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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
Tue Mar 28 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Phytochemical Study of Steroidal Sapogenin “Tigogenin” Present in the Leaves of Yucca aloifolia Cultivated in Iraq
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This study detects the presence of the most important steroidal sapogenin “Tigogenin” in the leaves of Yucca aloifolia widely cultivated in Iraq. The absence of any study concerning the Tigogenin content of this medicinal plant in Iraq, and the industrial importance of Tigogenin depending on its role as a precursor in the synthesis of some steroidal drugs, acquired this study its value. This study concerned with extraction, identification, isolation, and purification of Tigogenin from the leaves of Yucca aloifolia. Extraction of this compound was carried out using two methods. Identification of this compound was done using thin layer chromatography (TLC) where different solvent systems had been tried. Liberm

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Publication Date
Sun Mar 26 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Phytochemical Study of Steroidal Sapogenin “Tigogenin” Present in the Leaves of Agave americana Cultivated in Iraq
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The presence of the most important steroidal sapogenin “Tigogenin” in the leaves of Agave americana  cultivated in Iraq was detected. The absence of any study concerning the Tigogenin content of this medicinal plant in Iraq, and the industrial importance of Tigogenin depending on its role as a precursor in the synthesis of some steroidal drugs, acquired this study its value. This search include extraction,  isolation,  purification and dentification of Tigogenin from the leaves of Agave americana. Extraction of this compound was carried out using two methods. Identification of this compound is carried out by using thin layer chromatography (TLC) where three different mobile phase have been use

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
A study copepoda invertebrates ecology in lower Zab
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The samples were collected monthly crustaceans Mjmafah foot of two stations in tributary Zab down and two others in the Tigris River for one year with effect from November 2001 until October 2002 recorded during the study period the current 41 units taxonomic and were higher density of Mjmafah foot Guy Tigris River before the mouth of the tributary

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Publication Date
Wed Jan 30 2019
Journal Name
Journal Of The College Of Education For Women
Triumph in the Glorious Qur’an: A Semiotic study
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Triump is a happy end and a positive outcome of any good deed on the part of a human
being, or of any competition or contest in any field. A human being’s life abounds with gain
and loss. If one succeeds one will be happy psychologieally, physieally, etc. if one the other
hard one loses, one wil be in a state. Between loss and gain there are many a step.
However humans work hard to be a great success and a read winner.The life of the world constitutes a huge race-track where people try hard to head towards
the hereafter. Therefore, we find people who succed and gain the Garden, and people whose
habitation is the fire, The Glorious Qur’an has shown us in many a surah the way to success
when Allah mentions ‘great

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Publication Date
Sun Dec 01 2024
Journal Name
كلية التربية للبنات
Strategic Maneuvering in Commercial Advertisement: A Pragmatic Study
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This study deals with strategic maneuvering in advertisement from a pragmatic point of view found in some commercial advertisements in order to investigate and analyze the pragmatic devices that are used in the strategic maneuvering and stages. The study attempts to shed light on the most fuzzy areas in advertisements that is probably how the language of advertisements employed by advertisers to affect consumers positively. The primary goal of strategic maneuvering is to discover how the pragmatic devices have persuasive techniques that are used to gain a competitive advantage and more sales. This study is a contribution to the field of research in the language used in advertising. In this research, the effectiveness of strategic man

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Publication Date
Tue Aug 01 2023
Journal Name
Journal Of Engineering
Risk Response in Construction Project: A Review Study
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Construction projects are characterized as projects with multi phases and activities, complex, unique, and have many different parties and stakeholders. Risks could appear at one or more of the construction project stages and may affect the achievement of project objectives. Therefore, one of the key elements in the planning phase of any project is the risk management process (RMP). This study attempts to understand the terminology of risk in general, risk management, and response to risk in particular. This study is mainly a review of thirty-eight studies that have been published between 1997 and 2020 that demonstrate the importance of the crucial phase of risk response from the risk management process and its impact on

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Publication Date
Sun Oct 03 2010
Journal Name
Journal Of The Faculty Of Medicine Baghdad
Genitourinary tract infection in diabetic women: Bacteriological study
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Background: The influence of glucose metabolism is seen in many infectious diseases, making  diabetic patients more vulnerable to sepsis and other serious sequelae of bacterial invasion such as UTI and vaginitis.Patients and method: sixty two patients (women) were suffering from GUTIs consulting Al-Elwya hospital from November- 2009 to March -2010. Two samples were taken from those patients (urine samples and vaginal swabs); these samples were cultured on Blood, Chocolate, and MacConkey's agar for isolation of bacteria.Results: The study group consists of sixty two women suffering from (GUTI), their ages range from 18-55 years. Thirty eight of them were diabetic women and twenty four of them were non- diabetic women. Twenty t

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Publication Date
Mon Jul 25 2022
Journal Name
Studies In Pragmatics And Discourse Analysis
Negation in American Discourse: A Socio-Cognitive Study
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The present study cognitive aims to investigate the negation phenomenon in American political discourse under Critical Discourse Analysis (CDA) principles. The research sample includes two speeches given by Clinton and Trump in their election campaigns in 2016. Since the nature of the study follows the social-cognitive approach, the researcher adopted two models of analysis to achieve the study’s objectives: First, the theoretical framework of MST (developed by Fauconnier (1994), Fauconnier and Sweetser (1996) to examine meaning construction resulting from building different levels of negative mental spaces by two different genders the selected speeches. Second, pragmatic model to examine the role of gender from the functional per

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Publication Date
Sun Jun 15 2025
Journal Name
الذكوات البيض
Drugs in Iraq 1932-1968 (A Historical Study)
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The spread of drugs in Iraq during the period 1932-1968 was one of the most dangerous. phenomena affecting humans, as it leads to addiction, to the point where people cannot live without it, it also leads to the destruction of the user's nerves and body, and the inability to maintain balance, or even perform daily tasks. There are different types of drugs, and the side effects vary from one type to another However in all cases, drugs remain the scourge of the world, They are a toxic substance that attacks the nerves and tries to destroy them' The importance of the subject lies in the fact that it is anew and unstudied topic, and it studies a phenomenon that affects humanity in general and Iraq in Particular through it light can be shed on t

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Publication Date
Thu Mar 05 2026
Journal Name
Al–bahith Al–a'alami
Convincing methods in designing infographic content analytical study
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The research aims to reveal the recent trends used in providing information and to know the persuasive methods used in designing the content of the infographic as well as the nature of persuasive design methods and the topics presented by the infographic in the research sample.   The researcher used the survey method, specifically the survey, by using the content analysis method to analyze the infographic material from the sample selected from the press and news sites that are the subject of the research, based on the method of what was said? How was it said? The researcher relied on the intentional sample, and this sample depends on the researcher selecting the vocabulary of the sample based on experiences and evaluating the c

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