Preferred Language
Articles
/
bijps-706
Investigation of Solubility Enhancement Approaches of Ticagrelor
...Show More Authors

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).  

 

Scopus Crossref
View Publication Preview PDF
Quick Preview PDF
Publication Date
Sun Oct 01 2017
Journal Name
Journal Of Economics And Administrative Sciences
Financial performance evaluation using some indicators of value creation (Analytical study of selected sample of Iraqi banks)
...Show More Authors

The research of three-based financial indicators to create value for shareholders, have been identified research problem in a number of the questions revolved around the extent to which it can express its based performance metrics to create value for the essence and the reality of the surveyed enterprises performance, Can the departments surveyed companies to choose the scale or the most harmonizing index and an expression of the actual performance of the company, has the goal of research is to diagnose the strengths and weaknesses in the performance of the surveyed enterprises through the use of a number of based on the concept of creating economic value and the search for the most suitable indicator to the reality of the perfor

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Thu Apr 01 2021
Journal Name
Biochem. Cell. Arch.
Role of Spraying Potassium Fertilizer Types in Improving of flag Leaf Contribution in Grain Yield of Wheat
...Show More Authors

A field experiment was carried out during winter season of 2019 at Al-Muradiya research state, Babylon government, Iraq, to study the role of the sprayed types of potassium fertilizer in improving of flag leaf contribution in grain yield of wheat. The layout of the experiment was randomized complete block design in factorial arrangement at three replicates. The experiment included spraying common and nano potassium fertilizer at booting stage, in addition to control treatment (spraying of distilled water) as a first factor, and removal treatments (removal of flag leaf at 10% anthesis stage and nonremoval) as a second factor. The results showed that the spraying of nano potassium fertilizer was significantly superior in the dry matter transp

... Show More
Scopus (11)
Scopus
Publication Date
Sun Aug 01 2021
Journal Name
Journal Of Engineering
Seismic Vulnerability Assessment of Rizgary Hospital Building In Erbil City, the Capital City of KR of Iraq
...Show More Authors

Collapsing building structures during recent earthquakes, especially in Northern and Eastern Kurdistan, including the 2003 earthquake in Cewlig; the 2011 earthquake in Van; and the 2017 earthquake near Halabja province, has raised several concerns about the safety of pre-seismic code buildings and emergency facilities in Erbil city. The seismic vulnerability assessment of the hospital buildings as emergency facilities is one of the necessities which have a critical role in the recovery period following earthquakes. This research aims to study in detail and to extend the present knowledge about the seismic vulnerability of the Rizgary public hospital building in Erbil city, which was constructed before releasing the seism

... Show More
View Publication Preview PDF
Crossref
Publication Date
Thu Apr 30 2020
Journal Name
Journal Of Economics And Administrative Sciences
The impact of the of Six Sigma to improve the performance of dentists in albaladeat specialized Dental
...Show More Authors

The research aims at introducing the principles of six sigma and if it had any effect of the dimensions of six sigma to improve the performance of the dentists and the availability of an appropriate environment in the center Specialist respondent to the application of six sigma principles and how to adopt Specialized Center under the dimensions of the six sigma and if there informed enough with the management methodology six sigma, and if you can adopt six sigma as one of the entrances to reduce medical errors. So  Search creating six sigma five dimensions and are (the commitment and support of senior management, the focus  on the patient, continuous improvement, training and civil, and infrastructure) as a variable int

... Show More
View Publication Preview PDF
Crossref
Publication Date
Fri Apr 01 2016
Journal Name
Journal Of Engineering
Effect of Variation of Degree of Saturation with depth on Soil–Concrete Pile Interface in Clayey Soil
...Show More Authors

Bearing capacity of a concrete pile in fine grained cohesive soils is affected by the degree of saturation of the surrounding soil through the contribution of the matric suction. In addition, the embedded depth and the roughness of the concrete pile surface (expressed as British Pendulum Number BPN) also have their contribution to the shear strength of the concrete pile, consequently its bearing capacity. Herein, relationships among degree of saturation, pile depth, and surface roughness, were proposed as a mathematical model expressed as an equation where the shear strength of a pile can be predicted in terms of degree of saturation, depth, and BPN. Rel

