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Investigation of Solubility Enhancement Approaches of Ticagrelor
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ABSTRACT

                   Ticagrelor is an orally administered antiplatelet medicine, direct-acting P2Y12-receptor antagonist. Ticagrelor binds reversibly and noncompetitively to the P2Y12 receptor at a site distinct from that of the endogenous agonist adenosine diphosphate (ADP). Inhibition of platelet aggregation stimulated by ADP is a commonly used pharmacodynamic parameter for P2Y12-receptor antagonists.

                  Ticagrelor is a crystalline powder with an aqueous solubility of approximately 10?g/mL at room temperature. Ticagrelor exhibits no pKa value within the physiological range. Ticagrelor does not exhibit pH-dependent solubility and is defined as ‘low solubility low permeability’ under the Biopharmaceutics Classification System (Class IV). The mean absolute bioavailability of ticagrelor in healthy volunteers is 36 %

                   Nanoparticles preparation and complexation is one of the recently used approaches to enhance the solubility of drugs. The aim of the present work was to improve the solubility and dissolution of ticagrelor by preparing nanoparticles and cyclodextrin inclusion complex of ticagrelor and then incorporated in to tablet dosage form. Fifteen formulas of nanoparticles were prepared by antisolvent precipitation method (solvent displacement method) utilizing one of the three polymers (PVP, Poloxamer, and HPMC) at three different drugs: polymer and solvent: anti-solvent ratios and nine formulas of cyclodextrin inclusion complex with HP?CD  by three preparation methods, physical trituration, kneading and solvent evaporation, which increase the solubility and dissolution rate of ticagrelor via formation of inclusion complex with HP?CD.

              The prepared formulas were characterized regarding the saturated solubility, polydispersity index, particle size by nano laser particle size analyzer, % yield, entrapment efficiency, and flowability, FTIR, DSC, and SEM. The selected formulas were prepared as tablets.

             The prepared tablets were evaluated for drug content, weight variation, hardness, and friability. In vitro dissolution data of the prepared tablets were analyzed using similarity factor (f2) and dissolution efficiency (DE).  

           Among all the prepared nanoparticles formulas, formula (F12) which contain HPMC as a polymer at polymer: drug ratio of (1:1) and solvent: antisolvent ratio of (1:1) was considered as the optimum formula which shows good evaluation parameters in addition to the increment in the solubility to about 9 times than that of the pure drug. The nanoparticle of the selected formula (F12) incorporated tablets showed an acceptable tablet properties in addition to a considerable increase in the dissolution efficiency to (DE=92 % and 88 % in PH 1.2 and PH 6.8 respectively) in comparison to that of the marketed tablet (DE=89% and 85% in PH 1.2 and PH 6.8 respectively).  Moreover, the analysis by DSC and SEM of the nanoparticles of the selected formula (F12) indicate a reduction in the crystallinity and amorphization of the drug. It can be concluded that the selected formula is a promising formula for the preparation of ticagrelor nanoparticles the incorporation in a tablet dosage form.

          Regarding ticagrelor inclusion complex with HP?CD Solvent evaporation method was the most effective method regarding ticagrelor solubilization and optimum formula of inclusion complex (F23) show increment in saturated solubility about ten times that of pure drug.

          The ticagrelor inclusion complex of the selected formula (F23) incorporated tablets showed an acceptable tablet properties in addition to a considerable increase in the dissolution efficiency to (DE=92 % and 90 % in PH 1.2 and PH 6.8 respectively) in comparison to that of the marketed tablet (DE=89% and 85% in PH 1.2 and PH 6.8 respectively).  

 

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Publication Date
Sun Jun 02 2013
Journal Name
Baghdad Science Journal
Computational Optimization of the Radial and Spiral Distortion Aberration Coefficients of Magnetic Deflector
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Abstract:The optimum design of the magnetic deflector with the lowest values of the radial and spiral distortion aberration coefficients was computed. The optimized calculations were made using three models, Glaser bell-shaped, Grivet-lenz and exponential models. By using the optimum axial field distribution, the pole pieces shape which gave rise to those field distributions was found by using the reconstruction method. The calculations show that the results of the three models coincide at the lower values of the excitation parameter. In general the Glaser- bell shaped model gives the optimum results at the whole range of the excitation parameter under investigation.The negative values of the spiral distortion aberration coefficient appears

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Publication Date
Tue Jun 11 2019
Journal Name
Al-kindy College Medical Journal
Conservative Treatment of Tuberculosis of the Spine in Patients with no Neurological Deficits
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Background: Patients who have both neurological impairment and kyphotic deformity can be treated medically, and this treatment can be achieved with anti-tuberculous drugs alone.

Objective: To evaluate conservative medical management of patients with tuberculosis of the spine (Pott disease). The prognostic significance of various clinical, radiological, and long-term follow-up findings in these patients was also evaluated.

Methods: Between January 2009 and January 2018 data were collected prospectively at The Neurosciences Hospital/ Baghdad/ Iraq in 44 patients with Pott disease in the thoracic and lumbar spine. These patients had no major neurological deficits or

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Publication Date
Thu Jan 04 2024
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Measuring the impact of internal governance mechanisms on the quality of financial reports
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Abstract:

                The research aims to define the theoretical framework for corporate governance and its mechanisms and shed light on corporate governance in Iraq as well as the theoretical framework for the quality of financial reports and their relationship and the role of corporate governance in activating them. A commercial bank as a sample for the research, and a survey list was prepared to show the extent to which the research sample banks are committed to applying internal governance mechanisms. imposed on them by the local environment, which leads to improving the quality of financial reports for these banks.

