to determine the elimination of CIP and LVX utilizingtheEC method. Thefindingsshowed the adsorption of CIP and LVX on iron hydroxide flocs followed the Sips isotherm, with correlation coefficient values (R2) of 0.939 and 0.937. Threekinetic models were reviewed to determine the accurate CIP and LVX elimination methods using the EC method. The results showed that itfittedfor the second-order model, which indicated that the c

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Publication Date
Sat Nov 04 2023
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Preliminary Anti-Inflammatory and Anti-Microbial Evaluation of New 4,5-Dihydro-1H-Pyrazole Derivatives
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Abstract      Organic compounds with pyrazole cores have a variety of uses, notably in the pharmaceutical and agrochemical sectors. The interest in creating pyrazole compounds, examining their many features, and looking for potential uses is growing. Our work has concert with synthesis of  chalcones and pyrazolines, then finally pyrazoline-aniline derivatives and evaluation their anti-inflammatory, antibacterial and antifungal activities

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Publication Date
Thu Feb 01 2024
Journal Name
Doklady Chemistry
Synthesis, Characterization, and Biological Evaluation of New Cyclic Quinazoline Derivatives as Potential Antibacterial and Antifungal Agents
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Heterocyclic compounds are crucial for medicinal chemistry and the development of therapeutic agents like broad-spectrum antibiotics. This study devised a facile procedure to synthesize novel antimicrobial bicyclic heterocycles from 2-mercapto-3-phenylquinazolin-4(3H)-one. Advanced analytical techniques including 1 H and 13C NMR, elemental analysis, and FT-IR spectroscopy characterized the intricate chemical structures of the products. In vitro assays tested the heterocycles against aerobic and anaerobic bacterial strains using fluconazole and ciprofloxacin as antifungal and antibacterial controls. Results demonstrated the formidable broad-spectrum antibacterial and antifungal activities of the synthesized compounds, with growth inhibition

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Publication Date
Fri Apr 23 2021
Journal Name
International Journal Of Environmental Analytical Chemistry
Removal of levofloxacin and ciprofloxacin from aqueous solutions and an economic evaluation using the electrocoagulation process‏
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For this research, the utilisation of electrocoagulation (EC) toremove theciprofloxacin (CIP) and levofloxacin (LVX) from aqueous solutions was examined. The effective removal efficiencies are 93.47% for CIP and 88.00% for LVX, under optimum conditions. The adsorption isotherm models with suitable mechanisms were applied to determine the elimination of CIP and LVX utilizingtheEC method. Thefindingsshowed the adsorption of CIP and LVX on iron hydroxide flocs followed the Sips isotherm, with correlation coefficient values (R2) of 0.939 and 0.937. Threekinetic models were reviewed to determine the accurate CIP and LVX elimination methods using the EC method. The results showed that itfittedfor the second-order model, which indicated that the c

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Crossref (35)
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Publication Date
Sat Aug 01 2020
Journal Name
Research Journal Of Pharmacy And Technology
Evaluation of in vivo and in vitro protective effects of quercetin on lipopolysaccharide-induced inflammation and cytotoxicology
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Quercetin, one of the flavonoids family member, can be found in many vegetables, fruits, and beverages with a noticeable nutritional pharmacological properties. This study was aimed to evaluate the ability of quercetin to inhibit lipopolysaccharide (LPS) that induced lethal toxicity in vivo, and to elucidate the importance of the quercetin as an antitumor agent in breast cancer cell line MCF-7.In vivo experiments included the effect of hesperidin and LPS on the liver and spleen of male mice. In the liver, the antioxidant activity was measured by estimating the concentration of glutathione (GSH), and catalase (CAT), while in the spleen, the concentration of cytokines was measured including IL-33 and TNF-α. In vitro experiments included MTT

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Publication Date
Wed Sep 28 2022
Journal Name
Research Journal Of Pharmacy And Technology
Synthesis, Characterization and Preliminary Antimicrobial Evaluation of New Schiff bases and Aminothiadiazole Derivatives of N- Substituted Phthalimide
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A new series of schiff base and aminothiadiazole derivatives of N- substituted phthalimide (I-VI) were synthesized. In this work, the intermediate 4-(1,3-dioxoisoindolin-2-yl)benzaldehyde compound (I), was formed by reaction of 4-amino benzaldehyde with phthalic anhydride in glacial acetic acid(GAA). A series of Schiff bases (IV-VI) was prepared by the reaction of benzidine with compound (I) in ethanol and presence of GAA as a catalyst to form compound (IV) which react with compound (I) and p-nitro benzyldehyde to give compound (V) and (VI) respectively. A new phthalimide thiosemi-carbazone derivative (ll) was prepared by reaction of compound (l) with thiosemi-carbazide HCl in the presence of equimolar amount of sodium acetate. Fina

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Publication Date
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Preliminary Pharmacological Evaluation of Esters and Amides Derivatives of Naproxen as Potential Anti-Inflammatory Agents
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4-chloro and 4- nitro substituted phenol and aniline incorporated to a carboxylic group of naproxen a well-known non-steroidal anti-inflammatory drug (NSAID) to increase bulkiness were synthesized for evaluation as  a potential anti-inflammatory agents with expected COX-2 selectivity. In vivo acute anti-inflammatory activity of these compounds (I-IV) was evaluated in rats using egg-white induced edema model of inflammation in a dose equivalent to (2.5 mg/Kg) of naproxen. All tested compounds produced a significant reduction in paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, compounds I and IV might show higher effect comparable to that of naproxen and to that of compounds II & III whic

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