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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
Tue Apr 15 2025
Journal Name
Bulletin Of The Chemical Society Of Ethiopia
Synthesis, characterization and evaluation of anticancer and antioxidant activity of new azo dye derivatives from tryptamine and complexes
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This new azo dye 3-((2-(1H-indol-3-yl) ethyl) diazenyl) quinoline-2-ol was subsequently used to prepare a series of complexes with the metal ions of Cr+3, Cu+2, VO+2, Mn+2and Mo+6. The compounds identified by 1H and 13C-NMR, FT-IR, UV-Vis, mass spectroscopy, as well as TGA, DSC, and C.H.N., conductivity, magnetic susceptibility, metal and chlorine content. The results showed that the ligand behaves in a bidantate, and that the complexes gave octahedral, excepting for VO+2 square pyramid was given, that all complexes are non-electrolytes. The effectiveness of mention the compounds in inhibiting free radicals was evaluated by the ability to act as an antioxidant was measured using DPPH as a free radical and gallic acid as a standard s

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Publication Date
Fri Jan 01 2016
Journal Name
Der Pharmacia Lettre
Synthesis, characterization and anticonvulsant evaluation of new derivatives derived from 5-methoxy-2-mercapto benzimidazole
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A new series of 5-methoxy-2-mercapto benzimidazole derivatives were synthesized by the reaction of 5-methoxy- 2-mercaptobenzimidazole with chloroacetic acid and affords 2-((5-methoxy-1H-benzo[d]imidazol-2-yl)thio) acetic acid (1),which on cyclization with acetic anhydride and pyridine gives 7- methoxybenzo[4,5]imidazo[2,1-b]thiazol- 3(2H)-one(2), which on condensation with different aryl aldehydes in the presence of anhydrous sodium acetate in glacial acetic acid, furnishes a arylidene thiazolidinone. The purity of the synthesized compounds was confirmed by melting point and TLC.The structures were established by different spectral analysis such as FTIR,1HNMR, and CHN analysis. The newly synthesized compounds (3a-d) were in vivo evaluated f

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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, Characterization, Anti-Inflammatory, and Antimicrobial Evaluation of New 2-Pyrazolines Derivatives Derived from Guaiacol
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Abstract:         Chalcones were used to synthesis series of 2-pyrazoline derivatives and evaluated their antimicrobial and anti-inflammatory activities        (E)-1,3-diphenylprop-2-en-1-one (1-5) were synthesized by Claisen-Schmidt Condensation method through the reaction of acetophenone with five various para substituted benzaldehyde in presence of KOH, the reaction monitoring by TLC and the result intermediates were checked by melting point and FT-IR Various 2-Pyrazoline derivatives were prepared by one pot reaction that involved the refluxing of (E)-1,3-diphenylprop-2-en-1-one (1–5) and Hydrazine monohydrate in the presence of glacial acetic acid for 24 hours at a temperature of (45–50) °C fo

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Publication Date
Tue Dec 13 2011
Journal Name
Iraqi Journal Of Laser
Liver Repair in Rabbits Using 532 nm Nd:YAG Laser; In Vivo Study
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The main goal of this in vivo study was to evaluate the effect of 532nm Q-switched Nd: YAG Laser in combination with Human Serum Albumin 20% concentration (as a welding aid) on the liver tissue repair clinically, and histologically. The animals used in this study were 21 male rabbits divided into three main groups: control group (3 rabbits), conventionally treated group (9 rabbits) and Laser treated group (9 rabbits). Each two main groups (conventional and laser treated) consist of three sub-groups depending on the response evaluation at three different periods. The Laser group was treated using 532nm Q-switched Nd: YAG laser after adding human serum albumin immediately on the incised liver’s tissue. The energy of was 460mJ, and 4Hz fr

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Publication Date
Sun Jul 01 2018
Journal Name
Journal Of Global Pharma Technology
Preparation, Characterization and Biological Activity of New Derivatives of 3-Cyclic Oxazepine, 3-Cyclic Lactam and 3- Aminomethyl Imidazo (1, 2-a) Benzthiazol
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In this work a series of fourteen new compounds were synthesized. Compound [1] was formed from the reaction of 2-aminobenzothiazole and p-bromophenacyl bromide. Aldehyde group [2] was obtained from the reaction of compound [1] with pocl3 in presence of DMF and CHCl3 .After that shiff bases have been synthesized from the reaction of compound [2] with different aromatic amine to give new shiff bases [3- 5]. These new shiff bases have been reduced to their corresponding amine [6-8] by means of sodium borohydride. Then reaction of shiff bases [3-5] with phenyl isocyanate gives 3-cyclic lactam derivatives [9-11]. 3-cyclic Oxazepine derivatives [12-14] were obtained by reaction of shiff bases [3-5] with succinic anhydride. These new formed co

