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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
Tue Nov 09 2021
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Banking Liberalization and its impact on Attracting Customers: applied research in a sample of Iraqi banks listed on the Iraq Stock Exchange
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The research aims to shed light on banking liberalization and explain its impact on attracting customers, especially since Iraq adopted this policy after (2003) due to the changes that occurred, as the Central Bank of Iraq granted flexibility to banks in setting the interest rate on deposits and loans as well as allowing the entry of foreign banks in the local environment. The research relied on the analytical method for the dimensions of banking liberalization represented by (liberating interest rates, liberating credit, legal reserve requirements, entering foreign banks, privatization) as well as the factors affecting the attraction of customers, and a number of Iraqi banks listed in the Iraqi Stock Exchange were selected as a

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Publication Date
Sat Nov 15 2025
Journal Name
Journal Of Physical Education
Proposed Exercises Using Flexible Resisters And Their Effect On Developing Strength Endurance And The Performance of Some Offensive Skills In Youth Basketball
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Sat Jun 01 2024
Journal Name
University Of Thi-qar Journal Of Agricultural Research
A comparative histological, histometrical and hormonal study between the ovary and uterus of non-pregnant and pregnant local breed cat (Catus felius)
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Samples of the ovary and uterus of local breed cats used to investigate the histological, histometrical and hormonal features. The paraffin embedding technique was used for processing of tissue that stained by hematoxyline and eosin stain, and massons trichrom stain. Ovary of at proestrus or oestrus phases composed of outer cortex that covered by cuboidal germinal epithelium and inner medulla. Tunica albuginea composed of a thin layer of characterized by fusiform stromal cells. The cortex content groups of Oogonial cells, numerous primordial follicles, little primary, secondary and tertiary follicles in addition for 1-2 follicular cysts and mature corpus letium. In pregnant cat the thickness of ovarian cortex was significantly incre

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
The pathological changes of the digestive system for Anas platyrhychos in Baghdad and Kut in Iraq which infectel with platyhelminthes and nematodes
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A total of 247 Mallard ( Anas platyrhynchos platyrhynchos L.) from Baghdad and Kut were examined for the Cestodes Diorchis stefanskii Sobolevicanthes gracilis; Hymenolepis mastigopraditae and the Nematode Amidostomum acutum in the first time in Iraq . Among these , 151 birds were found infected by these helminthes It has been found small nodules on the external surface of the intestine , Ulceration of mucosa inflammatory infiltrate , Oedemats changes and hyperplasia in the section of infected intestine were noticed.

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Publication Date
Fri Dec 23 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Descriptive, Prospective Observational Study- Studying Possible Prediction Factors for Disease Severity and Progression among a Sample of COVD 19 Patients in Iraq
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Abstract

Coronavirus has affected many people around the world and caused an increase in the number of hospitalized patients and deaths. The prediction factor may help the physician to classify whether the patient needs more medical attention to decrease mortality and worsening of symptoms. We aimed to study the possible relationship between C reactive protein level and the severity of symptoms and its effect on the prognosis of the disease. And determine patients who require closer respiratory monitoring and more aggressive supportive therapies to avoid poor prognosis. The data was gathered using medical record data, the patient's medical history, and the onset of symptoms, as well as a blood sample to test the

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Publication Date
Sun Jun 04 2017
Journal Name
Baghdad Science Journal
Estimating of Fatty Acids, Tcopherols, Tocotrienols, Total Carotens, Study The Physiochemical Properties And Unsaponifiable Matters Extraction From Crude Red Palm Oil(1)
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The percentage of fatty acids, quantity of tocopherols, tocotrienols, carotens and physiochemical characteristics of crude red palm oil have been evaluated, in addition to specific chemical detection of active compounds unsaponifiable matters. Results of Gas Liquid Chromatography showed:- The major fatty acids in red palm oil is palmitic (44.36%) then oleic (39.65%), linolenic (10.55%), stearic (3.56%), myristic (1.22%), arachdonic (0.24%) and palmotic (0.19%). Red palm oil contains ? – ?- ?- ? – Tocopherols with concentration 258 , 121 , 259, 109 m/kg oil , ? – ?- ?- ? – Tocotrienol with concentration 462.77 , 571.03, 619.18, 509.07 m/kg oil respectively. Total tocopherols & tocotrienols 2909.05 m/kg oil and

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Publication Date
Sat Sep 30 2023
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The Extent of Applying Corporate Governance Requirements According to International Specification (ISO 26000:2010) in the National Insurance Company: A Research Application
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Abstract

                The research aims to identify the application of corporate governance requirements according to the international standard (ISO 26000:2010) in the National Insurance Company. Strengths and weaknesses were identified to study the current state of this requirement's application in the company under investigation. The descriptive-analytical approach was utilized through a checklist derived from ISO 26000:2010. Several personal interviews and field visits were conducted to understand the extent of application and documentation based on various statistical methods. The results revealed a level of applic

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Publication Date
Sun Mar 28 2021
Journal Name
Journal Of The College Of Education For Women
Argumentative Communication in RawdatAl-MuhebbenwaNozhattAl-Mushtaqeen’s Book by Ibn Al-Qayyem: The Foundations and Mechanisms of its Functioning: مريم إبراهيم علي غبان
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This research seeks to unravel the components of the argumentative discourse in the Book ofʻRawdat al-MuhebbeenwaNozhatt al-Mushtaqeenʼ - The Garden of Lovers and the Promenade of Longing People – by Ibn Al-Qayyem Al-Jawziyah. This is because this book has a moderate discourse with a sound Islamic thought that is characterized by its sustainability, popularity, realism, and interaction with the successive developments of the new age. This reflects the intellectual maturity the composing process has reached in the philosophy of love and its educational bases in every place and time. To explore the componets, properties, and the working mechanisms of an argumentative discourse in Ibn Qayyem’s book, the present work has been conducted

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Publication Date
Thu Aug 01 2013
Journal Name
Journal Of The College Of Basic Education
A laboratory assessment on the effect of powder from Foeniculum vulgare and Eruca sativa against saw-toothed grain beetle Oryzaephilus surinamensis (L.)
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Publication Date
Tue Jun 01 2021
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Influence of Varying Temperature and Concentration on Magnetohydrodynamics Peristaltic Transport for Jeffrey Fluid with a Nanoparticles Phenomenon through a Rectangular Porous Duct
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A mathematical model constructed to study the combined effects of the concentration and the thermodiffusion on the nanoparticles of a Jeffrey fluid with a magnetic field effect the process of containing waves in a three-dimensional rectangular porous medium canal. Using the HPM to solve the nonlinear and coupled partial differential equations. Numerical results were obtained for temperature distribution, nanoparticles concentration, velocity, pressure rise, pressure gradient, friction force and stream function. Through the graphs, it was found that the velocity of fluid rises with the increase of a mean rate of volume flow and a magnetic parameter, while the velocity goes down with the increasing a Darcy number and lateral walls. Also, t

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