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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
Mon Nov 21 2022
Journal Name
College Of Islamic Sciences
Sources of audio images in the poetry of the Islamic
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      الحمدُ للهِ رب العالمين ، والصلاة والسلام على نبيه الأمين محمد r وعلى آله الطيبين الطاهرين ، وأصحابه الغر الميامين:

             تعد الصورة السمعية مفهوما بيانيا نجده في البلاغة العربية واضحاً مؤثرا، مؤديا دورا جوهريا في إيصال الفكرة التي يروم الأديب إيصالها إلى المتلقي   ولا تبدو السمعية واضحة إلاّ إذا نظر إليها في حالة أدبيه تهز كيان الشاعر &nbsp

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Publication Date
Sun Oct 02 2011
Journal Name
Journal Of Educational And Psychological Researches
The effect of brainstorming in linguistically grow of garten child
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The study aimed to identification the effect of brainstorming in linguistically grow of garten child the sample of study is composed from (48)male and female children have been distributed for two groups,one of them is experimental and another is disciplined for every  per of garten and pre education,and they have been awarded in a number of variations. For measuring the subordinate variation(linguistically grow)the researcher prepared ascale for this purpose that consist of two parts:the first part the scale of linguistically grow of garten child(4-5 years)and the second part the scale of linguistically grow of pre education child (5-6 years).Consist of every one from (20)shapes of linguistically grow shapes for garten chil

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Publication Date
Sun Aug 09 2015
Journal Name
No
Stability and Instability of Some Types of Delay Differential Equations
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Publication Date
Sat May 15 2010
Journal Name
International Journal Of Poultry Science
Effect of Dietary Linseed on Egg Quality of Laying Quail
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This experiment was performed to investigate the effect of dietary supplementation with linseed on egg quality of laying quail. A total of 320 9-week-old Japanese quail (Coturnix coturnix japonica) 9-wk old were allocated to 4 treatment groups with 4 replicates containing 20 quail each. Birds were fed a commercial diet containing 0% (C), 2% (T1), 4% (T2), or 6% (T3) linseed. Birds received water and diet ad libitum during the total period of the experiment. Egg quality characteristics were monitored over 3 consecutive 21-d periods. Egg quality criteria involved in this experiment were egg weight, yolk diameter, yolk height, yolk weight, albumen height, albumen weight, shell weight, shell thickness, Haugh unit, albumen percentage, yolk perce

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Publication Date
Sun Jan 27 2019
Journal Name
Journal Of The College Of Education For Women
The issue of creation of AL-Muatazala and AL-Shaira
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words of God the Quranic text , is genera words have many faces and connotations a ccording to references, cutures and Ages.That the Quranic text is fixed , But the connotations are moveable the scientists agreed about the miracle of the Qurantic text , But they differd of the Position of miracLe including the muatazala and Al- Ashaira who have adopted the idea of sytem and miracle of linguistic . Most of them were lingustics, grammerians and writers as: AL- Jahith, AL- Faraa Abivbeida , Ibn kutaba , AL -Rumani , AL -katabi , AL- Bakilaai , AL- Gargani and Others.
They also differed in what the words of Allaah mean . Is the Quranic text creature or updated ,it is the issue that exhausted the effort.of muslim scientists though its imbo

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Publication Date
Mon Oct 09 2017
Journal Name
Osr Journal Of Pharmacy And Biological Sciences (iosr-jpbs
Blood Supply of female reproductive system of Lepuscapansisarabicus (Arabain hare)
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Summary:The anatomy of the arterial and venous vessels of the mammalian oviduct is well describedin women and in laboratory and farm animals. The arteries are derived from the ovarian anduterine stems; the relative contribution of these vessels, however, or variations in that contributionwith the menstrual or estrus cycle and/or gamete or embryo transport is unknown.

Publication Date
Mon Oct 07 2024
Journal Name
Научный форум:
FEATURES OF TRANSLATION OF POLYSEMANTIC VERBS FROM RUSSIAN INTO ARABIC
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Publication Date
Tue Sep 01 2015
Journal Name
Journal Of Engineering
Dynamic Analysis of Fluid – Structure Interaction of Axial Fan System
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Fluid-structure interaction method is performed to predict the dynamic characteristics of axial fan system. A fluid-structure interface physical environment method (monolithic method) is used to couple the fluid flow solver with the structural solver. The integration of the three-dimensional Navier-Stokes equations is performed in the time Doman, simultaneously to the integration of the three dimensional structural model. The aerodynamic loads are transfer from the flow to structure and the coupling step is repeated within each time step, until the flow solution and the structural solution have converged to yield a coupled solution of the aeroelastic set of equations. Finite element method is applied to solve numerically

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Publication Date
Sat Jan 01 2011
Journal Name
Advances In Condensed Matter Physics
Compositional Dependence of Structural Properties of Prepared Alloys and Films
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Results of a study of alloys and films with various Pb content have been reported and discussed. Films of of thickness 1.5 μm have been deposited on glass substrates by flash thermal evaporation method at room temperature, under vacuum at constant deposition rate. These films were annealed under vacuum around 10−6Torr at different temperatures up to 523 K. The composition of the elements in alloys was determined by standard surfaces techniques such as atomic absorption spectroscopy (AAS) and X-ray fluorescence (XRF), and the results were found of high accuracy and in very good agreement with the theoretical values. The structure for alloys and films is determined by using X-ray

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Publication Date
Wed Dec 15 2021
Journal Name
Journal Of Baghdad College Of Dentistry
Assessment of Coating Zirconium Implant Material with Nanoparticles of Faujasite
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Aim: To evaluate the wettability and microhardness of Zirconium (ZrO2) dental material when coated with different concentrations of Faujasite. Materials and methods: 30 circular disks produced from ZrO2, then each group is classified into 10 control groups, 10 coated groups with 3% Faujasite, and 10 coated groups with 7% faujasite by electro-spun tool to study variable properties in hardness and water contact angle of implant materials. Results: This study stated the high hardness in 7% of faujasite concentration for ZrO2, in addition, the contact angle decreased gradually until reach 0 ᵒ in 7% concentration of faujasite with ZrO2 Conclusion: Water contact angle (WCA) declined till disappeared in (7% wt.) of faujasite coated with the Z

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