Preferred Language
Articles
/
7xc3kpIBVTCNdQwCSrdB
Preparation, <i>In-vitro, Ex-vivo</i>, and Pharmacokinetic Study of Lasmiditan as Intranasal Nanoemulsion-based <i>In Situ</i> Gel
...Show More Authors
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.

Scopus Crossref
View Publication
Publication Date
Thu Mar 18 2021
Journal Name
Journal Of Research In Medical And Dental Science
Antibacterial Activity of Bioactive Glass 45S5 and Chitosan Incorporated as Fillers into Gutta Percha
...Show More Authors

Antibacterial Activity of Bioactive Glass 45S5 and Chitosan Incorporated as Fillers into Gutta Percha, Ahmed I AL-Jobory*, Raghad AL-Hashimi

View Publication Preview PDF
Publication Date
Mon Dec 30 2019
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Synthesis and Characterization of Nano Y Zeolite Using MWCNT as Media for Crystal Growth
...Show More Authors

   The present research was conducted to synthesis Y-Zeolite by sol-gel technique using MWCNT (multiwalled carbon nanotubes) as crystallization medium to get a narrow range of particle size distribution with small average size compared with ordinary methods. The phase pattern, chemical structure, particle size, and surface area were detected by XRD, FTIR, BET and AFM, respectively. Results shown that the average size of Zeolite with and without using MWCNT were (92.39) nm and (55.17) nm respectively .Particle size range reduced from (150-55) nm to (130-30) nm. The surface area enhanced to be (558) m2/g with slightly large pore volume (0.231) km3/g was obtained. Meanwhile, degree of crystallization decrease

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Mon May 01 2023
Journal Name
Journal Of Medicinal And Chemical Sciences
Organic Synthesis of Some New Compounds Derived from Furfural and Their Evaluation as Antioxidants
...Show More Authors

Heterogeneous organic compounds play an important role in our daily life as they contribute in many medical and industrial fields and are in continuous development as a result of the preparation of new derivatives with different properties. From this premise, the goal of this work appears, which is preparation of (four, five, six, and seven) membered ring systems derived from furfural, by its reaction with different aromatic aldehydes, and record their antioxidant activity by using free radical scavenging method of DPPH radicals. The new ring systems are synthesized by reacting the prepared Schiff-bases with different ring closure agents (chloroacetyl chloride, mercaptoaceticacid, anthranilic acid, and phthalic anhydride), the prep

... Show More
View Publication Preview PDF
Scopus (9)
Crossref (3)
Scopus Crossref
Publication Date
Thu Dec 06 2018
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Formulation and Characterization of Bromocriptine Mesylate as Liquid Self-Nano Emulsifying Drug Delivery System
...Show More Authors

Bromocriptine mesylate is a semisynthetic ergot alkaloid derivative with potent dopaminergic activity, used in the treatment of pituitary tumors, Parkinson's disease (PD), hyperprolactinaemia, neuroleptic malignant syndrome, and type 2 diabetes ,the oral bioavailability is  approximately 6%, therefore aim  its  prepare and evaluate bromocriptine mesylate  as liquid self nano emulsifying drug delivery system to enhance its solubility , dissolution and stability . Solubility study was made in different vehicles to select the best excipients for dissolving bromocriptine mesylate. Pseudo-ternary phase diagrams were constructed at 1:1, 2:1, 3:1 and 4:1 ratios of surfactant and co-surfactant, four formulations were pre

... Show More
View Publication Preview PDF
Scopus (23)
Crossref (14)
Scopus Crossref
Publication Date
Thu Apr 01 2021
Journal Name
Iop Conference Series: Earth And Environmental Science
Effect of Metals ( Au, Ag, and Ni) as Cathode Electrode on Perovskite Solar Cells
...Show More Authors
Abstract<p>Gold, silver and nickel used as electrodes in the fabrication of perovskite solar cell by using thermal evaporation deposition method with direct structure FTO\ TiO<sub>2</sub>\ MAPbI<sub>3</sub>\ spiro-MeOTAD\ metal electrode. The cell efficiency was compared between the electrodes material as a function of time to explaining the effect of these metals electrode on cell performance, X-ray diffraction pattern showed that the samples that contain gold and nickel do not contain a compound indicating the interaction of the metal with the components of the cell or the formation of a new compound, while in the cell containing silver it was found that silver iodide is fo</p> ... Show More
View Publication
Scopus (22)
Crossref (20)
Scopus Crossref
Publication Date
Wed Feb 05 2020
Journal Name
Political Sciences Journal
Frustrations of sectarian coexistence and mechanisms to activate peaceful coexistence: Iraq as a model
...Show More Authors

