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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 Apr 30 2022
Journal Name
Sport Tk-revista Euroamericana De Ciencias Del Deporte
Effect of a training program on the development of physical abilities in football goalkeepers
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The primary aim of this study was to find out the effect of a training program on the development of physical abilities in football goalkeepers. The current study was conducted on goalkeepers of the Academy of Espanyol Sports Club in the premises of Haifa Sports Club Stadium. The study was completed by the researchers within the timeline of May 2021 to August 2021. A total of 7 goalkeepers falling within the age group of 15-17 years were recruited as the sample participants for the study. Out of 7 goalkeepers, 5 goalkeepers were included in the primary experiment and 2 of them were excluded. The training program applied had a positive effect on the development of physical abilities in the football goalkeepers of the sa

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Publication Date
Thu Dec 15 2022
Journal Name
Journal Of Genetic And Environmental Resources Conservation
Anatomical study of the vegetative parts of the species Arum colocasia L. in Iraq
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The current investigation conducted to examine the anatomical aspects of the Arum colocasia L. cultured in Iraq. The study included the anatomical characteristics of the different plant parts, including the root, stem and leaf, the results of the study on the vegetative parts were shown the important anatomical characteristics in terms of the form of the sections reviewed and vertical in them, and the study of their tissues, as well as the stomata complexities and the thickness of the epidermis, vascular bundles, pith, additionally the dimensions of mesophyll and in blade of the leaf. The research was conducted as it is one of the monocotyledon plants and because of the lack of anatomical studies on it, therefore it was studied to know the

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Tue Jul 11 2023
Journal Name
Journal Of Educational And Psychological Researches
The Effect of Daniel's Model on the Achievement of Chemistry Among Fifth Grade Student
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The aim of this research is to find out the influence of Daniel's model on the skills of the twenty-first century among the students of the scientific-fifth grade at the secondary and preparatory government morning schools for the academic year 2022- 2023. Two groups were chosen out of five groups for the fifth-scientific grade, one of which represents the experimental group that is taught by the Daniel model, and the other is the control group that is taught in the traditional method. The equivalence of the two research groups was verified with a set of variables. As for the research tool, a scale was developed by the researchers for the skills of the twenty-first century, in which they adopted the framework of the Partnership Organizat

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Publication Date
Sat May 13 2023
Journal Name
Journal Of Population Therapeutics And Clinical Pharmacology
Synthesis, Characterization of Schiff's and Mannich bases of 5-Fluoroisatin and Preliminary Antimicrobial Evaluation
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With the aim of developing potential antimicrobials, a series of new 5-fluoroisatin derivatives incorporated with different secondary amines (piperidine, morpholine, pyrrolidine, dimethylamine, and diphenylamine) for monomer, and (piperazine) in case of dimer Mannich bases, separately in presence of formaldehyde to obtain Mannich bases of 5-fluoroisatin derivatives, which then each Mannich derivatives reacts with phenylhydrazine to form Schiff bases as final products. The resulting compounds were characterized by two spectroscopic analyses; (Fourier- transform infrared) FT-IR and proton nuclear magnetic resonance spectroscopy (¹H-NMR). In addition, the in vitro antibacterial and antifungal activities were tested against some human pathogen

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Publication Date
Thu Feb 01 2018
Journal Name
European Journal Of General Medicine
The Value of Longitudinal Strain versus Coronary Angiography in Detection of Coronary Artery Disease
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Publication Date
Tue Mar 08 2011
Journal Name
Research Opinions In Animal & Veterinary Sciences
Effect of dietary parsley (Petroselinum crispum) supplementation on semen quality of local Iraqi ganders
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This study was carried out to investigate the effect of dietary supplementation with different levels of parsley on semen quality of local Iraqi ganders. A total of thirty-two local ganders were used in this study during the period from the beginning of February to the end of April. The ganders were allocated for 4 treatment groups containing 8 ganders each. The treatment groups were as follows: Control diet (free from parsley); T1: Control diet + 80 g/d parsley; T2: Control diet + 160 g/d parsley; T3: Control diet + 240 g/d parsley. Semen samples were collected twice a week, fortnightly, from each gander by the dorsal-abdominal message method. The first semen collection was used to evaluate semen volume, sperm concentration, live in total

