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Preparation, <i>In-vitro, Ex-vivo</i>, and Pharmacokinetic Study of Lasmiditan as Intranasal Nanoemulsion-based <i>In Situ</i> Gel
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Background:

Lasmiditan (LAS) is a recently developed antimigraine drug and was approved in October, 2019 for the treatment of acute migraines; however, it suffers from low oral bioavailability, which is around 40%.

Objective:

This study aimed to improve the LAS bioavailability via formulation as nanoemulsionbased in situ gel (NEIG) given intranasally and then compare the traditional aqueous-LASsuspension (AQS) with the two successful intranasal prepared formulations (NEIG 2 and NEIG 5) in order to determine its relative bioavailability (F-relative) via using rabbits.

Method:

Two successfully prepared nanoemulsion (NE) formulas, a and b, were selected for the incorporation of different percentages of pH-sensitive in situ gelling polymer (Carbopol 934) to prepare NEIGs 1, 2, 3, 4, 5, and 6. The pH, gelation capacity, gel strength, and viscosity were predicted for the prepared NEIGs. The release (in vitro) and the nasal permeation (ex vivo) were determined for NEIG 2 and 5, and then both were subjected to pharmacokinetics in vivo studies. Eighteen male rabbits weighing 2.0 to 2.5 kg were employed in the parallel design study. The body surface area (BSA) normalization method was applied for LAS dose calculation. Serial blood samples were taken out and subjected to drug analysis using the HPLC method previously developed and validated by Kumar et al. Primary pharmacokinetics parameters, including maximum drug concentration in plasma (Cmax), time to reach C-max (T-max), and area under the concentration-time curve from time zero to affinity (AUCt0-∞) were calculated. Both NE (a and b), together with NEIG (2 and 5) formulas, were subjected to the stability study. Finally, a nasal ciliotoxicity study was carried out to evaluate the nasal toxicity of developed NEIGs 2 and 5.

Result:

The results showed that NEIGs 2 and 5 could be selected as the optimized NEIGs as both achieved 100% permeation within 20 min and then released within 25 and 35 min, respectively, thus achieving 3.3 folds with higher permeation percentages as compared to the AQS. Both NEIGs 2 and 5 exerted comparable release and permeation values as the corresponding NE a and b with more residence time in order to overcome the normal nasal physiological clearance. The values of C-max, Tmax, and AUC0- ∞ for NEIG 2 and NEIG 5 were 8066 ± 242 ng/ml, 0.75 ± 0.05 h, 19616.86 ± 589 ng. h/ml, and 7975.67 ± 239 ng/ml, 1.0 ± 0.05 h, 17912.36 ± 537 ng. h/ml, respectively, compared to the traditional AQS, which is equal to 4181.09 ± 125 ng/ml, 2 ± 0.2 h, and 8852.27 ± 266 ng. h/ml, respectively. It was discovered that NEIGs 2 and 5 had better intranasal delivery of LAS and could significantly (p < 0.05) achieve a higher value of permeability coefficient (3.3 folds) and 2.5 folds improvement in bioavailability when compared to AQS. The NE a, NE b, NEIG2, and NEIG5 formulations showed good stability at various temperatures. According to the nasal ciliotoxicity study, the nasal mucosal membrane, which was treated with NEIG 5, showed irritation with a bit of damage. However, damage was not observed when it was treated with NEIG 2, indicating the biocompatibility of the last one to be selected as the optimum formula.

Conclusion:

NEIG 2 and NEIG 5 are promising new intranasal formulas with a faster onset of action and greater bioavailability than the oral dosage form (AQS). Finally, the selected optimum gold formula that will be ready for further clinical study is NEIG 2.

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Publication Date
Wed Jun 04 2025
Journal Name
Engineering, Technology &amp; Applied Science Research
Investigating Fiber Reinforcement Effects on the Performance of Concrete Pavements under Repeated Load
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Concrete pavements are essential to modern infrastructure, but their low tensile and flexural strengths can cause cracking and shrinkage. This study evaluates fiber reinforcement with steel and carbon fibers in various combinations to improve rigid pavement performance. Six concrete mixes were tested: a control mix with no fiber, a mix with 1% steel fiber (SF1%), a mix with 1% carbon fiber (CF1%), and three hybrid mixes with 1% fiber content: 0.75% steel /0.25% carbon fiber (SF0.75CF0.25), 0.25% steel /0.75% carbon fiber (SF0.25CF0.75), and 0.5% steel /0.5% carbon fiber ((SF0.5CF0.5). Laboratory experiments including compressive, flexural, and splitting tensile strength tests were conducted at 7, 28, and 90 days, while Finite Element Analys