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Publication Date
Fri Feb 03 2012
Journal Name
Ibn Al-haitham Journal For Pure And Applied Science
Viscosity and Density of Chrom Alum in Aqueous Poly (Ethylene Glycol) Solution at Different Temperature
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Density data of alum chrom in water and in aqueous solution of poly (ethylene glycol) (1500) at different temperatures (288.15, 293.15, 298.15) k have been used to estimate the apparent molar volume (Vθ), limiting apparent molar volume (Vθ˚) experimental slope (Sv) and the second derivative of limiting partial molar volume [δ2 θ v° /δ T2] p .The viscosity data have been analyzed by means of Jones –Dole equation to obtain coefficient A, and Jones –Dole coefficient B, Free activation energy of activation per mole of solvent, Δμ10* solute, Δμ20* the activation enthalpy ΔH*,and entropy, ΔS*of activation of viscous flow. These results have been discussed in terms of solute –solvent interaction and making/breaking ability of so

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Publication Date
Mon May 08 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Viscosity and Density of Chrom Alum in Aqueous Poly (Ethylene Glycol) Solution at Different Temperature
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   Density data of  alum chrom in water and in aqueous solution of poly (ethylene glycol) (1500) at different temperatures (288.15, 293.15, 298.15) k have been used to estimate the apparent molar volume (Vθ), limiting apparent molar volume (Vθ˚) experimental slope (Sv) and the second derivative of limiting partial molar volume [δ2 θ v° /δ T2] p .The viscosity data have been analyzed by means of Jones –Dole equation to obtain coefficient A, and  Jones – Dole coefficient B, Free activation  energy of activation per mole of solvent, Δμ10* solute, Δμ20* the activation enthalpy ΔH*,and entropy, ΔS*of activation of viscous flow. These results have been discussed

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Publication Date
Sun Jan 01 2017
Journal Name
Pakistan Journal Of Biotechnology
Sequences of mitocondrial D-loop region in Iraqi persons
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Publication Date
Tue Dec 01 2020
Journal Name
Egyptian Journal Of Chemistry
Synthesis, Characterization, Industrial And Biological Application Of Co(II),Ni(II),Cu(II) And Zn(II) Complexes With Azo Ligand Derived From Metoclopramide Hydrochloride And 3,5-Dimethylphenol
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Four complexes of Co(II),Ni(II),Cu(II) and Zn(II) with the azo ligand (4-chloro-N-(2-(dimethylamino)ethyl)-5-((2-hydroxy- 4,6-dimethylphenol)diazenyl)-2-methoxybenzamide) L. The structure of ligand and complexes were confirmed on the basis of their analytical and spectral data, these dyes were tested as dyeing in cotton fabric, and also testing in light and cleaner firmness. Also, antimicrobial and antifungal activities of ligand and their complexes were evaluated and the results showed that the ZnL compound showed the higher antibacterial activity with inhibition zone of 13mm against Staphyloco-ccus epidermidis, Steptococcus sp. and Escherichia coli compared with ligand and other metal complexes .In case of ZnL compound the antifungal acti

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Publication Date
Fri Apr 27 2012
Journal Name
Al-qadisiyah Journal For Science
Synthesis and Characterization of azo Compound 5-(2-Benzoic acid azo)-8-hydroxy quinoline as Bidentate Ligand and It’s Complexeswith Co (II), Ni (II) and Cu (II) .
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Coupling reaction of 2-amino benzoic acid with the 8-hydroxy quinoline gave the azo ligand (H2L): 5-(2-benzoic acid azo )-8-hydroxy quinoline.Treatment of this ligand with some metal ions (CoII, NiII and CuII ) in ethanolic medium with a (1:2) (M:L) ratio yielded a series of neutral complexes with general Formula[M(HL)2],where: M=Co(II), Ni(II) and Cu(II), HL=anion azo ligand (-1).The prepared complexes were characterized using flame atomic absorption,FT-IR and UV-Vis spectroscopic methods as well as magnetic susceptibility and conductivity measurements.