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
Fri Mar 17 2017
Journal Name
Ibn Al-haitham Journal For Pure And Applied Sciences
Synthesis and Characterization of [N-(4-Methoxybenzoyl amino)-thioxomethyl ]Methionine acid (MbM) and It's Complexes with Some Divalent Transition Metals Ions (Mn , Co , Ni , Cu , Zn , Cd and Hg)
...Show More Authors

In this work , the ligand [N-(4-Methoxybenzoyl amino)-thioxomethyl] Methionine acid  has been synthesized by the reaction of 4- Methoxybenzoyl isothiocyanate with methionine acid . The metal complexes were prepared through the reaction of metals chlorides of Co(II) , Ni(II), Cu(II), Zn(II) and Cd(II) in ethanol as solvent . The ligand (MbM) and its metal complexes have been characterized by elemental analysis (CHNS), IR, 1H-13CNMR and UV- Vis spectra, magnetic susceptibility measurements, molar conductivity, melting points and atomic absorption. The metal-ligand ratio was determined by mole ratio method. The suggested structures for the Co(II), Ni(II), Cd(II) and Zn(II) complexes are tetrahedral geometry and  the Cu(II) complex

... Show More
View Publication Preview PDF
Publication Date
Fri Dec 01 2023
Journal Name
Baghdad Science Journal
Determining ACE-2 Level and Some Relevant Biochemical Parameters and studying the effect of Gender in Iraqi Diabetic Patients with Glomeruli and Renal Tubules Fibrosis as Early Prediction Marker
...Show More Authors

     Diabetic kidney disease is an illness of the glomerulus that interferes with the glomerular filtration barrier (GFB), which is worked to enable kidney to selective purification of water and solutes in addition to limiting the movement of large macromolecules such as albumin. In the glomerular endothelium, mesangial cells, foot cells, and the brush border of the proximal tubules, ACE-2 is expressed and that the kidneys represent the highest-expressing region of this enzyme. Thus, the current study aimed to evaluate ACE-2 level in this case compared to healthy condition. The study Conducted with 120 male and female ranging in age (30-65) years old. Ninety patients with type 2 diabetes subdivided into three groups on the basis of A

... Show More
View Publication Preview PDF
Scopus (3)
Scopus Crossref
Publication Date
Sun Mar 03 2024
Journal Name
Nasaq
Types and functions of comparisons (based on Russian and Arabic phraseological units) Типы и функции сравнений (на материале русских и арабских фразеологизмов) انواع ووظائف المقارنات )في االمثال الروسية والعربية
...Show More Authors

Comparison is the most common and effective technique for human thinking: the human mind always judges something new based on its comparison with similar things that are already known. Therefore, literary comparisons are always clear and convincing. In our daily lives, we are constantly forced to compare different things in terms of quantity, quality, or other aspects. It is known that comparisons are used in literature in order for speech to be clear and effective, but when these comparisons are used in everyday speech, it is in order to convey the meaning directly and quickly, because many of these expressions used daily are comparisons. In our research, we discussed this comparison as a means of metaphor and expression in Russia

... Show More
Publication Date
Thu Dec 31 2015
Journal Name
Al-khwarizmi Engineering Journal
Design and Construction of Electrical Magnate to Study its Efficiency and the Optimum Parameters to Produce Alkaline Magnetic Water and Treating the Sea Water to be Suitable for Irrigation
...Show More Authors

Abstract

Electrical magnate  was designed and constructed,  the optimum Magnetic flux  and the effect of time on the physical properties of the alkaline (magnetic water) produced from the bottled drinking water [the total dissolved solids (TDS) or the electrical conductivity, and pH] were studied, to simulate ZamZam water in Mekka Saudi Arabia. Also, the efficiency of magnetic field from this designed electrical magnate in decreasing the TDS of sea water (of 1500 ppm NaCl Content), to convert it to water suitable for irrigation (TDS<1000 ppm) was investigated in this work.The results show that the magnetic flux from our designed electrical magnate in the range of (0.013- 0.08) Tesla and 30 minut

... Show More
View Publication Preview PDF
Publication Date
Sun Mar 06 2011
Journal Name
Baghdad Science Journal
Isolation and Identification of Vibrio cholerae causes Epidemic cholera 2007 in Iraq by Rapid Method (Immunochromatographic one step rapid visual test) and comparing it with the traditional Bacterlogical Methods
...Show More Authors

This study was for searching for Cholera Bacteria serotype which causes epidemiology Cholera in the 2007 in a fast method which contains (Rapid Visual Test) (Crystal V.C.) which was used for the first time in Iraq to diagnosis of Cholera Bacteria & compared with the traditional bacteriology method. The Cholera disease is one of the most dangerous epidemiological diseases which lead to death with a percentage of (50 – 70) % in the severe cases for untreated patients . For this purpose, 100 samples of stool from the patients from a (13) hospitals in Baghdad Governorate in the period from August to the end of December. The Cholera was diagnosis in two methods, 1st method was the fast method using the nitrocellulose which is coated with anti-

