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Development of Lyophilized Ebastine-Loaded Novasome Tablets: Comprehensive Physicochemical Characterization and In Vitro/In Vivo Release Evaluation
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Introduction/Objective:

Ebastine, a second-generation H1 antihistamine, exhibits poor aqueous solubility and consequently low oral bioavailability, limiting its clinical therapeutic efficacy. Novasome is an advanced vesicular nanocarrier system that offers a promising approach to enhance the solubility and dissolution behavior of a poorly water solubility drug. Therefore, this study aimed to develop, optimize, and characterize ebastine-loaded novasomes and to compress them into tablets to enhance drug solubility, dissolution, and oral bioavailability.

Methods:

Ebastine-loaded novasomes were prepared and optimized, then converted into lyophilized tablets using a suitable cryoprotectant. The optimized formulation was characterized for Particle Size (PS), Polydispersity Index (PDI), Zeta Potential (ZP), and Entrapment Efficiency (EE). Solidstate properties were assessed via Differential Scanning Calorimetry (DSC) and X-Ray Diffraction (XRD), while drug-excipient compatibility was evaluated using Fourier-Transform Infrared Spectroscopy (FTIR). In-vitro release studies were performed under stimulated physiological conditions, and in-vivo pharmacokinetic evaluation was conducted in Wistar rats.

Results:

The selected ebastine-loaded novasome exhibited a mean particle size of 189.9nm, a polydispersity index of 0.31, and an entrapment efficiency of 86.19%. In-vitro release exceeded 90% over 12 hours, significantly surpassing the dissolution profile of pure ebastine. DSC and XRD analyses confirmed amorphization of the drug within the Novasomal matrix, while FTIR revealed no evidence of drug-excipient compatibility. In-vivo studies demonstrated a 493.88% increase in relative oral bioavailability compared to free drug suspension (p < 0.05).

Discussion:

The enhanced dissolution and bioavailability are attributable to drug amorphization, high surface area to volume ratio of the nanovesicles, and protective entrapment of ebastine within the bilayer structure, which together improved gastrointestinal solubilization and oral bioavailability.

Conclusion:

The lyophilized Ebastine-loaded novasome tablet constitutes a stable, effective, and pharmacokinetically superior oral dosage form, offering significant potential for enhance the oral bioavailability of poorly water-soluble drugs.

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Publication Date
Thu Jan 04 2024
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Environmental tax and its role in sustainable social development
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Abstract:

  The research aims to diagnose the relationship between the environmental tax and the development of the sustainable social dimension, where the environmental tax is considered a tool in promoting sustainable development according to its economic, social and environmental dimensions through the application of legislation and instructions for environmental protection, and that imposing an environmental tax will have a clear impact in achieving the dimensions of sustainable development and compliance With regard to the social dimension, the research relied on the financial data for the years (2019-2022) in obtaining information. The research reached a set of results, the most prominent of which was

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Publication Date
Wed Feb 01 2017
Journal Name
Journal Of Economics And Administrative Sciences
(Sustainable Agricultural Development in Iraq ... Solutions and Treatments Obstacles)
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Abstract:

    The achievement of agricultural development provide food security and to form a basis for economic growth and comprehensive social, requires a number of actions to overcome the obstacles and problems facing the development of this economic sector, to make it able to achieve food security and operation of the workforce, and reduce dependence on the outside in the provision of food peripherals, and so it is only available through the highest degree of efficiency and economic mobilization of resources, so most of the developed and developing countries alike seek to achieve sustainable agricultural development tobacco meet the food requirements and good jobs for c

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Publication Date
Tue May 16 2023
Journal Name
Political Sciences Journal
Educational Policies in Singapore and their Reflections on Development
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Singapore has invested its human resources for the development of the country since earlier times, so it has directed attention to the education sector. Education and development complement each other, as investment in education has contributed over several years to the development of Singapore economy and has made it one of the strongest economies in Asia and the world. Despite the obstacles that faced educational policies in Singapore, the presence of a wise leadership capable of overcoming difficulties and solving them, and providing the appropriate atmosphere for the development of education has contributed significantly to making it one of the most advanced educational systems in the world, and making this system the main pillar for

