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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 Dec 11 2021
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Ameliorative Role of Nutraceutical Quercetin and its Derivatives Against Cognitive Impairment Process Induced by Lead Exposure in Drosophila melanogaster(Fruit Fly)
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Cumulative lifetime lead (Pb) exposure has been associated with accelerated declines in cognition through the free radical generation and epigenetic effects. Several pieces of literature have identified a correlation between exposure to lead and neurodegenerative disorders. Harwich strain Drosophila melanogaster was exposed to lead acetate for two weeks, and changes in pulse transmission by acetylcholinesterase and systemic redox were evaluated. Besides, molecular docking studies of acetylcholinesterase against Quercetin and its most common derivatives contained in food have been performed. Pharmacokinetic studies on Quercetin and its derivatives have also been performed in silico toxicity. The data obtained showed alterations in antioxi

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Publication Date
Wed Feb 18 2026
Journal Name
Al–bahith Al–a'alami
THE IDEOLOGY OF UNIVERSITY STUDENTS TOWARDS POLITICAL DISCOURSE IN SATELLITE CHANNELS: A field study on media students at Al-Mustansiriya University))
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‏The speech delivered by political blocs and parties and broadcasted by satellite channels, social and communication media has different ideologies and orientations: moderate speech calling for calm or one raising crises.‏The latter is considered very challenging due to its local and international reference.‏, this paper aims at uncovering these challenges especially during the political crisis witnessed in Iraq. This paper sheds light on the most important crisis that spread in public opinion, broadcasted by satellite, and raised by politicians who are competing to gain authority leading to a lack of peoples, confidence in them.‏This matter should not be neglected at all; e

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Publication Date
Tue Sep 01 2020
Journal Name
Biochemical And Cellular Archives
SYNTHESIS, SPECTRAL AND THERMAL CHARACTERIZATION OF NI(II), CU(II) AND ZN(II) COMPLEXES WITH NEW LIGAND TOWARDS POTENTIAL BIOLOGICAL APPLICATION
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Series of new complexes of the type [M2 (L)Cl4 ] are prepared from the new ligand[N1 ,N4 -bis(benzo[d]thiazol-2- yl)succinamide (L) derived from ethan-1,2-dicarbonyl chloride and 2-aminobenzothiozole,where, M= Ni(ii), Cu(ii) and Zn(ii) alsocomplexes of mix-ligands, the type [M(L)(8-HQ)]Cl, where, M = Ni(ii), Cu(ii) and Zn(ii),8-HQ= 8-Hydroxyquinoline. Chemical forms are obtained from their 1 H, 13CNMR, Mass spectra (for (L)), FT-IR and U.V spectrum, melting point, molar conduct.Using flame (AA), % M is determined in the complexes.The content of C, H, N and S in the (L) and its complexes was specified. Magnetic susceptibility and thermal analysis (TGA) of prepared compounds were measured.The propose geometry for all complexes[M2 (L)Cl4 ] wa

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Publication Date
Thu Dec 31 2020
Journal Name
Journal Of Accounting And Financial Studies ( Jafs )
Premiums and compensations and their impact on the financial solvency of insurance companies: applied research in the Iraqi General Insurance Company
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The collected premiums and the compensations paid are among the main variables that have a prominent role in determining the level of financial solvency of insurance companies, as the higher the financial solvency of the insurance company, the more attractive it is to the target audience to acquire the company's insurance services.

Hence the importance of the issue of the solvency of insurance companies, as it is one of the critical matters on which the effectiveness of the insurance company and its continuation in the labor market depend.

In this research, we try to clarify the role of collected premiums and compensations paid in determining the level of operational solvency of t

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Publication Date
Mon Apr 03 2023
Journal Name
Journal Of Genetic And Environmental Resources Conservation, 2023, 11(1):53-59.
Comparative histomorphological and immunohistochemical study of parathyroid gland in two Iraqi mammals (Weasel, Herpestes javanicus and long-ear hedgehog, Hemiechinus auritus)
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The present study aimed to investigate the anatomy, histology, and immunohistochemistry of parathyroid gland in two Iraqi mammals (Weasel, Herpestes javanicus and Long-ear hedgehog, Hemiechinus auritus) as a comparative study. A total of (20) animal for each species were used in the present study. Animals collected were immediately anesthesia and dissected to get the parathyroid gland. Methods of Humason and Bancroft and Stevens were employed for histological techniques. Different stains were used (Hematoxylin- Eosin stain-(H & E), Periodic Acid Schiff stain-(PAS), Azan stain, and Methyl Blue stain-(MB)) for staining the histological sections. Anti-calcitonin, code140778 marker used for immune-histochemical study. Results of the present stu