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Publication Date
Sat Jan 22 2022
Journal Name
Aip Conference Proceedings 2437, 020032
Study and preparation of optoelectronic properties of AgAl1-xInxSe2/Si heterojunction solar cell applications
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􀀤􀁅􀁖􀁗􀁕􀁄􀁆􀁗􀀑􀀃􀀬􀁑􀀃􀁗􀁋􀁌􀁖􀀃􀁕􀁈􀁖􀁈􀁄􀁕􀁆􀁋􀀏􀀃􀀤􀁊􀀤􀁏􀀔􀀐􀁛􀀬􀁑􀁛􀀶􀁈􀀕􀀃􀀋􀀤􀀤􀀬􀀶􀀌􀀃􀁆􀁒􀁐􀁓􀁒􀁘􀁑􀁇􀀃􀁄􀁏􀁏􀁒􀁜􀁖􀀃􀁓􀁕􀁈􀁓􀁄􀁕􀁈􀁇􀀃􀁉􀁒􀁕􀀃􀁇􀁌􀁉􀁉􀁈􀁕􀁈􀁑􀁗􀀃􀁛􀀃􀀋􀀓􀀑􀀖􀀏􀀃􀀓􀀑􀀙􀀃􀁄􀁑􀁇􀀃􀀓􀀑􀀜􀀌􀀃􀁅􀁜􀀃􀁐􀁈􀁏􀁗􀁌􀁑􀁊􀀃 􀁗􀁋􀁈􀁐􀀃 􀁌􀁑􀀃 􀁄􀁑􀀃 􀁈􀁙􀁄􀁆􀁘􀁄􀁗􀁈􀁇􀀃 􀁔􀁘􀁄􀁕􀁗􀁝􀀃 􀁗􀁘􀁅􀁈􀀃 􀀋􀀕􀀑􀀘􀀍􀀔􀀓􀀐􀀖􀀃 􀁗􀁒􀁕􀁕􀀌􀀑􀀃 􀀤􀀤􀀬􀀶􀀃 􀁚􀁌􀁗􀁋􀀃 􀁇􀁌􀁉􀁉

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Publication Date
Wed Apr 01 2015
Journal Name
Journal Of Economics And Administrative Sciences
Multi-level model of the factors that affect the escalation of dust in Iraq
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In this research The study of Multi-level  model (partial pooling model) we consider The partial pooling model which is one Multi-level  models and one of  the Most important models and extensive use and application in the analysis of the data .This Model characterized by the fact that the treatments take hierarchical or structural Form, in this partial pooling models, Full Maximum likelihood FML was used to estimated parameters of partial pooling models (fixed and random ), comparison between the preference of these Models, The application was on the Suspended Dust data in Iraq, The data were for four and a half years .Eight stations were selected randomly  among the stations in Iraq. We use Akaik′s Informa

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Publication Date
Sat Aug 01 2020
Journal Name
Key Engineering Materials
Irradiation Duration Effect of Gamma Ray on the Compressive Strength of Reactive Powder Concrete
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Reactive Powder Concrete (RPC) could be considered as the furthermost significant modern high compressive strength concrete. In this study, an experimental investigation on the impact of micro steel fiber volume fraction ratio and gamma ray irradiation duration influence upon the compressive strength of RPC is presented. Three volume fraction ratios (0.0, 1.0 and 1.5) % was implemented. For each percentage of the adopted fiber ratios, six different irradiation duration was considered; these are (1, 2, 3, 4, 5 and 6) days. Gamma source (Cs-137) of energy (0.662) MeV and activity (6) mci was used. In a case of zero volume fraction ratio, the experimental results showed that gamma ray had a significant influence on the reducing of the

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Publication Date
Wed Feb 25 2026
Journal Name
Al–bahith Al–a'alami
The problem of defining the vocabulary of teaching Arabic language methodology in media colleges
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This study examined the problem of identifying the vocabulary of the methodology of teaching Arabic language in the faculties of Media. The researcher noticed the existence of an overlap between the syllabuses of the general specialization of the Arabic language and its Media sections in the universities with the special professional vocabulary that suits the study of the media student. Thus ,this study is regarded as a real attempt to present a methodological model of media language that concerns with fillfuling students ‘linguistic and knowledgeable needs relying on measuring their benefits from the methodological Arabic curriculum .  Key words:problem,  teaching’ methodology of Arabic language, media language.

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