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bijps-402
Preparation, Characterization, and in - vivo Evaluation of Daptomycin Poly(D,L-lactide-co-glycolide) Microspheres
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             Polymeric microsphere devices occupy a wide range in the field of controlled drug delivery. Subcutaneous injectable preparations of Poly(Lactide-co-Glycolide) (PLGA) microsphere of Daptomycine were prepared by solvent extraction/evaporation technique using different copolymers ratio and molecular weights. Four formulations were prepared (F1-F4) and characterized in term of particle size, surface morphology, bulk density and porosity in addition to the drug content. The effects of the above parameters on the in-vitro release study were evaluated. These formulas were evaluated also for their in-vivo release profile using rat (as an animal model) and their serum daptomycin concentration were evaluated accordingly. A trapezoidal method was used to estimate the cumulative AUC parameter and the effect of copolymers ratio and molecular weights on the shape of AUC for four formulas were evaluated. Simulation study was performed (for 7 or 10 days dosing of F1 and F2 and 15 day dosing for F3 and F4) as a predictor of the steady state concentration and other pharmacokinetics parameters. It was inferred from this study that by using tailored formulation approach, long and short acting preparations of injectable daptomycin microsphere could be developed helping to provide the clinicians more flexibility to select the suitable preparation according to the patient need.

Key words: Daptomycin, trapezoidal,microsphers ,simulation .

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Publication Date
Thu Dec 28 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Synthesis, Characterization and Biological Evaluation of New Dithiocarbamate Ligand and Its Complexes with some Metal Ions
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New bidentate dithiocarbamate ligand (NaL) namely [Sodium-2-(((3-methyl -4- “(2,2,2-tri fluoro ethoxy) pyridin-2”-yl) methyl) sulfinyl)-1H-benzoimidazole -1-carbodithioate] was prepared. This free ligand was synthesized from the reaction of a (RS)-2-([3-methyl -4-(2,2,2-tri fluoroethoxy) pyridin-2-yl] methyl sulfinyl)-1H benzoimidazole, CS2 and NaOH in methanol as solvent. From reaction of dithiocarbamate salt (NaL) with metal ions (M); Co(II), Ni(II), Cu(II), Zn(II), Cd(II) and Pd(II)”, have obtained the DTC complexes at general molecular formula [M(L)2(H2O)2] and [Pd(L)2]. To characterize the ligand and its complexes, used different analyses methods such FTIR, UV-Vis, elemental microanalysis, atomic absoreption, magnetic susceptibil

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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
Thu Feb 01 2024
Journal Name
Indonesian Journal Of Chemistry
Synthesis, Characterization, and Evaluation of MCF-7 (Breast Cancer) for Schiff, Mannich Bases, and Their Complexes
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A new synthesis of Schiff (K) 6 and Mannich bases (Q) 7 had formed compound (Q) 7 by reacting compound (K) with N-methylaniline at the presence of formalin 35% to given Mannich base (Q). Additionally, new complexes were formed by reacting Schiff base (K) with metal salts CuCl2·2H2O, PdCl2·2H2O, and PtCl6·6H2O by 2:1 of M:L ratio. New ligands and their complexes were characterized, exanimated, and confirmed through several techniques, including FTIR, UV-visible, 1H-NMR, 13C-NMR spectroscopy, CHN analysis, FAA, TG, molar conductivity, and magnetic susceptibility. These compounds and their complexes were screened against breast cancer cells. It was determined that several of these compounds had a significant anti-breast cancer effec

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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 Oct 10 2025
Journal Name
Pharmakeftiki
Synthesis, characterization, and biological evaluation of new cyclic oxazepine derivatives as potential antibacterial and antifungal agents
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In this study, Bis(4,4’-diaminophenoxy)ethane (compound C1) was synthesized via the reaction of p-hydroxyaniline with 1,2-dibromoethane. Schiff bases (compounds C2–C4) were subsequently obtained by condensing compound C1 with various aromatic aldehydes. These intermediates were further reacted with different anhydrides – namely phthalic anhydride and maleic anhydride – in order to yield the final derivatives (compounds C5–C10). All obtained compounds were characterized by using infrared spectroscopy and proton nuclear magnetic resonance, as well as through an assessment of their physical properties. Antimicrobial evaluation was conducted on some of the generated compounds using two bacterial strains (Escherichia coli and Staphyloc

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Publication Date
Tue Jan 26 2021
Journal Name
Journal Of Antimicrobial Agents
Antifungal Activity Evaluation of Co(II), Ni(II), Cu(II), Zn(II) and Fe(III) Mixed Ligand Complexes with Different Schiff Bases
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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis, Characterization and Antibacterial Activities of Ligand Type N2O4 Schiff base and its Novel Complexes with Co(II), Ni(II), Cu(II) and Zn(II) ions.
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The reaction of 2-amino benzoic acid with 1,2-dichloroethane under reflux in methanol and KOH as a base to gave the precursor [H4L]. The precursor under reflux and drops of CH3COOH which reacted with (2mole) from salicycaldehyde in methanol to gave a new type N2O4 ligand [H2L], this ligand was reacted with (MCl2) Where [M= Co (II), Ni(II), Cu(II) and Zn(II)] in (1:1) ratio at reflux in methanol using KOH as a base, to give complexes of the general formula [M(L)]. All compounds have been characterized by spectroscopic methods [1H NMR ( just to the ligand), FTIR, uv-vis, atomic absorption], melting point, conductivity, chloride content, as well as m

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Publication Date
Mon Mar 01 2010
Journal Name
Iraqi J Pharm Sci,
Synthesis, Characterization and Antibacterial Activities of Ligand Type N2O4 Schiff base and its Novel Complexes with Co(II), Ni(II), Cu(II) and Zn(II) ions
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The reaction of 2-amino benzoic acid with 1,2-dichloroethane under reflux in methanol and KOH as a base to gave the precursor [H4L]. The precursor under reflux and drops of CH3COOH which reacted with (2mole) from salicycaldehyde in methanol to gave a new type N2O4 ligand [H2L], this ligand was reacted with (MCl2) Where [M= Co (II), Ni(II), Cu(II) and Zn(II)] in (1:1) ratio at reflux in methanol using KOH as a base, to give complexes of the general formula [M(L)]. All compounds have been characterized by spectroscopic methods [1H NMR ( just to the ligand), FTIR, uv-vis, atomic absorption], melting point, conductivity, chloride content, as well as magnetic susceptibility measurements. From the above data, the proposed molecular structu

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Publication Date
Tue Sep 29 2026
Journal Name
Journal Of Baghdad College Of Dentistry
The Electrophoretic Deposition of Nano Al2O3 and AgNO3 on CpTi Dental Implant (An in vitro and in vivo study)
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Background: Even the wide use of dental implants, still there is a proportion of implants are failed due to infection. Much considerable attention has been paid to modify the implant surface. Coating of dental implant with a biocomposite material of suitable properties can improve osseointegration. And this is the main concern of this study. The aim of present study was to evaluate the use of a biocomposite coating of dental implant with (ceramic nano Al2O3 and metalic AgNo3) on the bond strength at bone – implant interface and tissue reaction. Materials and methods: A total number of forty-eight screws, CpTi dental implant used in this study. Half of these screws were coated with a biocomposite material of nano (Al2O3and AgNo3), thi

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