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Wed Jan 20 2021
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Earth And Environmental Science
Time Dependent Behavior of Engineered Cementitious Composite Concrete Produced from Portland Limestone Cement
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Conventional concretes are nearly unbendable, and just 0.1 percent of strain potential makes them incredibly brittle and stiff. This absence of bendability is a significant cause of strain failure and has been a guiding force in the production of an elegant substance, bendable concrete, also known as engineered cement composites, abbreviated as ECC. This type of concrete is capable of displaying dramatically increased flexibility. ECC is reinforced with micromechanical polymer fibers. ECC usually uses a 2 percent volume of small, disconnected fibers. Thus, bendable concrete deforms but without breaking any further than conventional concrete. This research aims to involve this type of concrete, bendable concrete, that will give solut

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Publication Date
Sat Oct 01 2022
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Baghdad Science Journal
Design of a Simple Dust Removal System for a Solar Street Light System
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      Dust and bird residue are problems impeding the operation of solar street lighting systems, especially in semi-desert areas, such as Iraq. The system in this paper was designed and developed locally using simple and inexpensive materials. The system runs automatically. It Connects to solar panels used in solar street lighting, and gets the required electricity from the same solar system. Solar panels are washed with dripping water in less than half a minute by this system. The cleaning period can also be controlled. It can also control, sensing the amount of dust the system operates. The impact of different types of falling dust on panels has also been studied. This was collected from different winds and studied their impact o

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Thu Oct 01 2020
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The operational matrix of Legendre polynomials for solving nonlinear thin film flow problems
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Sat Feb 01 2025
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On the Impact of Lacing Reinforcement Arrangement on Reinforced Concrete Deep Beams Performance
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The optimum design is characterized by structural concrete components that can sustain loads well beyond the yielding stage. This is often accomplished by a fulfilled ductility index, which is greatly influenced by the arrangement of the shear reinforcement. The current study investigates the impact of the shear reinforcement arrangement on the structural response of the deep beams using a variety of parameters, including the type of shear reinforcement, the number of lacing bars, and the lacing arrangement pattern. It was found that lacing reinforcement, as opposed to vertical stirrups, enhanced the overall structural response of deep beams, as evidenced by test results showing increases in ultimate loads, yielding, and cracking of

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Publication Date
Thu Apr 01 2021
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Assessment Of Municipal Wastewater Treatment Using Sequencing Batch Reactor Under Real Operation Conditions
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The Sequencing Batch Reactor system (SBR) is a major component of the municipal wastewater biological treatment system and water reclamation that provides high-quality water that could be reused in restricted plants that which require large quantities of water despite the lack of water. The research aims to investigate the performance of a pilot plant SBR unit under real operation conditions that was installed and operated in Al-Rustamiya Wastewater Treatment Plant (WWTP), Baghdad, Iraq. Results showed that the BOD5/COD ratio of the raw wastewater was within the average value at 0.66 emphasizing the organic nature of the influent flow and hence the amenability to biological treatment. The results also ensured that the treatment pro

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Publication Date
Thu Dec 12 2013
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Determination of Optimum Mechanical Drilling Parameters for an Iraqi Field with Regression Model
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Publication Date
Sat Jan 01 2022
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The Iraqi Postgraduate Medical Journal
Augmentation of depressed nasal dorsum by diced cartilage graft wrapped with fascia lata
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BACKGROUND: Dorsal reconstruction and augmentation for a saddle nose or generalized under projecting nose (familial ) require some type of grafting that increase the volume, raise the radix , raise the entire dorsum ,camouflage the osseocartilaginous junction or any irregularity along the dorsum, diced cartilage graft wrapped with fascia lata used to achieve that . AIM OF THE STUDY : The purpose of the study was to assess the aesthetic and functional outcome of dorsal augmentation by diced cartilage graft wrapped with fascia lata. PATIENTS AND METHODS: Between July 2018 and May 2019. 7 patients included ,4 females and 3 males ,their age ranged between 20 to 37 years ,5 were primary and 2 secondary case rhinoplasty,2 operated by closed appro

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Publication Date
Mon Dec 11 2017
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Evaluations of Potable Water Tanks Epoxy Coatings Performance Using Electrochemical Impedance Spectroscopic Method
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Abstract  

The aim of this paper is to investigate and discuss the mechanisms of corrosion of epoxy coatings used for potable water tanks. Two distinct types of Jotun epoxy coatings: Tankguard 412 contained polyamine cured epoxy and Penguard HB contained polyamide cured epoxy, were tested and studied using the electrochemical impedance spectroscopic (EIS) method. The porosity of epoxy coatings was determined using EIS method. The obtained results showed that the two epoxy coatings have excellent behavior when applied and tested in potable water of Basrah city. Polyamine is more resistance to water corrosion compared to polyamide curing epoxy and has high impedance values. Microscopic inspection after te

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Wed Jun 01 2022
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Behavioral nonlinear modeling of prestressed concrete flexural members with internally unbonded steel strands
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