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bijps-706
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 Oct 01 2022
Journal Name
Lark Journal
The problem of synonyms and similar words in the translation of the Holy Quran into Russian (based on the translation by Elmir Kuliev) اشكالية الترادف والكلمات المتقاربة في المعنى في ترجمة القران الكريم الى اللغة الروسية (بناءا على ترجمة إلمير كولييف) Проблема синонимов и близких по значению слов в переводе Священного Корана на русский язык (на материале перевода Эльмира Кулиева)
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In our research, we dealt with one of the most important issues of linguistic studies of the Holy Qur’an, which is the words that are close in meaning, which some believe are synonyms, but in the Arabic language they are not considered synonyms because there are subtle differences between them. Synonyms in the Arabic language are very few, rather rare, and in the Holy Qur’an they are completely non-existent. And how were these words, close in meaning, translated in the translation of the Holy Qur’an by Almir Kuliev into the Russian language.

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Publication Date
Wed Jun 18 2014
Journal Name
Geological Quarterly
Stable carbon and nitrogen isotopes and elemental composition and origin of organic matter from the Euphrates, Injana and Dibdibba formations in Iraq: discrimination between marine and terrestrial environments
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Publication Date
Thu Sep 02 2010
Journal Name
Journal Of Kerbala University
N3O3 Hexanuclear Complexes type are Synthesized and Characterised from the reaction of Diphenylmonoxime with (Mn(II) ,Co(II) ,Ni(II) ,Cu(II) ,Zn(II) , and Hg(II) ) ions.
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The new Hexadentate complexes type [M(H3L3)]K were prepared from the condensation reaction of Diphenylmonoxime and KOH with (Mn(II), Co(II), Ni(II), Cu(II), Zn(II), and Hg(II)) in methanol with 3:1 ligand : metal ratio to give a series of new complexes of the general formula [M(H3L3)]K (where: M(II) = Mn ,Co ,N ,Cu ,Zn and Hg).All compounds have been Characterized by spectroscopic methods [I.R, U.v-Vis, atomic absorption and microanalysis (C.H.N) along with conductivity measurements. The stability constant K and Gibbs free energy ∆G were calculated for [Co (H3L3)] K, [Ni (H3L3)] K and [Cu (H3L3)] K and complexes using spectrophotometer method. The obtained values indicate that these complexes stable in their solution. From the above data

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Publication Date
Sun Dec 04 2016
Journal Name
Baghdad Science Journal
Synthesis, Characterization, Antimicrobial and Theoretical Studies of V(IV),Fe(III),Co(II),Ni(II), Cu(II), and Zn(II)Complexes with Bidentate (NN) Donar Azo Dye Ligand
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The new 4-[(7-chloro-2,1,3-benzoxadiazole)azo]-4,5-diphenyl imidazole (L) have been synthesized and characterized by micro elemental and thermal analyses as well as 1H.NMR, FT-IR, and UV-Vis spectroscopic techniques. (L) acts as a ligand coordinating with some metal ionsV(IV), Fe(III), Co(II), Ni(II), Cu(II), and Zn(II). Structures of the new compounds were characterized by elemental and thermal analyses as well as FT-IR and UV-Vis Spectra. The magnetic properties and electrical conductivities of metal complexes were also determined. Study of the nature of the complexes formed in ethanol following the mole ratio method.. The work also include a theoretical treatment of the formed complexes in the gas phase, this was done using the (hyperch