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Publication Date
Sun Jan 01 2023
Journal Name
International Journal Of Economics And Finance Studies
THE ROLE OF EXTERNAL INDEBTEDNESS OF THE ECONOMIC AND FINANCIAL DEVELOPMENT IN IRAQ
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The imperative of achieving financial stability has transcended national boundaries, necessitating heightened attention from both researchers and policymakers. Consequently, this article delves into an examination of the impact of government debt and public debt on financial development within the context of Iraq. The study employs monetary policy, interest rate, inflation, and population growth as control variables to prognosticate financial development. Utilizing data extracted from the World Development Indicators (WDI) spanning the period from 1995 to 2022, the study employs the dynamic autoregressive distributed lag (DARDL) approach to scrutinize the associations under investigation. The findings underscore a negative association betwe

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Scopus
Publication Date
Sun Mar 05 2017
Journal Name
Baghdad Science Journal
Synthesis and Modification of Some New Transition Metal Complexes of Poly (vinyl chloride)
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Theligand4-[5-(2-hydoxy-phenyl)- [1,3,4- thiadiazole-2- ylimino methyl]-1,5-dimethyl -2-phenyl-1,2-dihydro-pyrazol-3-one [HL1] is prepared and characterized. It is reacted with poly(vinyl chloride) (PVC) in THF to form the PVC-L compounds ,PVC-L interacted with ions of transition metals to form PVC-L-MII complexes .All prepared compounds are characterized by FTIR spectroscopy, u.v-visible spectroscopy, C.H.N.S. analysis and some of them by 1HNMR

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Publication Date
Thu Dec 30 2021
Journal Name
Diyala Agricultural Sciences Journal
A Study of Some Biological Aspects of Pacu Piaractus Brachypomus (G. Cuvier, 1818)
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The present study attempts to shed light on some biological aspects and characteristics of Piaractus brachypomus, including some biometrics, phenotypic and feeding pattern that characterizes this species. Besides, the study touches upon the body shape and the Otolith. These fish species have recently been seen frozen in the Iraqi local market. The standard length of fish specimens in this study reach 26.55cm it exceeded the specimens of Pacu fish collected from other studies from other countries, As well the specimens weight was 632gm it exceeded other studies mentioned in this manuscript. As the irregularity in the distribution of teeth rows, especially in the lower jaw was clear in our specimens. The average weight of some skull b

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Publication Date
Thu Mar 16 2017
Journal Name
Ibn Al-haitham J. For Pure & Appl. Sci.
Isolation and Partial Purifiction of Arginase from Sera of Women with Uterine Fibroids
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The first aim of the present study was performed to assay the activity of arginase in sera of women with uterine fibroid.. This study consisted of(50) women with uterine fibroid as patient's group and (30) healthy women as control group. The age ranged between (30-55) years for the two groups. The results showed that highly significant increas (P< 0.0001) in the arginase activity in sera of women with uterine fibroid (7.99± 0.23) I.U/L is found when compared with healthy group (0.52±0.02) I.U/L. The second aim was performed to isolate arginase from sera of women with uterine fibroids. The purification is done by addition of ammonium sulfate, dialysis, gel filtration chromatography by using sephadex G-50 and ion exchange chromatography by

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Publication Date
Sat Feb 13 2021
Journal Name
Journal Of Lasers In Medical Sciences
Effects of Different Laser Treatments on Some Properties of the Zirconia-Porcelain Interface
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Introduction: This study was performed to compare the effect of Fractional CO2 laser or Q switched Nd:YAG laser of surface treatment on the shear bond strength of zirconia-porcelain interface. Methods: Fractional CO2 laser at 30 W, 2 ms, time interval 1 ms, distance between spots 0.3 mm, and number of scans is (4) or Q switched Nd:YAG laser at 30 J/mm2 and 10 Hz were used to assess the shear bond strength of zirconia to porcelain. Pre-sintered zirconia specimens were divided into three groups (n = 10) according to the surface treatment technique used: (a) untreated (Control) group; (b) CO2 group; (c) Nd:YAG group. All samples were then sintered and veneered with porcelain according to the manufacturer’s instructions. Surface morph

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Publication Date
Tue Dec 03 2013
Journal Name
Al-kindy College Medical Journal
The Role of Tibialis Posterior Tendon Transfer in Correction of Foot Drop Deformity
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Backgr ound: The transfer of the tibialis posterior tendon to the anterior aspect of the ankle not only replaces the function of the paralyzed muscles, but also removes the deforming force on the medial aspect of the foot. Objecti ves: In this study, we evaluated patients who underwent tibialis posterior tendon transfer for the treatment of foot drop, and comparison through interosseous membrane route versus anterior to lower tibia route of tibialis posterior tendon transfer, with evaluation of the results according to carayon criteria Methods: Nine patients with foot drop secondary to different causes treated with tibialis posterior tendon transfer from January 2011 to January 2012 were followed up for a mean of 12 months in Al Kindy Teach

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
the effect of ethanol on the level of sialic acid in the brain
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The study dosage ethanol in the total content of acid sialic TC and acid sialic associated fat (LBSA) in blood serum and congener brain Dkor Jerd eggs study included dosage 20 animals of male rat Ald ethanol daily for a period of four weeks and concentrations 20% and 30%, 40%, 50% and size of dose 5mlThe results of the study showed that levels of TSA homogeneous in the brain and blood serum significantly reduced Ankhvaza

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