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
Tue Dec 01 2015
Journal Name
Journal Of Engineering
Importance of New Use of Concrete in Iraq Analysis of Development And Use of Concrete in Architecture
...Show More Authors

Since its invention by the Ancient Romans and later developed during the mid-18th century, the concrete structure and finish, has been considered as the most powerful, practical, economic and constructional material that meets the building’s architectural and aesthetical requirements. By creating unique architectural forms, the pioneer architects used concrete widely to shape up their innovative designs and buildings.

The pre-mixed ultra-high performance concrete which manufactured by Lafarge.

The transparent concrete and cement that allow the light beams to pass through them, introduces remarkable well-lit architectural spaces within the same structural criteria. This product is a recyclable, sustainab

... Show More
View Publication Preview PDF
Publication Date
Sun Aug 17 2025
Journal Name
Journal Of Baghdad College Of Dentistry
Efficacy of arthrocentesis with injection of hyaluronic acid in the treatment of internal derangement of temporomandibular joint
...Show More Authors

Background: Temporomandibular joint disorders refer to a group of heterogeneous pain and dysfunction conditions involving the masticatory system, reducing life quality of the sufferers. Arthrocentesis is simple and less invasive surgical procedure for the treatment of internal derangement than arthroscopy and better than other conservative procedures such as drugs, occlusal appliances and physiotherapy. The aim of the study was to evaluate the effect of arthrocentesis with injection of hyaluronic acid in the treatment of internal derangement of temporomandibular joint for the restoration of its function, reducing pain and preventing further deterioration of the temporomandibular joint dysfunction. Materials and methods: This study was perfo

... Show More
View Publication Preview PDF
Publication Date
Sun Feb 03 2019
Journal Name
Journal Of The College Of Education For Women
The role of thclimate in the development of the performance of the administrative bodies of sports clubs
...Show More Authors

The role of the climate in the development of the performance of the administrative bodies of sports clubs

View Publication Preview PDF
Publication Date
Sun Aug 17 2025
Journal Name
Journal Of Baghdad College Of Dentistry
The Effect of LED Light on Depth of Cure and Microhardness of Three Types of Bulkfill Composite
...Show More Authors

Background: To evaluate the ISO depth of cure of bulkfill composites and depth of cure which determined by Vickers microhardness test. Materials and Methods: Bulkfill resin composite specimens (n=150) were prepared of three bulkfill composite materials (TetricEvo Ceram, Quixfil and SDR) and light cured by Flash max p3 for 3, 10, 20 seconds and by wood pecker for 10, 20 seconds respectively, a mold was filled with one of the three bulkfill composites and light cured. The specimens removed from the mold and scraped by plastic spatula and the remaining length (absolute length) was measured which represent the ISO depth of cure. After that the specimens were returned into the mold and a microhardness indentation device applied on the specimen

... Show More
View Publication Preview PDF
Crossref
Publication Date
Fri Jan 24 2020
Journal Name
Iraqi Journal Of Agricultural Sciences
THE EFFECT OF TERMITES EXTRACT ON INHIBITION OF GROWTH OF SOME PATHOGENIC BACTERIA AND SYNTHESIS OF BIOFILM
...Show More Authors

This study was aimed to extract the effective material from the dry nests of termites and detect its antibacterial activity against some pathogenic bacterial isolates and inhibit synthesis of its biofilm. Termites dry nests were collected and the effective material was extracted then the antibacterial activity was detected using the disc diffusion assay. Results were showed that the extract have antibacterial material from the Termites dry nests, this extract showed antibacterial activity against Gram positive bacteria (Staphylococcus aureus) at (21.5mm) and Gram negative bacteria ( Enterobacter sp. and Pseudomonas aeruginosa) at (26 mm and 20 mm) respectively by inhibiting their growth, as well as its effect on biofilm production o