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Publication Date
Tue Apr 01 2014
Journal Name
Journal Of Economics And Administrative Sciences
Multi-dimensional poverty and sustainable human development in Iraq
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The problem of poverty and deprivation constitute a humanitarian tragedy and its continuation may threaten the political achievements reached by the State. Iraq, in particular, and although he is one of the very rich countries due to availability of huge economic wealth, poverty indicators are still high. In addition, the main factor in the decline in the standard of living due to the weakness of the government's performance in the delivery of public services of water, electricity and sanitation. Thus, the guide for human development has been addressed which express the achievements that the state can be achieved both on a physical level or on the human level, so in order to put appropriate strategies and policies aimed at elimin

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Publication Date
Mon Nov 09 2020
Journal Name
Construction Research Congress 2020
How to Improve Workforce Development and Sustainability in Construction
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Publication Date
Wed Nov 22 2023
Journal Name
Drug And Chemical Toxicology
Preparation, characterization, and toxicity evaluation of microemulsion formulation containing prunetin for potential oral applications
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Publication Date
Mon Sep 30 2013
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Synthesis, Characterization and Evaluation of Overbased Magnesium Fatty Acids Detergent for Medium Lubricating Oil
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A series of overbased magnesium fatty acids such as caprylate, caprate, laurate, myristate, palmitate, stearate and oleate) were synthesized by the reaction of the fatty acids with active – 60 magnesium oxide and carbon dioxide (CO2) gas at 60 oC in the presence of ammonia solution as catalyst, toluene / ethanol solvent mixture (9:1vol/vol) was added.
The prepared detergent additives were characterized by FTIR, 1HNMR and evaluated by blending each additive in various concentrations with medium lubricant oil fraction (60 stock) supplied by Iraqi Midland Refineries Company. The total base number (TBN, mg of KOH/g) was determined, and the results of TBN were treated by using two-way analysis of variance (ANOVA) test. It was found that

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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)
Design, Synthesis, Characterization and Comparative Cytotoxic Evaluation of bis-(2- mercaptoacetate) gold (III) chloride
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In recent years , the interest in gold (III) species have gained more and more attention for cancer chemotherapy , this was stimulating by the possibility to develop new agents with mode of action and clinical profile different from the established platinum metalodrugs.

With this frame, recently new square planar Au(III)  complexes (Au(L)(L')n); where L=SCH2COO- ; L'=HSCH2COO- had been synthesized with S/O – donor ligands.

In this article and by the aim to replace, one of (L') ligand by anion chloride ligand (which supposedly more relevant for the biodistribution of the compound than for its pharmacodynamic effects), new complex (Au(L')

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Publication Date
Sun Nov 01 2020
Journal Name
Journal Of Physics: Conference Series
Synthesis, characterization and biological evaluation of thiazolyl azo ligand complexes with some metal ions.
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(E)-2-(benzo[d]thiazol-2-yliazenyl)-4-methoxyaniline was synthesized by reaction the diazonium salt of 2-aminobenzothiazole with 4-methoxyaniline. Identified of the ligand by spectral techniques (UV-Vis, FTIR,1HNMR and LC-Mass) and microelemental analysis (C.H.N.S.O) are used to produce of the azo ligand. Complexes of (Co2+, Ni2+, Cu2+ and Zn2+) were synthesized and identified using atomic absorption of flame, elemental analysis, infrared and UV-Vis spectral process as well conductivity and magnetic quantifications. Nature of compounds produced have been studied followed the mole ratio and continuous contrast methods, Beer's law followed during a concentration scope (1×10-4-3×10-4 mole/L). height molar absorptivity of compound solutions h

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Publication Date
Sat Dec 10 2016
Journal Name
International Journal Of Current Microbiology And Applied Sciences
Synthesis, Characterization and Biological Evaluation of Penicillin Derivatives Complexes with Some Transition Metal Ions
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