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Nanosuspensions of Selexipag: Formulation, Characterization, and in vitro Evaluation

Selexipag is an orally selective long-acting prostacyclin receptor agonist, which indicated for the treatment of pulmonary arterial hypertension. It is practically insoluble in water ( class II, according to BCS). This work aims to prepare and optimized Selexipag nanosuspensions to achieve an enhancement in the in vitro dissolution rate. The solvent antisolvent precipitation method was used for the production of nanosuspension, and the effect of formulation parameters (stabilizer type, drug: stabilizer ratio, and use of co-stabilizer) and process parameter (stirring speed) on the particle size and polydispersity index were studied. SLPNS prepared with Soluplus® as amain stabilizer (F15) showed the smallest particle size 47nm with PDI and Zeta potential value of 0.073 and -47mV, respectively. SLPNS exhibited an increase in the dissolution rate in phosphate buffer pH 6.8 (100% drug release during 60 min) compared to the pure drug ( 40% during the same time). This result indicates that SLPNS is an efficient way of improving the dissolution rate.

 

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Publication Date
Mon May 15 2023
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of Some New Nucleoside Analogues from Substituted Benzimidazole and Evaluation of Their Biological Activities

This research includes the synthesis of some new nucleoside analogues via 1,3-
dipolar cycloadditon reaction starting with 1,3,4,6- Tetra- O-benzoyl –2 – azido-2-
deoxy- β – D- fructofuranose (F3) which was prepared in three steps ,protection
(benzoylation ) , bromination and azotation ((F1-F3) from D- fructose as sugar
moiety while the base moiety , 2-substituted benzimidaole derivatives (A1-A5)
were synthesized by condensation of O-phenylenediamine with different aromatic
aldehyde .
Nucleophilic substitution of propargyl bromide with benzimidaole derivatives (gave
the N- substituted compounds (B1-B5) which were reacted with azido sugar through
1,3- dipolar cycloadditon reaction to give nucleoside analo

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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

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 Aug 09 2022
Journal Name
Journal Of Research In Medical And Dental Science
Evaluation of the Antibacterial Efficacy of Electrolyzed Oxidizing Water as an Irrigant against Enterococcus faecalis (An In vitro Study)

Evaluation of the Antibacterial Efficacy of Electrolyzed Oxidizing Water as an Irrigant against Enterococcus faecalis (An In vitro Study), Noor A Khait*, Muna Saleem Kalaf

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Publication Date
Sun May 26 2019
Journal Name
Iraqi Journal Of Science
Evaluation of Compounds Extracted from Eight Genera of Wild Mushrooms from Nigeria for Anti-cell Proliferation Activity in Vitro

     Mushrooms have bioactive compounds that have antimicrobial, anti-cancer and antioxidant activities among other medicinal benefits. In the present study, we examined the anti-cell proliferation activities of mushrooms from eight genera obtained from the wild in Nigeria. Saccharomyces cerevisiae was used as a model organism to screen mushroom extracts for anti-cell proliferation activity. Polyphenols, high molecular weight polysaccharides and low molecular weight compounds from aqueous extracts were obtained from the test mushrooms using methanol and water respectively. The extracts were screened in vitro at different concentrations of extracts with the CyQuant cell proliferation assay. The high molecular

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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

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
Sun Jul 31 2022
Journal Name
Iraqi Journal Of Science
Synthesis, Characterization and Evaluation of Some Pyranopyrazole Derivatives as Multifunction Additives for Medium Lubricating Oils

      The current work involves synthesis of 6-amino-4-(4-hydroxyl-3-methoxyphenyl)-3-methyl-1-phenyl-1,4- dihydropyrano[2,3-c]pyrazole-5-carbonitrile (2) by condensation of 2-(4-hydroxyl-3-methoxybenzylidine) malononitrile (1) with 3-methyl-1-phenyl-2-pyrazolin-5-one. The product 2 was then reacted with various aldehydes to form a series of Schiff base derivatives 3a-h. The reaction of the chosen Schiff base derivatives (3a and 3b) with mercaptoacetic acid gave thiazolidinone derivatives (4a and 4b). The structures of prepared compounds were confirmed using FT-IR, 1H NMR, and 13

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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

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
Thu Apr 29 2021
Journal Name
Iraqi Journal Of Science
Synthesis and Characterization of Silver Nanoparticles Using Prodigiosin Pigment and Evaluation of Their Antibacterial and Anti-Inflammatory Activities

This study focused on the biological synthesis of silver nanoparticles (AgNPs), using prodigiosin pigment produced by Serratia marcescens. The effect of parameters such as pH, temperature, time, with various concentrations of silver nitrate (AgNO3) and prodigiosin on the synthesis of AgNPs were also studied.  Optimized results of the biosynthesis process revealed an increase in the intensity of Surface Plasmon Resonance (SPR) bands of nanoparticles with shifting at the wavelength of 400 nm. In addition, optimum synthesis of AgNPs was achieved at pH 12, temperature 55℃, and reaction time 24 h, with concentrations of prodigiosin, as a reducing agent, of 12.5 µg/ml and silver ion concentration of 1 mM. Measuremen

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Publication Date
Thu Nov 05 2020
Journal Name
Methods And Objects Of Chemical Analysis
Derivative Spectrophotometric Determination for Simultaneous Estimation of Isoniazid and Ciprofloxacin in Mixture and Pharmaceutical Formulation

A simple analytical method was used in the present work for the simultaneous quantification of Ciprofloxacin and Isoniazid in pharmaceutical preparations. UV-Visible spectrophotometry has been applied to quantify these compounds in pure and mixture solutions using the first-order derivative method. The method depends on the first derivative spectrophotometry using zero-cross, peak to baseline, peak to peak and peak area measurements. Good linearity was shown in the concentration range of 2 to 24 µg∙mL-1 for Ciprofloxacin and 2 to 22 µg∙mL-1 for Isoniazid in the mixture, and the correlation coefficients were 0.9990 and 0.9989 respectively using peak area mode. The limits of detection (LOD) and limits of quantification (LOQ) were

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Publication Date
Sun Apr 16 2017
Journal Name
Tikrit Journal For Dental Sciences
Evaluation of Apical Transportation and Curve Straightening of Curved Root Canals after Preparation with Different Nickel - Titanium Rotary Systems (Comparative in Vitro Study)

The goals of endodontic preparation were to shape and clean the space of the root canal and remove microorganisms, affected dentin and pulp, the apical foramen and the canal curve should be protected from being transported during endodontic canal preparation. The aim of this study was to evaluate the curve straightening of curved root canals and apical transportation after preparation with four rotary systems. Forty mesial roots of the lower 1st molars teeth only the mesiobuccal canals were used, these roots were immersed into cold clear acrylic , the teeth roots divided into four groups according to rotary system used for preparation of the canals (ten roots for each group):. group I: ProTaper Next rotary system, group II: IRaCe Plus rotar

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