... Show More
View Publication Preview PDF
Crossref
Publication Date
Tue Jun 15 2021
Journal Name
Al-academy
Shorthand the representative performance in the theatrical festival performances of the education teams for teachers in primary schools , in secondary schools and artistic supervisors 2019 AD: خضر عبد خضير
...Show More Authors

Arts acts to reduce and exclude everything that is not necessary in the delivery of meaning, especially representative performance, which is based on the intensification of the physical and vocal actions, and in drawing the dimensions of the character. And because that, the artistic staff, among others in the ministry of education, are considered the cornerstone, in the development of theatrical activities in schools, this research came to find out the extent to which teachers in primary schools, in secondary schools and artistic supervisors rely on shorthand mechanisms in the representative performance.
The current research relied on the descriptive approach, in analyzing his sample, which was deliberately chosen, Among the most imp

... Show More
View Publication Preview PDF
Crossref
Publication Date
Mon Jun 01 2015
Journal Name
Journal Of The College Of Languages (jcl)
Das literarische Bild und die sprachliche Struktur der Sprichwörter bei der gegenseitigen Übersetzung im Deutschen und Arabischen The literary image in the translation of the German and Arabic proverbs
...Show More Authors

Vorwort:

                              Die Übersetzung gilt in der Vergangenheit als Brücke zwischen  verschiedenen Gesellschaften. Sie spielt eine große Rolle im Bereich Kulturaustausch der Länder. Die Araber haben das früh betrachtet, und die Übersetzung als Wissenschaft wird eine der wichtigsten Lehren. Viele griechische Wissenschaften waren durch Übersetzung in den arabischen Ländern bekannt.

In dieser Forschung findet man einen Überblick über die Wichtigkeit der Sprichwörterübersetzung und welche Rolle spielt diese Übersetzung im Z

... Show More
View Publication Preview PDF
Publication Date
Thu Dec 29 2022
Journal Name
Journal Of The College Of Languages (jcl)
The morphological structure of nouns and verbs in the novel "Astonishment" by the novelist Aharon Applefield, Morphological study.: מבנה שמות עצם והפעלים ברומן תימהון לסופר אהרון אפלפלד עיון מורפולוגי
...Show More Authors

This research sheds light on the morphological structure of nouns and verbs in the novel "ASTONISHMENT" by the novelist Aharon Applefield by analysing selected models from the novel in a morphological analysis in order to identify the most important morphological features of this structure according to a statistical analytical approach.

 The morphological structure is the main pillar of the linguistic structure of the literary text. Morphology is the science that studies the word, by which its structure and original letters are known, and the change that has occurred to it.  The aesthetics of the fictional text is reflected in this structure, through which the writer conveys his ideas and narrations to the reader.  The research

... Show More
View Publication Preview PDF
Crossref
Publication Date
Fri Sep 20 2024
Journal Name
Journal Of Nano Research
Impact of Copper Doping on Nanocrystalline SnO&lt;sub&gt;2&lt;/sub&gt; Thin Films Synthesized by Sol-Gel Coating and Chemical Bath Deposition for Gas Sensor Applications
...Show More Authors

This work focuses on the preparation of pure nanocrystalline SnO2 and SnO2:Cu thin films on cleaned glass substrates utilizing a sol-gel spin coating and chemical bath deposition (CBD) procedures. The primary aim of this study is to investigate the possible use of these thin films in the context of gas sensor applications. The films underwent annealing in an air environment at a temperature of 500 C for duration of 60 minutes. The thickness of the film that was deposited may be estimated to be around 300 nm. The investigation included an examination of the structural, optical, electrical, and sensing characteristics, which were explored across various preparation circumstances, specifically focusing on varied

... Show More
View Publication
Scopus (1)
Scopus Clarivate Crossref
Publication Date
Sun Mar 01 2020
Journal Name
Iop Conference Series: Materials Science And Engineering
The Influence of x ratio and Annealing Temperatures on Structural and Optical Properties for (CuO)<sub>x</sub>(ZnO)<sub>1-x</sub> Composite Thin Films Prepared by PLD
...Show More Authors
Abstract<p>Thin films of (CuO)<sub>x</sub>(ZnO)<sub>1-x</sub> composite were prepared by pulsed laser deposition technique and x ratio of 0≤ x ≤ 0.8 on clean corning glass substrate at room temperatures (RT) and annealed at 373 and 473K. The X-ray diffraction (XRD) analysis indicated that all prepared films have polycrystalline nature and the phase change from ZnO hexagonal wurtzite to CuO monoclinic structure with increasing x ratio. The deposited films were optically characterized by UV-VIS spectroscopy. The optical measurements showed that (CuO)<sub>x</sub>(ZnO)<sub>1-x</sub> films have direct energy gap. The energy band gaps of prepared thin films </p> ... Show More
View Publication
Scopus (5)
Crossref (4)
Scopus Crossref