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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
Sat Feb 14 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Incidence of Hodgkin's lymphoma of head and neck in Baghdad city
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Background: Hodgkin's lymphoma (HL), formerly called Hodgkin's diseases is an uncommon form of lymphoma. The incidence of Hodgkin's lymphoma shows marked heterogeneity with respect to age, gender, race, geographic area, social class and histological subtype. This study was carried out in an attempt to evaluate the incidence of Hodgkin's lymphoma of head and neck in Baghdad city. Materials and Methods: The diagnosed cases of Hodgkin's lymphoma of head and neck region in Baghdad city between (1990-1999) were collected and analyzed according to age, gender, site and the histopathological subtypes of the tumor. Results: Out of (702) cases of Hodgkin's lymphoma of ten years between (1990-1999),(362 ) of them were occurred in the head and neck

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Publication Date
Sat Jan 12 2019
Journal Name
Journal Of The College Of Education For Women
The geomorphological associated of Sebkha in the Mesopotamia- plain of Iraq
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The Sebkha of geomorphological aspects of evaporative where climate leads active role, which forms part of the earth's surface in the form of Iraqi Mesopotamia plain who of the most fertile land, and because of natural factors and human Common turned most of the arable land to the territory of Sebkha. It was to determine the exact geomorphological associated of Sebkha formats by field work such as: Alnbaka, lakes, salt flats, and other forms of Small is: bridges salt, mud cracks, salt ponds, Rectangles and polygons salt, Sahaf salt, salt domes, salt gravel, bumps saline (salt points), Ash salt, salt bows, in detail and accurately documented Terrestrial Photogrammetry field and were compared to the levels and standards varieties have been

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Publication Date
Wed Dec 14 2022
Journal Name
Nasaq Journal
The Effect of Co-text on the Comprehensibility of World Englishes
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MR Younus, Nasaq Journal, 2022

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Publication Date
Tue Jan 01 2019
Journal Name
Aip Conference Proceedings
Improvement of electrical features of SnO2 based varistor doped with Al2O3
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One of the important objectives of the varistor is for a sustainable environment and reduce the pollution resulting from the frequent damage of the electrical devices and power station waste. In present work, the influence of Al2O3 additives on the non –linear electrical features of SnO2 varistors, has been investigated, where SnO2 ceramic powder doped with Al2O3 in three rates (0.005, 0.01, and 0.05), the XRD test improved that SnO2 is the primary phase, while CoCr2O4, and Al2O3 represent the secondary phases. The electrical tests of all prepared samples confirmed that the increasing of Al2O3 rates and sintering temperature improves and increase the electrical features, where the best results obtained at Al2O3 (0.05) and 1000℃, the non

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Publication Date
Mon Mar 13 2017
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of Osseointegration of Dental Implants Prepared by Piezosurgery (Clinical Study)
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ABSTRACT Background: Piezosurgery device is a system developed recently to overcome the limitation of the traditional surgical technique in implant site preparation, which use the principle of ultrasonic microvibrations to create precise & selective cut in bone in harmony with the surrounding tissues. The aim of this study was to evaluate the outcomes of implants inserted by ultrasonic implant site preparation protocol (UISP) using piezosurgery device, regarding the survival rate, stability and other related factors, at 16 weeks postoperative follow up period. Materials and Methods: A total of (24) patients, (6) males and (18) females, aged between (19-51) years old, contributed in this study receiving a total of (42) implants, all of these

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Publication Date
Sat Aug 12 2017
Journal Name
Journal Of Engineering
Influence of Temperature Upon Permanent Deformation Parameters of Asphalt Concrete Mixes
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        The performance of asphalt concrete pavement has affected by many factors, the temperature is the most important environmental one which has a large effect on the structural behavior of flexible pavement materials. The main cause of premature failure of pavement is the rutting, Due to the viscoelastic nature of the asphalt cement, rutting is more pronounced in hot climate areas because the viscosity of the asphalt binder which is
inversely related to rutting is significantly reduced with the increase in temperature resulting in a more rut susceptible paving mixtures. The objective of this study is to determine the effect of temperatures variations on the permanent deformation parameters (perm

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Publication Date
Thu Dec 28 2017
Journal Name
Al-khwarizmi Engineering Journal
Mathematical Modeling of Glucose Regulation System in Term of Perturbed Coefficients
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In this research a recent developed practical modeling technique is applied for the glucose regulation system identification. By using this technique a set of mathematical models is obtained instead of single one to compensate for the  loss of information caused by the optimization technique in curve fitting algorithms, the diversity of members inside the single set is interpreted in term of restricted range of its parameters, also a diagnosis criteria is developed for detecting any disorder in the glucose regulation system by investigating the influence of variation of the parameters on the response of the system, this technique is applied in this research practically  for 20 cases with association of  National Center for

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Publication Date
Tue Dec 30 2008
Journal Name
Al-kindy College Medical Journal
Evaluation of the Potential Role of Serum Selenium in Diabetic Patients
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Background: The altered status of some essential trace elements observed in diabetes could have deleterious influences on the health of the diabetics. Objectives: To estimate and study the potential role of serum Selenium in type 1, type 2 diabetics and healthy subjects; and its relation with lipid profile and glycemic index. Methods: A case control designed study was carried out at the National Diabetes Center (NDC) / Al-Mustansiria University; on a total of 94 participants formed of 32 type 1 diabetics, 32 type 2 diabetics and 30 healthy control participants. Data collected about age, sex and BMI; also, blood samples examined for FPG, HbA1C, serum total cholesterol, HDL cholesterol, non-HDL cholesterol, serum triglyceride and sera were

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Publication Date
Wed Mar 29 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation and Evaluation of Physical and, Rheological Properties of Clotrimazole Emulgel
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         Recently, emulgel has emerged as one of the most interesting topical preparations in the field of pharmaceutics. In this research clotrimazole was formulated as topically applied emulgel ; different formulas were prepared. The prepared emulgels were evaluated for their physical appearance , rheological behaviour , and in vitro drug release . The influence of the type of gelling agent (carbopol 934 and methyl cellulose), the concentration of both the emulsifying agent (2% and 4% w/w of mixture of span 20 and tween 20) and the oil phase (5% and 7.5% w/w of liquid paraffin) and the type of oil phase (liquid paraffin and cetyl alcohol), on the drug release from the prepared emulgels was invest

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Publication Date
Wed May 29 2019
Journal Name
Iraqi Journal Of Physics
Effect of thickness on structural properties of BixSb2-xTe3 thin films
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BixSb2-xTe3 alloys with different ratios of Bi (x=0, 0.1, 0.3, 0.5, and 2) have been prepared, Thin films of these alloys were prepared using thermal evaporation method under vacuum of 10-5 Torr on glass substrates at room temperature with different deposition rate (0.16, 0.5, 0.83) nm/sec for thickness (100, 300, 500) respectively. The X–ray diffraction measurements for BixSb2-xTe3 bulk and thin films indicate the polycrystalline structure with a strong intensity of peak of plane (015) preferred orientation with additional peaks, (0015) and (1010 ) reflections planes, which is meaning that all films present a very good texture along the (015) plane axis at different intensities for each thin film for different thickness. AFM measureme

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