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Investigation of Solubility Enhancement Approaches of Ticagrelor
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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).  

 

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Publication Date
Sun Sep 07 2025
Journal Name
Alqalam Journal Of Medical And Applied Sciences
Atypical Presentation of Fibroepithelioma of Pinkus: A Case Report and Review of the Literature
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Fibroepithelioma of Pinkus (FEP) is a slowly growing, low-grade malignant tumor with very low metastatic potential that is considered a distinct variant of basal cell carcinoma (BCC). It usually manifests as sessile or polypoidal lesions on the trunk of middle-aged patients. However, it may present in younger age groups, even in children. In this case, we present a rare case of FEP atypically presenting as a scaly plaque on the lower back for several years in an elderly female who was eventually diagnosed by excisional biopsy and histopathology.

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Publication Date
Sat Mar 30 2002
Journal Name
Iraqi Journal Of Chemical And Petroleum Engineering
Effects of Drying Conditions on the Properties of Dried Particles of Powdered steep Liquor
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Publication Date
Thu Feb 01 2024
Journal Name
Baghdad Science Journal
Significance and Conservation of Birds of the Genus of Bee-eater (MEROPS) in Uzbekistan
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The purpose of this article is to identify and evaluate the importance of birds of the genus Merops (European Bee-eater -Merops apiaster and Blue-cheeked Bee-eater -Merops persicus) in Uzbekistan, as well as to develop recommendations aimed at solving some problems associated with its conservation. As a result of the study, in the aspect of biocenotic relations, the natural significance of these species was revealed. The economic value is determined and analyzed in beekeeping farms. From the study of the remains of food contained in the stomachs, throats and nests of M.apiaster, a preliminary list of the main species of the food spectrum has been compiled. Based on the bioacoustic repellent "Korshun-8"

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Publication Date
Mon Dec 25 2023
Journal Name
Journal Of Legal Sciences
The Principle of Prohibiting the Diversion of the Natural Course of International River Waters
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The research deals with the principle of the prohibition of international waterway diversion in the law of international watercourses. The research reviews individual and collective doctrinal efforts that have touched upon the principle as an internationally wrongful act because of its serious damage and consequences for downstream States. The research addresses the nature of the principle of the prohibition of diversion of international watercourses; its various effects; principles of international law establishing the principle of prohibition of diversion; and its application in State practice and international justice. This principle has been enshrined in most international treaties and judicial decisions. The principle of prohibition

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Publication Date
Tue Feb 05 2019
Journal Name
Journal Of The College Of Education For Women
Spatial contrast of the slums in the unity of the new municipal of Baghdad
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The slums one of the main problem plaguing the city of Baghdad in general and
the unity of municipality of New Baghdad, especially, where the characteristics of the study
area a prominent role in population growth and the emergence of slums where a private,
although the region suffer from the housing crisis is the lack of the number of housing units
compared to the number of families in which, With high land prices and the level of rent
which was accompanied by the absence of the law, which was followed by the year 2003, has
become the study area and one of the most municipalities of the city of Baghdad Contain
slums which took fills abandoned buildings and acquires vacant land agricultural ones and
allocated to d

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Publication Date
Fri Mar 01 2019
Journal Name
Iraqi Journal Of Physics
Determination of uranium concentrations for soil of Tigris river and rainwater of Baghdad city
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In this study, phosphorescence analysis (KPA) is used for determining soil collected from the Tigris River from Al- Karrada and Bab Al-Sharq in Baghdad and samples were taken from rainwater collected from Al-Rashad, Al-Obeidi, Al-Dora and Al-Sadr City in Baghdad. The measurements were carried out by the Iraqi Ministry of Health and Environment, in the Radiation Protection Center. The collection, removal and evaporation of the samples ranged from January to the end of March 2018. The results show the presents of concentration of 238U and 235U in soil samples and the rainwater samples. The conclusion of this work is the concentration of uranium in soil samples is more than recommendations by ICRP value of 1.9 μg /l. While all water sample

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Publication Date
Wed Nov 13 2019
Journal Name
Al-kindy College Medical Journal
Outcome Of Surgical Treatment Of Tuberculosis Of The Spine In Patients With Motor Deficits
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Background: Significant numbers of patients with spinal tuberculosis (TB), especially in developing countries, still present late after disease onset with severe neurological deficits.

Objective:This study was conducted to assess the outcome of surgery in patients with tuberculosis of the spine with motor deficits.

Type of the study: Retrospective study.

Methods: We retrospectively analyzed data obtained in all the patients with severe motor deficits due to spinal TB admitted to and surgically treated in four hospitals in Baghdad/Iraq during the period from January 2012 to January 2014. History, examination, imaging, histological, postoperative, a

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Publication Date
Thu Jun 18 2015
Journal Name
Journal Of Kerbala University
Effect of Carbamazepine drug on formation of decidual tissue in femal of Mus musculus
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Implantation of blastocyst is considered as a sensitive process in the life of growing embryo. Thus this critical period could be under threat from the harmful effect of many drugs ,among them is the carbamazepine which is used by many women for a treatment of epilepsy . The present experiment was designed to study the effect of this drug on the process of implantation ;especially during the days 7 and 9 of pregnancy. For those purpose 169 pregnant albino mice, of 25 gm weight for each one, were used .The mice were divided into control group given orally normal saline, and treated group given orally carbamazepine with concentration of 15 mg\kg. Samples from pregnant uteri containing the embryos were used. They were first fixed in Boun's sol

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Publication Date
Sat Jul 01 2000
Journal Name
Bulletin Of The Iraq Natural History Museum (p-issn: 1017-8678 , E-issn: 2311-9799)
UTTILIZATION OF LIPIDS AS SOURCE OF ENERGY DURING HIBERNATION OF RANA RIDIBUNDA PALLAS, 1771
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The aim of this study is to calculate the ene expenditure from fatty substance contents of the
frog. Rana ridibunda during its hibernation. It was found that, almost, all frogs enter
hibernation during the last week of December and emerge from hibernation during the first
week of March. Hence, January and February are considered the hibernation period.
December is the pre-hibernation period and March is the post-hibernation period. The
reduction in percent of body lipid during the hibernation period was 4.8% in males and 7.7%
in females. The reduction in percent of lipid of fat bodies during the hibernation period was
2.758% in males and 0.733% in females.
The calorific value of R. ridibunda lipid amounted to 1233

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Publication Date
Mon Aug 30 2021
Journal Name
Al-kindy College Medical Journal
Quality of Life of Parents of Children with Type I Diabetes Mellitus, Baghdad 2017
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Background: Diabetes is defined by the World Health Organization as a metabolic disorder characterized by chronic hyperglycemia with disturbances of carbohydrate, fat and protein metabolism resulting from defects in insulin secretion, insulin action, or both. Families are co-regulating systems in which the stresses and strains of one family member affect the well-being of another member of the family. Caregivers of children with chronic illness report experiencing more parental stress than parents of healthy children.

Objective: A descriptive cross-sectional study had been conducted in four centers of endocrine diseases in Baghdad city and data was collected by using self-administered questionnaire regarding qua

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