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 Sep 15 2019
Journal Name
Al-academy
The Reality of the Artistic Direction of Illustrations in the Textbooks: امل ابراهيم محسن
...Show More Authors

The images and drawings reduce the intellectual, symbolic and cognitive dimensions inside them that make them an intermediary that imposes itself on the educational method, as they have become responsive to all the needs of the student in the modern era unlike the previous periods. The artistic direction of the illustrations in the scientific books meets the educational and pedagogical needs of the learner and their frame in an illustrative educational method that contributes in developing the student's abilities to benefit from the scientific curricula in the age of scientific and cognitive development.

Here, the researcher finds that the artistic direction of the illustrations lacks the achievement of scientific and technical p

... Show More
View Publication Preview PDF
Crossref
Publication Date
Sun Feb 03 2019
Journal Name
Iraqi Journal Of Physics
Impact of thickness and heat treatment on some physical properties of thin Cu2SnS3 films
...Show More Authors

Copper tin sulfide (Cu2SnS3) thin films have been grown on glass
substrate with different thicknesses (500, 750 and 1000) nm by flash
thermal evaporation method after prepare its alloy from their
elements with high purity. The as-deposited films were annealed at
473 K for 1h. Compositional analysis was done using Energy
dispersive spectroscopy (EDS). The microstructure of CTS powder
examined by SEM and found that the large crystal grains are shown
clearly in images. XRD investigation revealed that the alloy was
polycrystalline nature and has cubic structure with preferred
orientation along (111) plane, while as deposited films of different
thickness have amorphous structure and converted to polycrystalline

... Show More
View Publication Preview PDF
Crossref
Publication Date
Thu Jan 10 2019
Journal Name
Journal Of The College Of Education For Women
Spatial analysis of population growth in the district of Tuz Khurmatu for (1977-2012)
...Show More Authors

The study population growth of the most important demographic phenomena upon which planners to meet changes in the size of the population increase is through knowledge of the requirements of population growth can be planned for the future. On this basis, Tuz District was chosen for the study of population growth, which set her period (1977-2012), and compared with the growth of the population of the province and the extent of the variation in population growth, according to the administrative units, has touched search numerical and proportional distribution of the population according to the administrative aspects of the judiciary, as well as environmental distribution.

The elimination of the study population growth dramatically

... Show More
View Publication Preview PDF
Publication Date
Thu Aug 01 2019
Journal Name
Biochemical And Cellular Archives
PARTIAL PURIFICATION AND CHARACTERIZATION OF ACID PHOSPHATASE FROM SERA OF OBESE DIABETES MELLITUS PATIENTS
...Show More Authors

The study aimed to purification of acid phosphatase (ACP) from sera of obesetype 2 diabetes mellitus patients, this study included from thirty T2DM patients and thirty control, purification process was done with several steps included precipitation with inorganic salt (NH4 ) 2SO4 30%-80%, dialysis, ion exchange chromatography by DEAE sepharose anion column and size exclusion chromatography by Sepharose 6B.ACP, BMI, FBS, HbA1c, Lipid profile, Urea, Creatinie, Insuline, Homa-IR were determined. Results showed the precipitate and concentrated protein appeared four peaks in ion exchange column. ACP located in the first and second peak with purification fold (21.1), (37.2) yield of enzyme and specific activity (173.3) IU/ml, which obtained a si

... Show More
View Publication Preview PDF
Scopus
Publication Date
Thu Dec 31 2020
Journal Name
Pollution Research Journal
ANALYSIS OF THE HYDRAULIC CHARACTERISTICS OF AL MAHAWIL STREAM USING HECRAS: A FIELD STUDY
...Show More Authors

A water resources management for earthen canal/stream is introduced through creating a combination procedure between a field study and the scientific analytical concepts that distinguish the hydraulic problems on this type of stream with using the facilities that are available in HECRAS software; aiming to point the solutions of these problems. Al Mahawil stream is an earthen canal which is subjected to periodic changes in cross sections due to scour, deposition, and incorrect periodic dredging processes due to growth of the Ceratophyllum plants and weeds on the bed and banks of the stream; which affect the characteristics of the flow. This research aims to present a strategy of water resources management through a field study that conducte