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Publication Date
Fri Sep 27 2019
Journal Name
Journal Of Baghdad College Of Dentistry
The Impact of Chronic Periodontitis on Mother-Infant Bonding Status in Relation to Salivary Tumor Necrosis Factor Alpha and Interleukin-6
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Background: Chronic periodontitis is a bacterial infection that result in bone destruction associated with the increasing level of salivary tumor necrosis alpha and interleukin6 that affect Mother-infant bonding status. The aim of the present study was to assess the relationship between the Mother-infant bonding status in mothers with chronic periodontitis in relation to Salivary Tumor necrosis factor alpha and Salivary Interleukin6. Materials and Methods: The selected sample consisted of mothers with chronic periodontitis compared with mothers with healthy periodontium in postpartum period, their age ranged between 30-40 years. Both groups were subjected to postpartum Bonding Questionnaire (PBQ). Periodontal health status was assessed f

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Publication Date
Mon Aug 26 2019
Journal Name
Global Proceedings Repository American Research Foundation
Preparation, Spectra and Biological Properties of Transition Metals ((III) and (II) Mixed - Ligand Complexes with 5-Chlorosalicylic Acid and L-Valine
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Mixed ligand metal complexes of CrIII, FeIII,II, NiII and CuII have been synthesized using 5-chlorosalicylic acid (5-CSA) as a primary ligand and L-Valine (L-Val) as secondary ligand. The metal complexes have been characterized by elemental analysis, electrical conductance, magnetic susceptibility measurements and spectral studies. The electrical conductance studies of the complexes indicate their electrolytic nature. Magnetic susceptibility measurements revealed paramagnetic nature of the all complexes. Bonding of the metal ion through –OHand –COOgroups of bidentate to the 5-chlorosalicylic acid and through –NH2 and –COOgroups of bidentate to the L-valine by FT-IR studies . The agar diffusion method has been used to study the antib

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Publication Date
Sun Sep 27 2020
Journal Name
Iraqi National Journal Of Nursing Specialties
Effectiveness of an Instructional Program Concerning Healthy Lifestyle on Patients’ Attitudes after Percutaneous Coronary Intervention at Cardiac Centers in Baghdad City
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Abstract:

Objective: The study’s aim to evaluate the effectiveness of instructional program about healthy lifestyle on patients’ attitudes after undergoing percutaneous coronary intervention.

Methodology: Quasi-experimental design/ has been utilized for the current study starting from December 2018 to March 2020 to achieve the objectives of the study. Non-probability (purposive) sample of 60 patients was divided into intervention and control groups. Data were analyzed by the application of descriptive and inferential statistical methods.

Results: findings reported that before intervention both study and control groups demonstrated low total mean of score relat

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Publication Date
Sun Jun 04 2017
Journal Name
Baghdad Science Journal
Electrical Dielectric Authorship of Polyvinyl-Acetate and Toluene Diisocyanate (PVA-TDI) with Manufactured Sulfonated Phenol-formaldehyde (SPF) Viscous Mass Material Composite
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The electrical insulation of the manufacture sulfonated phenol-formaldehyde viscous material (product) has been studied with Polyvinyl-acetate (PVA) and toluene diisocyanate (TDI) blend has been prepared by fixing percentage by weight 3:1 and mixed with different percentages by weight of the product sulfonated phenol formaldehyde viscous mass (SPF). The Fourier transform infrared (FTIR) spectroscopy is done on (SPF) resin powder and prepared film of PVA-TDI-SPF viscous mass. The quality factor (Q), dissipation factor (D), parallel resistance (Rp), series resistance (Rs), parallel capacitance (Cp), series capacitance (Cs) and phase shift (?) are measured. The calculated maximum dielectric constant (??) is 3.49x107 at sample (1) wt.1% SPF vis

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Publication Date
Wed Oct 18 2023
Journal Name
Ieee Access
A New Imputation Technique Based a Multi-Spike Neural Network to Handle Missing Data in the Internet of Things Network (IoT)
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