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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 Feb 25 2024
Journal Name
Iraqi Journal Of Agricultural Sciences
THE EFFICIENCY OF GUM-SILICA CMPOSITE FOR REMOVING OF WASTEWATER TURBIDITY
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A novel mixed natural coagulant has been developed to remove sewage pollutants and heavy metals from Qanat- al- Jayesh by using low cost adsorbent natural materials. In these materials, significant interaction contains Arabic gum mixed with extracted silica from rice husk ash (natural coagulants) by the Batch device approach, using two variables, pH values ranging from 5-8 and contact times between 0.25-5 hrs. All wastewater samples were collected after treatment by adsorbents and examined for determination of residual heavy metal concentrations: Pb, Ni, Zn and Cu by atomic absorption spectroscopy (AAS), turbidity, pH, total dissolved salts (TDS), electrical conductivity (EC) and total salinity (TS). The results obtained indicate Th

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Publication Date
Thu Feb 07 2019
Journal Name
Journal Of The College Of Education For Women
(Love and Love) in the light of the significance of Quranic
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Thanks allah and peace be upon our prophet muhammed and upon his family and his
followers……
Love means in holy quran what comes to people s mind nowadays and what it inspired its
signi ficence is related with sensual desire and it means adore and passion .by the waythe
word (ishiq) adore wasn’t mentioned in holy quran which means that both of their bases are
farfrom each oiter in m eaning.
The significance of love means virtue while adore means the excess and desire so adore is
dis praised . as al askari said (died 395h )between love and adore.adore is the strain of desire
to get the purpose from lovers if it was ahuman who intended to make love affairs.
Today both of love and adore changed in their meani

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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Antiamoebic activity of extracted alkaloids of Capparis spinosa in Laboratory mice
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The current study was concerned with the effect of alkaloid extract of the aerial parts of Capparis spinosa against Entamoeba histolytica and compared with drug Metronidazole in the laboratory mice .Stool samples were collected from people infected with maebiasis to infect laboratory mice . The alkaloid compounds were separated by thin chromatography technique (TLC) and identified by spectral methods represented by spectral infrared (IR) and altraviolate (UV) . the stady include determining mid-term lethal dose LD50 of the extract as the concentration was 21.65 g / kg . The effect dose of the extract was tested on the infected experimental mice with Entamoeba histolytica after 10 days of the infection compared with the mice infected

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Publication Date
Thu Sep 12 2019
Journal Name
Al-kindy College Medical Journal
Reliability of fine needle aspiration biopsy in diagnosis of breast lump
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Background: breast cancer is commonest cancer globally and the 1st cancer in Iraq among females, its management and prognosis depend on early diagnosis, the traditional method was excisional biopsy which is expensive and invasive leading to delayed diagnosis, FNAB is cheap nom invasive more acceptable to women, Aim of the study: to test the reliability of FNAB in preoperative diagnosis of breast lump.

Methodology: This is a retrospective study of 204 cases, 102 breast cancer cases and 102 benign breast lesions, taken between Jan. 2017 – Nov. 2017. The sample taken from the breast cancer early detection center in  Al-Alwiyaa maternity teaching hospital, during the year 2017

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Publication Date
Tue May 16 2023
Journal Name
Political Sciences Journal
Criticism of the Green Political Thought of the Modernist Intellectual Output
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In the last decades of the twentieth century, ideas emerged that were increasingly being floated, stating that the planet is suffering from a population explosion, depletion of resources, and environmental problems that require action to be addressed. Although these problems in practice need scientific solutions, the problem is that these solutions collide with ideologies. Here the green political thought emerges, based on the criticism of many ideological axioms. The owners of green thinking agree that most environmental damage is due to the humanist doctrine. It criticizes modernity accompanied by a scientific revolution, where this criticism centered around (the rationality of the scientific and technological mind), here the green pol

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Publication Date
Sun Sep 01 2013
Journal Name
Journal Of Economics And Administrative Sciences
The reality of Taxation in Iraq and Aspect of it’s Development
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This research is considered a simple attempt and effort which is it first and last target is to point at the procedures of the taxes account that aims to reduce the taxes from the persons and give free to the person who estimates the tax to practice what comes from the competent authorities to describe the person who estimates the tax and not an accountant who practice the accountant procedures which are imposed on him by the annual terms from higher administrations , So he can not evaluate   state of the person who pay the tax , and he might be dissatisfied with his job , because his role can’t  be activated from the general foundation taxes.

And so , this research includes four fields:-

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Publication Date
Tue Sep 01 2020
Journal Name
Baghdad Science Journal
Identification of Acinetobacter baumannii and Determination of MDR and XDR Strains
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The current study focuses on the bacterium Acinetobacter baumannii due to its importance as a nosocomial infections source in addition to its increased resistance against antibiotics. Different clinical and hospital environment samples were collected, and cultured on A. baumannii selective media: Leed Acinetobacter agar and Herellea agar. A. baumannii have been identified by traditional methods, followed by confirmation using molecular identification to detect blaoxa-51 like gene which is considered a diagnostic gene since it is present in genome of all A. baumannii strains. The result was, nineteen bacterial isolates of A.baumannii were obtained, from twenty-seven suspected isolate

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Publication Date
Tue Jun 01 2021
Journal Name
Al-khwarizmi Engineering Journal
Prediction of Surface Roughness after Turning of Duplex Stainless Steel (DSS)
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Feed Forward Back Propagation artificial neural network (ANN) model utilizing the MATLAB Neural Network Toolbox is designed for the prediction of surface roughness of Duplex Stainless Steel during orthogonal turning with uncoated carbide insert tool. Turning experiments were performed at various process conditions (feed rate, cutting speed, and cutting depth). Utilizing the Taguchi experimental design method, an optimum ANN architecture with the Levenberg-Marquardt training algorithm was obtained. Parametric research was performed with the optimized ANN architecture to report the impact of every turning parameter on the roughness of the surface. The results suggested that machining at a cutting speed of 355 rpm with a feed rate of 0.07 m

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Publication Date
Sun Apr 07 2013
Journal Name
Journal Of Educational And Psychological Researches
The effect of relaxation music in reducing symptoms of dental anxiety
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Many behavioral researchers pointed out the importance of relaxation techniques in the treatment of different psychological disorders where find  the importance of these techniques in reducing anxiety and stress and the resulted of behaviors and habits, with the development of these techniques are being used to gain public health, whether mental health or physical or mentality, and one of these techniques is music therapy that reduces tension and anxiety and operates a state of relaxation, which is used in the treatment of  patients of dental clinic.                        

Re

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Publication Date
Wed Jan 01 2020
Journal Name
Corporate Ownership And Control
Planning and controlling of intellectual capital: The role of beyond budgeting
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The purpose of this study is to explore whether the adoption of Beyond Budgeting (BB) as a management accounting practice (MAP) contributes to developing intellectual capital (IC) and creating value in Iraqi companies. This requires an understanding of the views of the Iraqi managers about the nature of the information provided by this practice, which may be used to determine whether this information is relevant in the management of IC in the context of Iraq. This research aims also to explore the challenges of the adoption of the BB in planning and controlling IC in Iraq. The study adopts a qualitative approach and an interpretive paradigm. It also adopts a semi-structured interview method of collecting data from executive managers

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