... Show More
View Publication Preview PDF
Publication Date
Wed Jun 15 2022
Journal Name
Al-adab Journal
Linguistic features of the semantic translation of the Holy Quran from Arabic into Russian
...Show More Authors

This article discusses some linguistic problems that arise when translating the Holy Quran from Arabic to Russian. We analyze lexical, syntactic and semantic problems and support them with Examples of verses from the Qur'an, since the Qur'an is the word of Allah. It contains prayers and instructions full of both literal representations and figurative comparisons. The identification of linguistic and rhetorical features challenges translators of the Holy Qur'an, especially when translating such literary devices as metaphor, assonance, epithet, irony, repetition, polysemy, metonymy, comparisons, synonymy and homonymy. The article analyzes: metaphor, metonymy, ellipsis, polysemy.

View Publication
Crossref
Publication Date
Thu Sep 02 2021
Journal Name
International Journal Of Drug Delivery Technology
Role of Lactobacillus plantarum and Lactobacillus acidophilus as a Treatment of Cryptosporidiosis in Mice
...Show More Authors

Objective: To evaluate the therapeutic activity of probiotics mixture of Lactobacillus plantarum and Lactobacillus acidophilus towards Cryptosporidium infection in experimentally infected mice. Oocysts of Cryptosporidium were separated from the stool of humans to infect mice. Methods: Forty male albino mice were split equally into four groups, every group contained 10 mice, the group I (early treated group), were treated from the 1st day from infection to the 11th post-infection, group II (late treated group), were treated from the 4th day from infection to the 15th post-infection, and group (III) (untreated group), were mice considered as a positive control group. Results: It was showed that daily application of a mixture of L. plantarum w

... Show More
Scopus (1)
Scopus
Publication Date
Sat Sep 30 2017
Journal Name
Al-khwarizmi Engineering Journal
Implementation of Transmitter Zigbee System based on Wireless Sensor Network of IEEE 802.15.4 Standard
...Show More Authors

Abstract

 

Zigbee is considered to be one of the wireless sensor networks (WSNs) designed for short-range communications applications. It follows IEEE 802.15.4 specifications that aim to design networks with lowest cost and power consuming in addition to the minimum possible data rate. In this paper, a transmitter Zigbee system is designed based on PHY layer specifications of this standard. The modulation technique applied in this design is the offset quadrature phase shift keying (OQPSK) with half sine pulse-shaping for achieving a minimum possible amount of phase transitions. In addition, the applied spreading technique is direct sequence spread spectrum (DSSS) technique, which has

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Wed Jan 01 2020
Journal Name
Biochem. Cell. Arch.
ANATOMICAL AND CHEMICAL STUDY OF ALTHEAE OFFICINALIS L. SPREAD IN THE NORTH OF IRAQ
...Show More Authors

Scopus (3)
Scopus
Publication Date
Fri Apr 21 2023
Journal Name
Chemical Methodologies
Spectroscopic and Antimicrobial Studies of Some Metal Complexes of Furfural Schiff Base Derivative Ligand
...Show More Authors

A new furfural Schiff base derivative ligand (L-FSB) named N-(4- Bromo-2-methylphenyl)-1-(furan-2-yl)methanimine, was synthesized from the condensation reaction of furfural (fur) with 4-Bromo-2- methylaniline (bma) in 1:1molar ratio. A new series of VO(II), Cr(III), Mn(II), Co(II), Ni(II), Cu(II), Zn(II), and Cd(II) metal complexes are synthesized according to the metal content analysis in an 2:1 ligand:metal ratio. The stereochemistry of the ligand complexes have been deduced by Fourier Transform-Infra Red (FT-IR), Atomic Adsorption (A.A), Ultra violate-Visible Spectra (UV-Vis Spectra), (Mass Spectra, Proton,13Carbon-Nuclear Magnetic Resonance) (1H-NMR,13CNMR) for ligand), magnetic susceptibility at 25oC and conductivity measurements. Fr

... Show More