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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 Dec 05 2023
Journal Name
Baghdad Science Journal
Synthesis of Multifunctional Polymers Based on Tert-Butyl Acrylamide/Octyl Acrylate as Lubricant Additives and Adsorbents for Copper Ion from Aqueous Solution
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Two homopolymeric and three copolymeric additives for base oil were synthesized using octyl acrylate (OA) and tert-butyl acrylamide (TBA) monomers. The two additives named P1 and P2 are the homopolymers of TBA and OA, respectively, whereas copolymeric additives named Co1, Co2, and Co3 were synthesized by varying the ratios of TBA:OA as 1:3, 3:1 and 1:1, respectively. The prepared polymers were characterized by Fourier Transform Infrared (FTIR). Based on the solubility of synthesized polymers in base oil and reactivity ratios of TBA/OA copolymer (0.222, 0.434) calculated by Fineman-Ross method, P2, Co1, Co2 and Co3 were selected to evaluate their performance as pour point depressant (PPD), viscosity improver (VII), and anticorrosion addit

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Publication Date
Thu Jan 25 2024
Journal Name
Biomedical Materials
Enhancing the therapeutic potential of curcumin: a novel nanoformulation for targeted anticancer therapy to colorectal cancer with reduced miR20a and miR21 expression
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Abstract<p>Curcumin (Cur) possesses remarkable pharmacological properties, including cardioprotective, neuroprotective, antimicrobial, and anticancer activities. However, the utilization of Cur in pharmaceuticals faces constraints owing to its inadequate water solubility and limited bioavailability. To overcome these hurdles, there has been notable focus on exploring innovative formulations, with nanobiotechnology emerging as a promising avenue to enhance the therapeutic effectiveness of these complex compounds. We report a novel safe, effective method for improving the incorporation of anticancer curcumin to induce apoptosis by reducing the expression levels of miR20a and miR21. The established</p> ... Show More
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Publication Date
Tue Apr 18 2023
Journal Name
Al–bahith Al–a'alami
Counter Psychological Warfare in the partisan press during the operations of Mosul liberation: An analytical study in the “Tareek Al Shaab” Newspaper
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The research aims to monitor the methods of Counter psychological warfare in the Iraqi press during the operations to liberate Mosul from the control of the terrorist organization ISIS.The research used the survey method, and “Tareek Al Shaab” Newspaper as a research sample, chosen according to the systematic random sample.
The research reached the following results:
1- The Communicator’s relied on the contents of the counter-psychological warfare and its methods in the battle of “Qadimun Ya Naynawa” used in the newspaper. The methods used were labels assigning such as : inevitable victory, prodding and morale, consensus, breaking of opposition morale, stereotyping, demonization of the opponent

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Publication Date
Tue Jan 01 2013
Journal Name
Photonics &amp; Lasers In Medicine
The assessment of pathological changes in cerebral blood flow in hypertensive rats with stress-induced intracranial hemorrhage using Doppler OCT: Particularities of arterial and venous alterations/Die Beurteilung von pathologischen Veränderungen der Hirndurchblutung bei hypertensiven Ratten mit Stress-induzierten intrakraniellen Blutungen mittels Doppler-OCT: Besonderheiten von arteriellen und venösen Veränderungen
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Abstract<p>Hemorrhagic insult is a major source of morbidity and mortality in both adults and newborn babies in the developed countries. The mechanisms underlying the non-traumatic rupture of cerebral vessels are not fully clear, but there is strong evidence that stress, which is associated with an increase in arterial blood pressure, plays a crucial role in the development of acute intracranial hemorrhage (ICH), and alterations in cerebral blood flow (CBF) may contribute to the pathogenesis of ICH. The problem is that there are no effective diagnostic methods that allow for a prognosis of risk to be made for the development of ICH. Therefore, quantitative assessment of CBF may significantly advance the underst</p> ... Show More
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Publication Date
Tue May 09 2017
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
TIME MANAGEMENT AND WORK PRESSURE AND THEIR RELATIONSHIP TO ADMINISTRATIVE LEADERSHIP/ A CASE STUDY AT THE HIGHER INSTITUTE FOR ADMINISTRATIVE DEVELOPMENT OF SECURITY AND ADMINISRATIVE: TIME MANAGEMENT AND WORK PRESSURE AND THEIR RELATIONSHIP TO ADMINISTRATIVE LEADERSHIP/ A CASE STUDY AT THE HIGHER INSTITUTE FOR ADMINISTRATIVE DEVELOPMENT OF SECURITY AND ADMINISRATIVE
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The research aims to determine the strength of the relationship between time management and work pressure and administrative leadership, where he was taken a sample of (47) of the administrative leadership at the Higher Institute of security and administrative development in the Ministry of Interior was used questionnaire as a key tool in collecting data and information and analyzed the answers to the sample surveyed by using Statistical program (spss) in the arithmetic mean of the calculation and test (t) and the correlation coefficient, the research found the most important results: the existence of significant moral positive relationship between both time management and work pressure and administrative leadership, the leadership of th