... Show More
View Publication Preview PDF
Publication Date
Fri Sep 15 2023
Journal Name
Al-academy
The social imagination and its representations in the paintings of students of the Department of Art Education
...Show More Authors

The aim of this research is to identify how to employ the social imagination and its representations in the paintings of the students of the Department of Art Education. Students of the Department of Art Education in the light of this tool, and the researcher reached a number of results, the most important of which are:
1. The indicator of the social imagination in the excitement of the artist and the recipient, because the representations are embodied in forms within the painting and close to reality.
2. An artistic sample of the representational imagination and the creative imagination was found to be more than the imaginary imagination.
3. Individual symptoms related to the term.
4. The representations of the socia

... Show More
View Publication Preview PDF
Crossref
Publication Date
Thu Apr 18 2019
Journal Name
Al-kindy College Medical Journal
Demonstration of the value of diffusion weighted MR imaging for differentiation of benign from malignant breast lesions
...Show More Authors

Background: Radiologic evaluation of breast lesions is being achieved through several imaging modalities. Mammography has an established role in breast cancer screening and diagnosis. Still however, it shows some limitations particulary in dense breast.

Methods : Magnetic resonance imaging is an attractive tool for the diagnosis of breast tumors1 and the use of magnetic resonance imaging of the breast is rapidly increasing as this technique becomes more widely available.1 As an adjunct to mammography and ultrasound, MRI can be a valuable addition to the work-up of a breast abnormality. MRI has the advantages of providing a three-dimensional view of the breast, performing wit

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Feb 28 2023
Journal Name
Iraqi Journal Of Science
Properties of Ground-State of 17,19,20,24,26F using the Wave Functions of Harmonic-Oscillator and Spherical Hankel Functions
...Show More Authors

     The nuclear size radii, density distributions and elastic electron scattering charge form factors for Fluorine isotopes (17,19,20,24,26F) were studied using the radial wave functions (WF) of harmonic-oscillator (HO) potential and free mean field described by spherical Hankel functions (SHF) for the core and the valence parts, respectively for all aforementioned isotopes. The parameters for HO potential (size parameter ) and SHF were chosen to regenerate the available experimental size radii. It was found that using spherical Hankel functions in our work improved the calculated results quantities in comparison with empirical data.   

View Publication
Scopus (3)
Crossref (1)
Scopus Crossref
Publication Date
Sun Mar 02 2008
Journal Name
Baghdad Science Journal
Determination Of Micro Amount Of Spironolactone In Some Of Pharmaceutical Preparate By Using a Molecular Luminescence Technique.
...Show More Authors

The present study include a new developed method of analysis for determination of drug Spironolaction (SP) in some Pharmaceuticals by Spectrofluorometric method. Spironolaction was determined under optimal experimental condition that follows :- The excitation spectrum was (l=351 nm), the emmetion spectrum was (l=518 nm), pH=1, the suitable temperature for reaction 60oC and the optimal time less than (3) minute. The analysis and rang statistical data was:-Linear dynamic rang (1-10) ?g.ml-1, the detection limit (D.L = 0.023 ?g.ml-1), Molar absorptivity (? = 29875 liter mole-1 cm-1), Relative standard deviation (%RSD = 0.78), (%Erel = 3.3) and recovery (Rec = 96.6) percentage. Determination of Spironolactone was accomplished by two methods

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sun Nov 01 2015
Journal Name
Iosr J Dent Med Sci
Upsurge of cases of lichen planus in Iraqi population in Baghdad City with frequency of hepatitis viruses
...Show More Authors

KE Sharquie, AA Noaimi, AA Zeena, IOSR J Dent Med Sci, 2015 - Cited by 5

View Publication