Abstract The study aimed at demonstrating the reality of sectarian coexistence in Iraq, which was characterized by the tolerance and coercion caused by the successive government policies to govern Iraq and to this day. The study was based on the hypothesis that coexistence between Islamic sects in Iraq can be achieved as long as there are strong bonds linking its components, and these bonds can produce coexistence between the sects based on peace. The study concluded that the hypothesis is correct, in addition to drawing a set of observations aimed at identifying weaknesses for advancing them through the adoption of mechanisms that address these weaknesses to yield towards a genuine peaceful coexistence among Islamic sects in Iraq.

View Publication Preview PDF
Crossref
Publication Date
Sun Jul 31 2022
Journal Name
Iraqi Journal Of Science
Adsorption of Biebrich Scarlet Dye into Remains Chromium and Vegetable Tanned Leather as Adsorbents
...Show More Authors

Chromium tanned leather wastes (CTLW) and vegetable tanned leather wastes (VTLW) were used as adsorbent materials to remove the Biebrich scarlet dye (BS), as an anionic dye from wastewater, using an adsorption method. The effects of various factors, such as weight of leather waste, time of shaking, and the starting concentration of Biebrich scarlet dye, temperature and pH were studied. It described the adsorption process using Langmuir and Freundlich isotherm models. The obtained results agreed well with the Langmuir model, and the maximum adsorption capacities of CTLW and VTLW were 73.5294 and 78.1250 mg.g⁻¹, respectively, suggesting a monolayer adsorption process. The adsorption kinetic was found to follow a pseudo-second-order kinetic

... Show More
Scopus (15)
Crossref (8)
Scopus Crossref
Publication Date
Sun Jun 09 2019
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Synthesis and Preliminary Anticancer Evaluation of 6-Mercaptopurine –Methotrexate Conjugate as Possible Mutual Prodrug
...Show More Authors

Small molecules drug conjugate mutual prodrug design  (SMDC) composed of folate and lethal agent conjugate, rigidly bonded via hydrophilic bridge and self immolative disulfide  bond   ;  represent new interesting approaches for cancer treatment , the component of SMDC intended  for targeting    folate receptor , along with greater conservation  of component until reaching  the target tumor tissue . The  designing and synthesis of compound VI and VIII derived from 6-Mercaptopurine (6-MP) and Methotrexate ( MTX) conjugate altogether as mutual prodrugs were  processed forward  successfully by multistep reaction  procedures , and by Thin Layer Chromatography (TLC) for

... Show More
View Publication Preview PDF
Scopus (1)
Scopus Crossref
Publication Date
Sun Apr 02 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Conjugation of Steroidal and Non – Steroidal Anti- Inflammatory Drugs as Possible Mutual Prodrug
...Show More Authors

Prednisolone (SAID) was conjugated with ibuprofen (NSAID) through an amino acid (glycine) as a spacer arm to synthesize the following compound:

Prednisolone – glycine – ibuprofen.

    The method employed consists of converting the carboxylic acid function of (R,S) – ibuprofen – glycine to the highly reactive acid chloride and subsequent reaction with the C21 hydroxyl group of prednisolone. This reactive intermediate was found to react as well with the C17 tertiary hydroxyl group of the steroid to form three compounds and eight diastereomers. These results were confirmed by T.L.C, and the desired compound was separated by column chromatograph

... Show More
View Publication Preview PDF
Crossref
Publication Date
Mon Apr 01 2019
Journal Name
Journal Of Educational And Psychological Researches
Psychological and Health Risks of Children Toy-Related Injuries: Pellet-Gun as a Model
...Show More Authors

The research aims to identify the psychological and health risks that a child might be exposed to by playing with hazardous toys such as pellet guns. To this end, the researcher has visited Ibn Al-Haytham Eye Hospital in Baghdad, the emergency department to figure out the rate of injuries in Children for the consecutive years (2017-2018) and the first Month of (2019). The psychological risks as a result of disability are represented by the inability to accommodate the surrounding environment well. Additionally, the child experiences a kind of tension, conflict, and going in psychological crises through introversion, isolation, withdrawal tendencies, and poor conformity with himself and the Society.

View Publication Preview PDF