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 Jan 01 2023
Journal Name
Journal Of Namibian Studies
The Effect of Investment Risks on the Efficiency of Stock Pricing - Analytical Research
...Show More Authors

The research aims to know the effect of investment risks measured by the beta coefficient on the efficiency of stock pricing measured by the pricing error. The research was applied in the banks listed in the Iraq market for the period (2017-2020). That affects the value of the shares of the companies listed in it and the risks associated with it, as the risks are a dynamic process that changes over time depending on the variables that affect the general development of the economy, so these fluctuations should be taken into account to achieve maximizing returns and reducing risks and what is reflected in stock prices in the Iraqi markets Securities, through which the following question was asked: How does investment risk affect the efficienc

... Show More
Publication Date
Thu Sep 03 2020
Journal Name
Al-kindy College Medical Journal
Unusual Location of Giant Cell Tumor of the Tendon Sheath .. A Case Report
...Show More Authors

Locking of the knee is a one of the commonest orthopedic outpatient presentation. This patient usually need magnetic resonance imaging (MRI) when there is suspected lesion in the soft tissue clinically. Meniscal tears is the first differential diagnosis when accompany with painful knee. (1, 2)Giant cell tumor (GCT) is benign a localized nodular tenosynovitis often occur in the tendon sheath , Mostly involve the hand tendons in middle age group between 30 and 50 years old , female affect more than male.(3,4) The WHO defines two well-known kinds of giant cell tumor: (1) pigmented villonodular synovitis ( generalized type), which mainly involve the joints of the lower limb and (2) giant cell tumor of the tendon sheath ( localized type)

... Show More
Preview PDF
Crossref
Publication Date
Tue Oct 01 2024
Journal Name
Assiut Veterinary Medical Journal
DETECTION OF ANTIMICROBIAL RESISTANCE OF LISTERIA MONOCYTOGENES ISOLATED FROM ABORTED COWS IN IRAQ
...Show More Authors

Listeria spp. is one of the abortion causative agents in animals, especially in ruminants. This work aimed to detect Listeria spp. in milk and aborted fetus cows in Iraq. A total of 50 organ samples from aborted cow fetuses, including (brain, liver, and spleen), and 50 milk samples from the same aborted cows were collected from Baghdad farms, Iraq from (October 2023- March 2024). The bacteria were identified by conventional culture methods, biochemical tests, and the VITEK2 compact system, followed by molecular confirmation. The antimicrobial resistance pattern assay was performed using the disc diffusion method against eight antibiotic agents, and the L.monocytogenes virulence genes involving prfA,actA, and hylA genes were detected using t

... Show More
View Publication
Scopus (1)
Crossref (1)
Scopus Crossref
Publication Date
Mon Mar 01 2021
Journal Name
Al-khwarizmi Engineering Journal
Influence of Aging Heat Treatment on Pitting Corrosion Resistance of Martensitic Stainless Steel
...Show More Authors

In this research is to study the influence of the aging heat treatment on the pitting corrosion resistance of martensitic stainless steel (MSS), where a number of specimens from martensitic stainless steel were subjected to solution treatment at 1100 oC for one hour followed by water quenching then aging in the temperatures range (500-750) oC for different holding times (1,5,10,15&20) hr. Accelerated chemical corrosion test and immersion chemical corrosion test were performed on samples after heat treatment. The results of the research showed that the pitting corrosion resistance is significantly affected by the aging temperature. Where found that the aging samples at a temperature of 500 °C have the highest ra

... Show More
View Publication Preview PDF
Scopus (3)
Crossref (1)
Scopus Crossref
Publication Date
Fri Nov 09 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Impact of Training Program Upon Nurse-Midwives’ Practices Concerning Third Stage of Labor
...Show More Authors

Objective: The aim of this study is to identify the impact of training education program applied on
nurse-midwife practice concerning care during third stage of labor in labor room. Examine the
relationship between their knowledge regarding practices and some Demographic information’s.
Methodology: A quasi-experimental design conducted on non-probability (purposive) sample of fifty
two nurse-midwives selected during period from3
th August to 10thNovember 2011. The study is
conducted at the Ministry of Health (Baghdad health directorate in Al-Karhk and Al-Risafa sector) in
four hospitals. The questionnaire form is consisted of three parts which included demographic data,
knowledge concerning practice during third

... Show More
View Publication Preview PDF
Publication Date
Wed Oct 04 2023
Journal Name
Journal Of Al-qadisiya In Arts And Educational Sciences
The use of the digital book and the future of the paper book
...Show More Authors

The current research aims to know the complementary use of the paper book and the digital book by defining the paper book and the digital book and knowing the methods and methods of obtaining each of them and indicating the extent of their use and for what purpose and knowing the difficulties that researchers face in using each of them and which is better using the paper book or the digital book in preparing research Studies and for no reason. The research relied on the descriptive approach and the questionnaire as a tool for data collection, and it was distributed to professors and students of Iraqi universities. The research sample reached (219) individuals and reached a set of results, the most important of which are: Preference for the

... Show More
View Publication Preview PDF
Publication Date
Mon Jul 01 2019
Journal Name
Iop Conference Series: Materials Science And Engineering
Characteristic Zero Resolution of Weyl Module in the Case of the Partition (8,7,3)
...Show More Authors
Abstract<p>In this paper, we studied the resolution of Weyl module for characteristic zero in the case of partition (8,7,3) by using mapping Cone which enables us to get the results without depended on the resolution of Weyl module for characteristic free for the same partition.</p>
View Publication
Scopus (16)
Crossref (2)
Scopus Crossref
Publication Date
Thu Mar 19 2015
Journal Name
Al-academy
The importance of social acceptability of the universal design: عبد الكريم علي حسين
...Show More Authors

The industrial development and raise the level of income that has emerged clearly in the middle of the last century in many rich and medium rich countries has great influence on the risen of the health care level. Which led to a significant increase in the reconstruction of people over 65 years and this in turn has produced markets for products and services through modifications to the existing products to meet their physical needs. The importance of research also has the universal design of a comprehensive actually so that it covers as much as possible from human physical & cultural activities. The importance of research locally is to concentrate on this subject who has not been taken into consideration so far to accommodate the eld

... Show More
View Publication Preview PDF
Crossref
Publication Date
Mon Apr 01 2024
Journal Name
Iraqi Postgraduate Medical Journal
Estimation of Prevalence rate of Sjogren’s syndrome among Rheumatology clinic patients in Iraq
...Show More Authors

View Publication
Crossref
Publication Date
Fri May 01 2020
Journal Name
Journal Of Physics: Conference Series
Recent modification of Homotopy perturbation method for solving system of third order PDEs
...Show More Authors

This paper presents new modification of HPM to solve system of 3 rd order PDEs with initial condition, for finding suitable accurate solutions in a wider domain.

Scopus (19)
Scopus