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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
Fri Jun 01 2012
Journal Name
Journal Of Economics And Administrative Sciences
Dumping Policy & Its Impact In The Development of Agricultural Production In Iraq (2003- 2009)
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Dumping policy considered as one of the policies occurs severe damages to the developing countries apparently this is happens due to the potential weakness in (productive, technical, legislative, legal institutions) comparing with other developed countries who are members in WTO.

Iraq consider as one of the developing countries that has been effected by the dumping policy, the events in Iraq since downfall of the formal regime, and the allied forces domination of Iraq have all together accelerated in the apace of deterioration , particularly , after the temporary coalition authority  has forced Iraq to adopt a free foreign trade policy& exclusion of the state from the market mechanism & to consolidate import and deac

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Publication Date
Wed Oct 16 2013
Journal Name
International Journal Of Pharmacy And Pharmaceutical Sciences
Effects of mucoadhesive polymers combination on the properties of lisinpril buccal tablets prepared by wet granulation method
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Publication Date
Fri Mar 31 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
The Effect of some Variables on the Formulation of Captopril as Tablets Shaymaa Nazar Al – Sammarrai
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Captopril is an angiotensin converting enzyme inhibitor (ACEI) used to treat hypertension,
congestive heart failure, and myocardial infraction.
The only dosage form available for captopril is the plain tablet in strength of 12.5,25,50 and 100mg
tablet.
This investigation is concerned with factors affecting the formulation of captopril as a plain
tablet dosage form of 50mg. Many trials were made to prepare satisfactory tablets for the drug by
using wet – granulation methods with various additives. It was found that poly vinyl pyrrolidone
(P.V.P.) as binder gave the most satisfactory tablets. At the same time a shorter disintegrantion time
and slower dissolution rate were obtained with the addition of starch

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Publication Date
Fri Sep 15 2023
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of alpha amylase and peroxidase in saliva of pregnant women
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Background: Pregnancy is a natural physiological state that involves several biochemical modifications. Saliva is consisted of many types of proteins such as salivary alpha amylase and salivary peroxidase that might be affected by pregnancy. The former enzyme is considered one of the most prevalent proteins that is released by highly differentiated epithelial acinar cells and has been shown to have enzymatic activities while the latter has been approved that it  has a significant role in oral health. The purpose of this study was to the evaluate the salivary levels of alpha-amylase and peroxidase in pregnant and non-pregnant women. Materials and Methods: Sixty pregnant women were grouped according to the pregnancy trimesters. The first

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Publication Date
Tue Aug 05 2014
Journal Name
International Journal Of Pharmacy And Pharmaceutical Sciences
FORMULATION AND EVALUATION OF FLOATING ORAL IN-SITU GEL OF METRONIDAZOLE
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Scopus (21)
Scopus
Publication Date
Wed Nov 11 2020
Journal Name
Sys Rev Pharm
Recent Development In Oxine Complexes AndTheirMedical Application: A Review
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This review is concluded of 8-Hydroxyquinline (8HQ) compound and derivatives which has a very significant interests with a strong fluorescence , furthermore the relationship between divalent metal ions and characteristic of chelating . In the same way coordinated features have increase of its organic action and inorganic behavior by giving many samples of compounds which are a good chelating agents ligands with more capable of forming very stable complexes.Therefore, the role of (8HQ) is not limited on complexes only but its applications in different fields so this review will focus on demonstration preparation methods and properties of (8HQ) derivatives with their complexes and applications, hopefully that we will cover a part of scientifi

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Publication Date
Fri May 02 2014
Journal Name
International Journal Of Scientific & Technology Research
Synthesis, Structure And Characterization Of Zns Qds And Using It In Photocatalytic Reaction
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ZnS nanoparticles were prepared by a simple microwave irradiation method under mild condition. The starting materials for the synthesis of ZnS quantum dots were zinc acetate (R & M Chemical) as zinc source, thioacetamide as a sulfur source and ethylene glycol as a solvent. All chemicals were analytical grade products and used without further purification. The quantum dots of ZnS with cubic structure were characterized by X-ray powder diffraction (XRD), the morphology of the film is seen by scanning electron microscopy (SEM). The particle size is determined by field effect scanning electron microscopy (FESEM), UV-Visible absorption spectroscopy and XRD. UV-Visible absorption spectroscopy analysis shows that the absorption peak of the as-prep

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Publication Date
Sun Jan 01 2023
Journal Name
Journal Of Advanced Pharmaceutical Technology &amp; Research
Use of factorial design in formulation and evaluation of intrarectal in situ gel of sumatriptan
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Publication Date
Tue Oct 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
Stock Exchange and its Impact on Economic Development In the Kingdom of Saudi Arabia (KSA)
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this research paper aims at measuring and analyzing the influence of the stock exchange on the economic development in the Kingdom. This is done through comparing the Gross Domestic Product (GDP) as a changeable factor affiliated with some independent variables in the KSA stock exchange. These variables are (All Share Index {TASI}, Market Value, Trade Volume Index, number of companies and number of shares). The study covers the period from 2003 to 2017 and adapts the measuring method in analyzing this relation using the Multiple Linear Regression (Stepwise) and (SPSS). The study affirmed the validity of the

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Publication Date
Tue Nov 27 2018
Journal Name
Al–bahith Al–a'alami
The Role of Local Satellite Channels toward the Social and Cultural Development in U.A.E Society
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The study seeks to analyze the perceptions of audience in UAE towards the performance of Emirates Satellite TV Channels. It analyzed the exposure motivations of audience to satellite TV channels, its positive and negative aspects and to what extent they abide by media ethics. A survey is conducted with a sample of four hundred. The study shows significant differences between male and female towards the characteristics of TV channels, its positive and negative aspects and its commitments to media ethics.

            The study also shows that the expectancy value model and third person effect model are applicable in studying the perceptions of audience and media people in UAE t

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