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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 Aug 01 2024
Journal Name
Journal Of Engineering Research
Design, analysis and development of a proton exchange membrane in fuel cell
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Publication Date
Mon Jul 20 2020
Journal Name
Australian Journal Of Crop Science
The application of zinc fertilizer reduces Fusarium infection and development in wheat
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Fusarium pseudograminearum and Fusarium graminearum commonly cause crown rot (FCR) and head blight (FHB) in wheat, respectively. Disease infection and spread can be reduced by the deployment of resistant cultivars or through management practices that limit inoculum load. Plants deficient in micronutrients, including zinc, tend to be more susceptible to many diseases. On the other hands, and zinc deficiency in cereals is widespread in Australian soils. Zinc deficiency may have particular relevance to crown rot, the most important and damaging Fusarium disease of wheat and barley in Australia. Four wheat genotypes; Batavia, Sunco and two lines from the International Maize and Wheat Improvement Center (CIMMYT) were tested for response

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Publication Date
Tue Feb 18 2025
Journal Name
International Journal Of Scientific Research In Science, Engineering And Technology
A Comprehensive Review on Cryptography Algorithms: Methods and Comparative Analysis
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The evolution of cryptography has been crucial to preservation subtle information in the digital age. From early cipher algorithms implemented in earliest societies to recent cryptography methods, cryptography has developed alongside developments in computing field. The growing in cyber threats and the increase of comprehensive digital communications have highlighted the significance of selecting effective and robust cryptographic techniques. This article reviews various cryptography algorithms, containing symmetric key and asymmetric key cryptography, via evaluating them according to security asset, complexity, and execution speed. The main outcomes demonstrate the growing trust on elliptic curve cryptography outstanding its capabi

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Publication Date
Tue Dec 13 2022
Journal Name
Dental Hypotheses
Comparative Evaluation of Marginal Microleakage Between Bulk-Fill, Preheated Bulk-Fill, and Bulk-Fill Flowable Composite Resins Above and Below Cemento-Enamel Junction Using Micro-Computed Tomography: An In Vitro Study
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Objective: The aim of this study was to compare the marginal microleakage between bulk-fill, preheated bulk-fill, and bulk-fill flowable composite resins above and below cemento-enamel junction (CEJ) using micro-computed tomography. Methods: Sixty freshly extracted premolar teeth were prepared with a slot shaped cavities of a total of 120 Class II: 3mm (bucco-lingual), 2mm (mesio-distal) with mesial-gingival margin located 1mm coronal to CEJ, and distal gingival margin located 1mm apical to the CEJ. The samples were randomly divided into two main groups according to the restorative material (Tetric EvoCeram and 3M Filtek), and each group was further sub-divided into three subgroups according to the consistency (bulk fill, preheated bulk fil

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Publication Date
Fri Apr 01 2016
Journal Name
Journal Of Economics And Administrative Sciences
Private Financial Institutions and their Role in the Development of Small and Medium sized Enterprises in Iraq
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the reality of small and medium enterprises analysis reflects weaknesses plaguing these enterprises and strengths that are characterized by, and thus the formulation of appropriate solutions to the obstacles faced by these enterprises to enhance its contribution to the achievement of economic and social development. Iraqi small and medium enterprises suffer from several obstacles stand in front of development and  support their competitiveness, the finance one of the main obstacles which impede growth and development of these enterprises, noting the banking system in Iraq reluctance to lend to small and medium-sized enterprises, as a result of the high cost of lending these enterprises compared to large projects, as well as

