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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
Wed Jun 01 2016
Journal Name
Journal Of Economics And Administrative Sciences
Assessing the financial performance of the Chambers of the municipalities of Babylon , Karbala ,applied research comparative ((Search unsheathed))
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Abstract
             Shorten the research problem that there is no system or model to evaluate the financial performance of the departments of municipalities where it is not possible for a person or institution both to know or to know their success in terms of the financial work of failure and where it is now than those without assessing the financial performed, authorized to be and necessities FATF is the financial performance assessment, which is the work unfinished aspects without Hence the work came in this study to study and diagnose and analyze financial data in a sample of municipal departments in order to develop a model to assess the financ

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Publication Date
Thu Feb 12 2026
Journal Name
Journal Of Baghdad College Of Dentistry
Histological evaluation of the effect of topical application of Curcumin powder and essential oil on skin wound healing
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Background: Herbal medicine can be called one of the branches of medicine in various forms. Turmericcurcumin has proved its efficiencies a coloring, flavoring agent and has been traditionally used in medicine, exhibiting remarkable anti-inflammatory and antioxidant properties. The varied biological properties of curcumin and lack of toxicity even when administered at higher doses makes it attractive to explore its use in various disorders like diseases of skin. It is good potential agent for wound healing. Materials and methods: Sixty four new Zealand rabbits were used in this study ,they were divided into four groups,each group was subdivided as follows:Experimental groups(8 rabbits) right facial side of animals for essential oil applicati

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Publication Date
Sat Jun 18 2022
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Evaluation of the Detrimental Effects of some Antiepileptic Drugs on the Height and Weight of Children with Epilepsy
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Growth is a multifactorial process influenced by genetic, nutritional, hormonal, psychosocial and other factors including the general health of a child. Epilepsy defined as a chronic condition characterized by recurrent clinical events or epileptic seizures, which occur in the absence of a metabolic or toxic disease the drugs that use in the treatment of this condition can affect patients growth due to their mechanisms of action. This study aimed to evaluate the effect of some antiepileptic drugs on growth (height and weight) in children with epilepsy. This work involved 51 newly diagnosed children with a different form of epilepsy (Generalized, absent and partial). Patients divided into three groups according to the treatment (group one

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Publication Date
Wed Dec 12 2018
Journal Name
Iraqi National Journal Of Nursing Specialties
Study of Gender Differences in Health Promoting Behaviors for a Sample of Students Attending Institute of Technology, Baquba
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Objective: To find out any gender differences in health promoting behaviors for a sample of students attending Institute of Technology/ Baquba. Methodology: An analytical, cross-sectional study conducted randomly for a sample of students attending Technical Institute/ Baquba, during the period from 10th November 2015 to 10th April 2016. A questionnaire used to collecting data, this questionnaire was consisted from two domains related to health promoting behaviors including (Dietary domain and domain of some daily life activities like sleep duration, rise time, bedtime and walking period per week). The

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Publication Date
Thu Mar 14 2013
Journal Name
Journal Of Kerbala University 11 (3)‏
Effect of chemical fertilization and gibberellic acid on the contentofsomechemical compounds of Nepali and Khudairi cultivars of olive‏
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Publication Date
Sun Jan 01 2023
Journal Name
Journal Of Population Therapeutics And Clinical Pharmacology
Evaluation of the Expression of RCC and KIM-1 Biomarkers in Nephrotoxicity of Rabbits Treated with Ochratoxins A
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Publication Date
Sat Jun 01 2019
Journal Name
Journal Of Economics And Administrative Sciences
Diagnosis of factors affecting the strategic implementation of sewage projects ( Case study in General Directorate of sewage projects )
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  This  Research aim to identify the factors affecting the strategic implementation of sewage projects and to seek to activate the real follow-up of projects to identify the factors that accompany their implementation, The study included a sample of the projects of the investment plan implemented for the Directorate General of sewage in the governorates of Iraq, which was completed during the six years period (2010-2016). The sample of the research was four projects: The project of implementation and processing of the treatment plant and the lifting station and the conveyor line for the project of IMARA/The third stage/Al-Sanaf marshland , The project of the processing and implementation of the treatment plant with the

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Publication Date
Tue Jun 15 2021
Journal Name
Al-academy
The authority of identification and alienation of existence in the theater of the oppressed: عبلة عباس خضير التميمي
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This research is represented by exploring the experience of "the theater of the oppressed" by (Augusto Boal) as an experiment that represents a different aesthetic pattern in the presentation of theatrical performance which is in contrast with the Aristotelian and Brechtian patterns, and as a result of the increasing problems of the individual in societies according to his needs and an attempt to express the suffering of human and the loss of his rights in general.
The research also tries to uncover the power of identification and the alienation of existence in the theater of the oppressed as that power, with its diversity of legal, legitimate, religious, political, economic and social capabilities has become a burden instead of being

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Publication Date
Thu Nov 21 2019
Journal Name
Al-kindy College Medical Journal
The The Role of Breast Sonography and Ductography in the Evaluation of Different Causes of the Nipple Discharge
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ABSTRACT

 

Background : The aim of this work is to assess the role of breast sonography  and ductography in the evaluation of different causes of nipple discharge.

Methods :  The study will be carried out on twenty-five female patients referred to the Radiodiagnosis department at Alexandria Main University Hospital presenting with nipple discharge.

They were divided into two groups:

Group I include 10 patients (40%) with surgically significant nipple discharge who were the patients with unilateral, uniorificial surgically significant colour type nipple discharge .They were investigated by mammography, sonography, and ductography.

Group II include 15 patients

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Publication Date
Wed Jul 17 2024
Journal Name
Healthcare
Impact of Nonsurgical Periodontal Treatment of Periodontitis Stages 2 and 3 on Oral Health-Related Quality of Life
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This study investigates the impact of nonsurgical periodontal treatment (NSPT) on oral health-related quality of life (OHRQoL) in patients with periodontitis stages (S)2 and S3, and the factors associated with the prediction of patient-reported outcomes. Periodontitis patients (n = 68) with moderately deep periodontal pockets were recruited. Responses to the Oral Health Impact Profile (OHIP)-14 questionnaire and clinical parameters including plaque index, bleeding on probing (BOP), probing pocket depth (PPD), and clinical attachment loss (CAL) were recorded. All patients received supra- and subgingival professional mechanical plaque removal. All clinical parameters and questionnaire responses were recorded again 3 months after NSPT.

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