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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 Dec 05 2010
Journal Name
Baghdad Science Journal
Measuring the concentration of some hormones in patients sera of polycystic ovaries
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Extensive evaluation of 76 women with polycystic ovary syndrome compared with 25 fertile women as control group was achieved by routine investigations and hormonal study of each female which were done in one period during the menstrual cycle. Then the women with PCOS have been divided into 2 groups according to their menstrual cycle (irregular menstrual cycle) during assessing their hormonal profiles as follow:- 1- (54) Patients with oligomenorrhea. 2- (22) Patients with menorrhea. This study shows that the women with PCOs have different clinical features taken from a history of disease of all of the women. Those features were distributed as follow: 57.92% of them suffer from hirsutism. 19.24% suffer from irregular menstr

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Publication Date
Wed Jun 04 2025
Journal Name
Journal Of Discrete Mathematical Sciences And Cryptography
Some properties of the result involution graph of Harada-Norton group HN
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Assume that G ≅ HN the Harada–Norton group. In this paper, effective investment for the graph ΓRI HN standard features to acquire meaningful algebraic results for the graph ΓRI HN and its corresponding group HN. For instance, marketing a modern methods to understand the way of create a precise small subgroups in G. Furthermore, performing a full investigation for getting particular ΓRI HN parameters.

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Publication Date
Wed Jan 01 2020
Journal Name
Journal Of Southwest Jiaotong University
Evaluation of Photovoltaic Solar Power of a Dual-Axis Solar Tracking System
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In this research project, a tip-tilting angle of a photovoltaic solar cell was developed to increase generated electrical power output. An active, accurate, and simple dual-axis tracking system was designed by using an Arduino Uno microprocessor. The system consisted of two sections: software and apparatus (hardware). It was modified by using a group of light-dependent resistor sensors, and two DC servo motors were utilized to rotate the solar panel to a location with maximum sunlight. These components were arranged in a mechanical configuration with the gearbox. The three locations of the solar cell were chosen according to the tilt angle values, at zero angles, which included an optimal 33-degree angle for the Baghdad location and

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Publication Date
Mon Jun 15 2020
Journal Name
Journal Of Baghdad College Of Dentistry
Effect of plasma treatment on some surface properties of acrylic resin polymer
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Background: Polymer surfaces usually present problems in bonding and finishing due to their low hydrophilicity. The aim of this study is to investigate the effect of plasma treatment with the use of two types of gases (oxygen and argon) on surface roughness, and chemical surface properties of acrylic resin denture base polymer material. Materials and Methods: Three heat cured acrylic resin specimens of (2*8*30 mm) dimensions were prepared for each test carried out in this study. Two tests were conducted, surface roughness test and chemical surface analysis test. Results: Application of plasma treatment increased surface roughness for both oxygen and argon plasma treated acrylic resin specimen groups compared with control untreated group,

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Publication Date
Sun Jun 21 2020
Journal Name
Baghdad Science Journal
Synthesis of C60 Nanotube from Pyrolysis of Plastic Waste (Polypropylene) with Catalyst
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Fullerene nanotube was synthesized in this research by pyrolysis of plastic waste Polypropylene (PP) at 1000 ° C for two hours in a closed reactor made from stainless steel using molybdenum oxide (MoO3) as a catalyst and nitrogen gas. The resultant carbon was purified and characterized by energy dispersive X-ray spectroscopy (EDX), X-ray powder diffraction (XRD). The surface characteristics of C60 nanotubes were observed with the Field emission scanning electron microscopy (FESEM). The carbon is evenly spread and has the highest concentration from SEM-EDX characterization. The result of XRD and FESEM shows that C60 nanotubes are present in Nano figures, synthesized at 1000 ° C and with pyrolysis tempera

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Publication Date
Thu Mar 30 2017
Journal Name
Iraqi Journal Of Pharmaceutical Sciences ( P-issn 1683 - 3597 E-issn 2521 - 3512)
Preparation of a New Dosage Form of Metoclopramide Hydrochloride as Orodispersible Tablet
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Metoclopramide HCl (MTB) is a potent antiemetic drug used for the treatment of nausea and vomiting. Many trials were made to prepare a satisfactory MTB orodispersible tablet using direct compression method.Various super disintegrants were used in this study which are croscarmellose sodium (CCS), sodium starch glycolate (SSG) and crospovidone (CP). The latter was the best in terms of showing the fastest disintegration time in the mouth.Among the different diluents utilized, it was found that a combination of microcrystalline cellulose PH101 (MCC 101), mannitol, dicalcium phosphate dihydrate (DPD) and Glycine was the best in preparing MTB orodispersible tablet with fastest disintegration time in the mouth.The physical parameters of the pre

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Publication Date
Sun Aug 25 2019
Journal Name
Journal Of University Of Babylon For Engineering Sciences
Observation of Consolidation and Permeability Parameters of Soil Stabilized By Cutback Asphalt
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For design purposes, it`s necessary to know the compression rate of soil layers which might be happened when it`s subjected to effective stresses. Also, it`s essential to know the rate of flow through soil mass specially for the design of marine structures or earth embankment. These two important behavior could be predicted from the coefficient of consolidation (Cv) and the coefficient of permeability (k). This study shows the effect of cutback asphalt stabilization on Cv and k and other compressibility factors, the investigation was done for silty clay samples, specimens were prepared by mixing the soil with different percentage of asphalt from (0-10)% and subjected to one-dimensional consolidation test of 50mm diameter and 20mm height wer

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Publication Date
Mon Jun 01 2009
Journal Name
Al-khwarizmi Engineering Journal
Automatic Optimization System of Cutting Condition for Different Types of Machining Processes
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This research aims at calculating the optimum cutting condition for various types of machining methods, assisted by computers, (the computer program in this research is designed to solve linear programs; the program is written in v. basic language). The program obtains the results automatically, this occur through entering the preliminary information about the work piece and the operating condition, the program makes the calculation actually by solving a group of experimental relations, depending on the type of machining method (turning, milling, drilling). The program was transferred to package and group of windows to facilitate the use; it will automatically print the initial input and optimal solution, and thus reduce the effort and t

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Publication Date
Thu Apr 13 2017
Journal Name
Journal Of Multidisciplinary Engineering Science Studies (jmess)
The Effect Of Thickness On Some Physical Properties Of CdSe Thin Films
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Publication Date
Wed Mar 10 2021
Journal Name
Baghdad Science Journal
The Effect of Preservation on the Shelf Life of Laboratory Processed Biscuit
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This study has been conducted to investigate the influence of preservatives(sodium propionate and potassium sorbate) at different levels to extend the storage life of laboratory processed biscuit.The results have shown that When%0.10 sodium propionate was added bacteria and fungi was not found for three months while found in the fourth month of storage.However bacteria and mold didnot grow until the sixth month of storage as %0.20 and %0.30 concentration was used. On the other side as %0.03 potassium sorbate was used,the growth of bacteria was cheched for 3 months and 4 months for molds..When %0.06 potassium sorbate was used no growth of bacterial or mold was found until the sixth month of storage . Three types of bacteria have been appeare

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