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Publication Date
Thu Jun 27 2024
Journal Name
Iraqi Journal Of Pharmaceutical Sciences( P-issn 1683 - 3597 E-issn 2521 - 3512)
Impact of Gliclazide Modified Release or Glimepiride as Add-on Therapy to Metformin on Glycemic and Oxidative Stress Parameters in Type 2 Diabetic Patients
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Background: Type 2 diabetes mellitus is a condition characterized by an elevation of oxidative stress, which has been implicated in diabetic progression and its vascular complications. Aim: Assessing the impact of gliclazide modified release (MR) versus glimepiride on oxidative stress markers, glycemic indices, lipid profile, and estimated glomerular filtration rate in uncontrolled type 2 diabetic patients on metformin monotherapy. Methods: This was an observational comparative study conducted in Thi-Qar specialized diabetic, endocrine, and metabolism center. Sixty-six patients were randomized into two groups based on the addition of the sulfonylureas (SUs). Group 1 (33 patients) was on gliclazide MR, whereas Group 2 (33 patients)

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Publication Date
Tue Mar 15 2016
Journal Name
International Journal Of Pharmacy And Pharmaceutical Sciences
SYNTHESIS, CHARACTERIZATION AND PRELIMINARY ANTIMICROBIAL EVALUATION OF NEW SCHIFF BASES OF AMPICILLIN AND AMOXICILLIN DERIVED FROM ISATIN DERIVATIVES
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Objectives: Six different Schiff bases were synthesized from ampicillin and amoxicillin with isatin, 5-bromoisatin, and 5-nitroisatin. Methods: Ampicillin and Amoxicillin are linked directly through their α-amino groups to the acyl side chain with isatin and isatin derivatives by nucleophilic addition using glacial acetic acid as a catalyst. Results: chemical structures of these Schiff bases were confirmed using FTIR, 1H NMR and elemental microanalysis. The antibacterial activity was evaluated by measuring minimum inhibitory concentration (MIC) values and showed various degrees of antibacterial activities when compared with parent drugs. Compounds 1a and 2b, which are the Schiff bases of ampicillin and amoxicillin with isatin, showed very

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Publication Date
Thu Jun 23 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
In silico, In vitro studies of Anti-Oxidant and Anthelminthic Abilities of Phytoconstituents from Rhynchosia cana (Wild.) DC.
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Helminthiasis is a significant economic burden on grazing cattle. Increased resistance to currently available synthetic anthelmintics used to treat helminthiasis, and anthelmintic residues in meat and dairy products pose a significant worldwide health threat. These obstacles require the development of new anthelmintics capable of combating drug resistance while also exhibiting improved safety profiles. Rhynchosia cana (Fabaceae) is a herb that has historically been used as a worm expeller. To evaluate the phytochemical profile and explore the anti-oxidant and anthelmintic effects of different extracts of Rhynchosia cana (R. cana) by In silico and In vitro methods. Using standardised chemical t

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Publication Date
Tue Feb 12 2019
Journal Name
Iraqi Journal Of Laser
Effects of Ho: YAG Laser (2100nm) in Prostate Tissue: An in vitro Study
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Benign prostate hyperplasia (BPH), non-cancerous enlargement of prostate, is the most prevalent disease entity in elderly men. BPH affects 40% of men after the age of 60year worldwide. BPH causes problems for patients with significant lower urinary tract obstructive symptoms, if not responding to medical therapy, surgical intervention is instituted. One method of the treatment of symptomatic BPH is laser prostatectomy. The understanding of tissue effects by laser radiation is very important for the safe clinical application of laser. Objective: study the 2100 nm Ho: YAG laser gross tissue effects in the prostate at different laser dose settings in an vitro model prostate tissue samples harvested from same specimen of open surgery prostat

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Publication Date
Sun Oct 11 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Radiopacity of modified microhybrid composite resin:(An in vitro study)
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Background: The aim of this study was to measure the radiopacity (RO) of modified microhybrid composite resins by adding 2 types of nanofillers (Zinc Oxide and Calcium Carbonate) in two concentrations 3% and 5% and comparing them to unmodified microhybrid composite resins and to nanofilled composite resin. Materials and Methods: Two types of composite resin were used (Microhybrid composite MH Quadrent anterior shine and Nanofilled composite resin Filtek Z350 XT), for each tested group five disk-shaped specimens (1-mm-thick and 15 mm diameter) were fabricated. The material samples were radiographed together with the aluminum step wedge. The density of the specimens was determined with a transmission densitometer and was expressed in term of

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