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Publication Date
Sat Feb 09 2019
Journal Name
Journal Of The College Of Education For Women
The Effect of Combining Video Lectures and Kolb Experiential Learning on EFL Student-Teachers’ Ability to Teach Communicative Coursebook and their Teaching Competencies
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Communicative-based textbooks are developed and disseminated throughout the country.
However, it is difficult for teachers who themselves have learnt English through the traditional
approaches to suddenly be familiar with CLT (Communicative Language Teaching) principles
and teach communicatively. Therefore, many teachers remain somewhat confused about what
exactly CLT is and others familiar with CLT but unable to achieve communicative classroom
teaching. Consequently, those teachers need to be introduced to the CLT principles and they need
training in how to put CLT principles into practice. Accordingly, this study aims to find out the
effect of combining video lectures and Kolb experiential learning on EFL student-t

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Publication Date
Wed Jun 24 2020
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
INCREASED PREFERENCE OF DARKLING BEETLES AKIS SUBTRICOSTATA REDTENBACHER, 1850 AND TRACHYDERMA PHILISTINA REICHE AND SAULCY, 1857 (COLEOPTERA, TENEBRIONIDAE) FOR VEGETATION WITH INCREASING TEMPERATURE
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   A square experimental arena with vegetation on one interior side was deployed in a Sharjah, United Arab Emirates desert. Individual darkling beetles (Coleoptera, Tenebrionidae) Akis subtricostata Redtenbacher, 1850 and Trachyderma philistina Reiche and Saulcy, 1857 were placed inside the arena at temperatures ranging between 27 - 49°C. Whether they chose the vegetated side of the arena or not was recorded, as well as how long it took for them to reach the vegetated side, if they chose it. Both species preferred the vegetated side at all temperatures, and the chance of them choosing the vegetated side increased significantly with increasing temperature (logistic regression, p = 0.0096 and p = 0.0003 for

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Publication Date
Thu Mar 08 2018
Journal Name
Iosr Journal Of Applied Chemistry
synthesis, Composition, Spectral, Geometry and Antibacterial Applications ofMn(||),Ni(||),Co(||),Cu(||) and Hg(||) schiff Base complexes of N2O2 mixed donor with 1,10-phenanthroline
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synthesis, Composition, Spectral, Geometry and Antibacterial Applications ofMn(||),Ni(||),Co(||),Cu(||) and Hg(||) schiff Base complexes of N2O2 mixed donor with 1,10-phenanthroline

Publication Date
Thu Dec 30 2021
Journal Name
College Of Islamic Sciences
The omission of letters according to Zakaria al-Ansari in his book (Fath al-Rahman by revealing what is ambiguous in the Qur’an)
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Summary

The book (Fatah al-Rahman reveals what is ambiguous in the Qur’an), which is a book of verbal similarities that tries to touch the Qur’an expression, and the subtle differences between its expressions and expressions. It appeared when it appeared in many chapters, from which I chose to delete in monolithic letters such as Ba and Ta, and to heal and delete in non-monosymbols such as (that) and (may) and (no), so the search came to two chapters The first is for deleting the monolithic letters, and the second is for deleting non-monosyllabic letters, preceded by introductory discussions revolving around the linguistic and idiomatic definition of deletion, a brief translation of the

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Publication Date
Sat Mar 02 2019
Journal Name
Biochem. Cell.arch.
EVALUATION OF PRIMARY IMPLANTS STABILITY IN IMMEDIATE AND DELAYED TREATMENT PROTOCOLS ACCORDING TO BONE DENSITY, JAWS, GENDER AND AGE UTILIZING PERIOTEST M DEVICE
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