... Show More
View Publication
Scopus (3)
Scopus Crossref
Publication Date
Mon Oct 01 2018
Journal Name
Journal Of Educational And Psychological Researches
The Effect of PDEODE Strategy on the Acquisition of Historical Concepts of First Class of Intermediate Students
...Show More Authors

The research aims to find out the effect of PEDODE Strategy on the acquisition of historical concepts of First Intermediate Grade. To achieve this goal, the researcher has put forward this zero hypothesis: There is no statistically significant difference at the level of (05,0) between the mean of the students' marks in the experimental group who study the history subject using PEDODE strategy and that of the students' marks in the control group who study the subject according to the traditional method in the post-testing on the acquisition of historical concepts. The sample of the study consists of (62 female-students) of First Intermediate Grade in the Directorate of Baghdad Education/ Karkh2nd for the academic year 2016-2017. The sampl

... Show More
View Publication Preview PDF
Publication Date
Thu Aug 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
Development of methods of treatment of medical waste in the hospitals of Baghdad health Department / (Rusafa survey)
...Show More Authors

Purpose: To contribute to the development of an appropriate program for the management of medical waste based on clear-cut principles in order to reach the overall goal of improving the public health and environment of the population in our country.

Design / Approach / Introduction: The research is based on the analytical descriptive approach as a method of study in the field of data collection using a check list and analysis of the data through the use of some statistical treatments.

 Results: The need is to establish a medical waste management in hospitals and follow international standards in all stages of waste management from sorting, collection, transportation and treat

... Show More
View Publication Preview PDF
Crossref (1)
Crossref
Publication Date
Tue Apr 26 2016
Journal Name
Iraqi Journal Of Market Research And Consumer Protection
Study of environmental pollution to soil of power station Dezlat alJadiriyah / University of Baghdad.: Study of environmental pollution to soil of power station Dezlat alJadiriyah / University of Baghdad.
...Show More Authors

The study aimed to measure the concentration of some heavy metal elements and represented by (Pb, Cd,Cu) through the use of atomic absorption spectrometer Flame AAS-7000 type SHIMADZU underwent a process modeling to twelve samples from the soil of electricity Dezlat al Jadiriyah station in the Baghdad University compound at a depth of 30-60 cm from the surface and divided the samples into two groups first included six samples from inside the station while the second included six samples from outside the station. For the element of Pb was higher concentration reached by 29.32ppm and less concentration 17.56ppm. were elements Cd and Cu are growing and less and proportions of certain while the highest concentration of copper 9.69 ppm and le

... Show More
View Publication Preview PDF
Publication Date
Fri Feb 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
The extent of the contribution of internal marketing in the management of human talent survey study of the views of some administrative leaders at the University of Mosul
...Show More Authors

 Abstract

Investment in the human resource has become an important part of the strategies of educational organizations so that they can be competitive, so that the access of academics in universities to the international awards as a result of their research excellence indicates the effectiveness of this human talent so the interest has emerged in the implementation of a strategy to manage these human talent in organizations in general and educational ones In particular as one of the power sources  that can not be imitated. The focus of the organization on the interaction between the working people has increased attention to the human element in order to achieve the desired quality levels, which called for organi

... Show More
View Publication Preview PDF
Crossref
Publication Date
Wed Jun 01 2011
Journal Name
Journal Of Economics And Administrative Sciences
The role of the cognitive peak and its implications for achieving outstanding performanceAnalytical study of the views of a sample of the staff of the University of Baghdad
...Show More Authors

        Knowledge represents the foundation stone for the work of all organizations, are working who leads the thinking of individuals is the ability that leads to behavior based on rationality, it is the work that creates value to the organization and thus gain access to performance winning where that knowledge is a new type of capital based on the thought and experience and is the so-called intellectual capital, which is renewable and is constantly evolving. The study sought to explain the role of the climax  knowledge in achieving the highest levels of performance Organizational and then access to the performance winning in educational organizations the study sample, was found to be a co

... Show More
View Publication Preview PDF
Crossref