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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 Nov 01 2020
Journal Name
Iop Conference Series: Materials Science And Engineering
Classification of Optical Images of Cervical Lymph Node Cells
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Abstract<p>the study considers the optical classification of cervical nodal lymph cells and is based on research into the development of a Computer Aid Diagnosis (CAD) to detect the malignancy cases of diseases. We consider 2 sets of features one of them is the statistical features; included Mode, Median, Mean, Standard Deviation and Maximum Probability Density and the second set are the features that consist of Euclidian geometrical features like the Object Perimeter, Area and Infill Coefficient. The segmentation method is based on following up the cell and its background regions as ranges in the minimum-maximum of pixel values. The decision making approach is based on applying of Minimum Dista</p> ... Show More
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Publication Date
Sat Dec 28 2024
Journal Name
Medicni Perspektivi
The impact of Sudafed on spleen of albino mice
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Pseudoephedrine (PSE), often known as Sudafed, belongs to a class of medications known as sympathomimetic amines, which affect the digestive system, respiratory system, and cardiovascular system. This drug has a long history of medical use; it is helpful in treating symptoms of the common cold and flu, sinusitis, asthma, and bronchitis. Due to its central nervous system (CNS) stimulant properties and structural similarity to amphe­tamine, it is also used for non-medical purposes such as doping agent, to increase focus, and as a substance that gets rid of exhaustion and drowsiness. Nevertheless only a few studies, backed up its impact on solid abdominal organs. The aim of this task is to investigate the effect of some dosages of PSE

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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)
Synthesis of new derivatives of Ceftazidime as possible Prodrugs
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Five new ceftazidime derivatives were designed and synthesized in an attempt to improve the acid stability and may increase the spectrum of ceftazidime. The synthesized compounds included;  Schiff base of ceftazidime (compound 1), ceftazidime lysine amide Schiff base (compound 2), ceftazidime lysine amide (compound 3), ceftazidime-di-lysine amide Schiff base (compound 4) and ceftazidime-di-lysine amide (compound 5). New ceftazidime derivatives were successfully prepared characterized and identified using spectral and elemental microanalysis (CHNS) analyses and the results comply with the calculated measurements.

Compounds 1 and 2 were subjected to a stability study in phosphate buffer (0.2M, pH 7.4) and in KCl/HCl buffer (0.

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Publication Date
Mon Mar 08 2021
Journal Name
Baghdad Science Journal
some properties of the nonscillatory solutions of second order
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in this paper the second order neutral differential equations are incestigated are were we give some new suffucient conditions for all nonoscillatory

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Publication Date
Sun Oct 12 2025
Journal Name
Al–bahith Al–a'alami
Legal Protection of the Printing Format of the Newspaper
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This research has been devoted to the objective and important issue which is the legal protection of the printing form of the newspaper in the Iraqi press.

As this issue constitutes the integrated unit of the printing format in addition to achieving legal protection for the illustrative image used in the press. Such matter, on both level the integrated unit of the printing format and the legal protection, is out of reach of study due to the comprehension of the subject is concerned.

Although there is a justification for dealing with both of them together as the explanatory image is one of the foundations on which the printing format of the newspaper is built. This case generates, at least, the same legal subject that appe

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Publication Date
Sat Oct 27 2018
Journal Name
Surface And Coatings Technology
Effect of surface treatment of zirconia-ceramic dental restorations
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The zirconia ceramic restoration (ZCR) is used as substitutes for the metal-ceramic restoration. Clinical studies demonstrating of ZCRs showed a high fracture incidence of veneering layer than metal-ceramic restorations. This attributed to the low bond strength of zirconia to veneering ceramic as a result of lacking of glass content in its matrix. Surface treatment was proposed to improve the bonding strength between zirconia and veneering ceramic. Several studies revealed that some treatment such as airborne particle abrasion (APA) is responsible for generating chipping of veneering ceramic. The study aimed to develop a new zirconia coatings to increase bonding strength between zirconia substrate and veneering porcelain. Three groups of 15

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Publication Date
Tue Nov 30 2021
Journal Name
Research Journal Of Pharmacy And Technology
Effect of Palliative Radiotherapy in controlling pain of Malignancy
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Background: Radiation therapy reported to be an effective in palliating pain. Objective: To describe roles of palliative radiotherapy in controlling pain in metastatic cancerous patients, and evaluation of radio-therapy doses in pain management. Methods: A prospective observational study carried out at the Baghdad Radiotherapy and Nuclear Medicine Center/Baghdad Medical City Complex, Baghdad, Iraq, from 1st of December 2018 to 30th of May 2019. 88 Patients, were included. Patients were assessed before applying radiotherapy, and at the end of treatment. Pain scoring used from 0 to 10. Kaplan Meier survival curve used. Result: The mean±SD of age was 55.44±11.1 years, and the most frequent age group was 41-50years as 37(42.1%). Breas

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Publication Date
Tue Jun 11 2019
Journal Name
Al-kindy College Medical Journal
Effect of HLA-B27 on Development of Psoriatic Arthropathy
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Background: Psoriatic arthritis is a type of arthritis that can often affect some patients who suffer from psoriasis. Approximately 40-50% of individuals with psoriatic arthritis have the HLA-B27 genotype

Objective: To investigate whether we could confirm the role of HLA-B27 alleles and psoriatic arthritis in Iraqi Arab Muslims patients.

Method: A cross sectional case control comparative study included thirty Iraqi Arab Muslims who had psoriatic arthritis that consulted the Dermatological and Rheumatological Department in AL-Kindy Teaching Hospital from November 2014 to June 2015. HLA-genotyping for HLA-B27 were assessed. A control group consisted of fifty-one healthy vol

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Publication Date
Sat May 16 2009
Journal Name
Journal Of Planner And Development
Aesthetic Elements of Urban Townscape of al Nasiriyah City
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the visual and aesthetic characteristics of the city depending on understanding several levels of visual and aesthetic characteristics to the city, starting with the study of the physical characteristics and morphology of the city in general, and urban style to it, and then study of visual composition of the city from the optical components that affect the composition of the image (visual composition) of the city represent by pathways, borders, regions and the specific features as classified by (Kevin Lynch), and then studying the details and the attention of all elements that would confer the beautiful appearance as necessary for the needs of society and the environment in general, for example, interest in the distribution and c

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Publication Date
Tue Jun 20 2023
Journal Name
Baghdad Science Journal
Determination of Molecular Weight and Viscosity of Irradiated Polystyrene
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The varied applications of polystyrene in various fields of life led to examining the cause of radiation influence on some rheological behavior of commercial Polystyrene (PS) solution in the chloroform (CHCl3) solvent. Polystyrene grains shape samples were irradiated using the radioactive element Cesium- 137 with (9 µci) activity for 10, 20, and 30 minutes. The viscosity of the polymer solution depends on the concentration and size (i.e. molecular weight) of the dissolved polymer. Experimental data showed that the radiation dose affected the value of viscosity (shear, relative, specific, and reduced). The viscosity value significantly reduced at 10 min radiation dose and when increasing the dose, the viscosity value increased

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