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Publication Date
Sun Jan 01 2023
Journal Name
International Journal Of Physiology, Nutrition And Physical Education
The effect of effort perception training according to race speed rhythm control for developing speed endurance, adapting maximum heart rate, and achieving 3000 m running/hurdles for men
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Publication Date
Thu May 22 2025
Journal Name
Journal Of Baghdad College Of Dentistry
Evaluation of marginal gap at the composite/enamel interface in Class II composite resin restoration by SEM after thermal and mechanical load cycling (An in vitro comparative study)
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Background: This study compared in vitro the marginal adaptation of three different, low shrink, direct posterior composites Filtekâ„¢ P60 (packable composite), Filtekâ„¢ P90 (Silorane-based composite) and Sonic fillâ„¢ (nanohybrid composite) at three different composite/enamel interface regions (occlusal, proximal and gingival regions) of a standardized Class II MO cavity after thermal changes and mechanical load cycling by scanning electron microscopy. Materials and methods:Thirty six sound human maxillary first premolars of approximately comparable sizes were divided into three main groups of (12 teeth) in each according to the type of restorative material that was used: group (A) the teeth were restored with Filtekâ„¢ P6

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Publication Date
Fri Jul 29 2022
Journal Name
Journal Of Environmental Science And Health, Part A
Comparing the efficiency of N-doped TiO<sub>2</sub> and commercial TiO<sub>2</sub> as photo catalysts for amoxicillin and ciprofloxacin photo-degradation under solar irradiation
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Publication Date
Sun Dec 01 2024
Journal Name
Energy Storage
Comprehensive Study of <scp>PAN</scp>‐<scp>NaBF<sub>4</sub></scp> Solid Polymer Electrolytes: Insights Into Optical, Structural, Thermal, Electrical, and Electrochemical Properties for Sodium‐Ion Batteries
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ABSTRACT<p>This research explores the use of solid polymer electrolytes (SPEs) as a conductive medium for sodium ions in sodium‐ion batteries, presenting a possible alternative to traditional lithium‐ion battery technology. The researchers prepare SPEs with varying molecular weight ratios of polyacrylonitrile (PAN) and sodium tetrafluoroborate (NaBF<sub>4</sub>) using a solution casting method with dimethyl formamide as the solvent. Through optical absorbance measurements, we identified the PAN:NaBF<sub>4</sub> (80:20) SPE composition as having the lowest energy band gap value (4.48 eV). This composition also exhibits high thermal stability based on thermogravimetric analysis results. </p> ... Show More
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Publication Date
Tue Jan 01 2013
Journal Name
Advances In Physics Theories And Applications
Adsorption Study of Symmetrical Schiff Base Ligand 4,4’-[hydrazine-1,2-diylidenebis(methan-1-yl-1-ylidene) bis (2-methoxyphenol)] on Granulated Initiated Calcined Iraqi Montmorillonite via Columnar Method.
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The adsorption ability of Iraqi initiated calcined granulated montmorillonite to adsorb Symmetrical Schiff Base Ligand 4,4’-[hydrazine-1, 2-diylidenebis (methan-1-yl-1-ylidene)) bis (2-methoxyphenol)] derived from condensation reaction of hydrazine hydrate and 4-hydroxy-3-methoxybenzaldehyde, from aqueous solutions has been investigated through columnar method.The ligand (H2L) adsorption found to be dependent on adsorbent dosage, initial concentration and contact time.All columnar experiments were carried out at three different pH values (5.5, 7and 8) using buffer solutions at flow rate of (3 drops/ min.),at room temperature (25±2)°C. The experimental isotherm data were analyzed using Langmuir, Freundlich and Temkin equations. The monol

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Publication Date
Wed Jan 23 2019
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
The Active Role of Admin strative Skills in Reinforcing Strategic Entrepreneur Ship Through Organizational Flexibility: دراسة استطلاعية لأراء عينة من الإدارات العليا والوسطى في المصارف العراقية الخاصة / بغداد
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The study has tackled three important variables on the strategic and organizational level, that are : (Administrative skill, strategic Entrepreneurship  and organizational flexibility). Through the statistical analysis is, the research hers have sought to identify the relation among them. The study has been applied on a sample of (44) private banks in Iraq. A questionnaire, which has been designed according to a number of international standards, has been used. It's made of (29) items that cover the three variables to test their hypotheses. A number of statistical tools have been used A number of conclusion have been reached and recommendations have also been suggested.

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