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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
Tue Jul 19 2022
Journal Name
Arabian Journal For Science And Engineering
Investigation of the Impacts of Nanomaterials on the Micromechanical Properties of Gypseous Soils
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Publication Date
Fri Oct 01 2010
Journal Name
Iraqi Journal Of Physics
Investigation of plasma characteristics of center region of post cylindrical magnetron sputtering device
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A d.c. magnetron sputtering system was designed and fabricated. The chamber of this system is consisted from two copper coaxial cylinders. The inner one used as the cathode and the outer one used as anode with magnetic coil located on the outer cylinder (anode). The axial behavior of the magnetic field strength along the cathode surface for various coil current (from 2A to 14A) are shown. The results of this work are investigated by three cylindrical Langmuir probes that have different diameters that are 2.2mm, 1mm, and 0.45mm. The results of these probes show that, there are two Maxwellian electron groups appear in the central region. As well as, the density of electron and ion decreases with increases of magnetic field strengths.

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Publication Date
Sun Jan 10 2016
Journal Name
British Journal Of Applied Science & Technology
Illumination - Invariant Facial Components Extraction Using Adaptive Contrast Enhancement Methods
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The process of accurate localization of the basic components of human faces (i.e., eyebrows, eyes, nose, mouth, etc.) from images is an important step in face processing techniques like face tracking, facial expression recognition or face recognition. However, it is a challenging task due to the variations in scale, orientation, pose, facial expressions, partial occlusions and lighting conditions. In the current paper, a scheme includes the method of three-hierarchal stages for facial components extraction is presented; it works regardless of illumination variance. Adaptive linear contrast enhancement methods like gamma correction and contrast stretching are used to simulate the variance in light condition among images. As testing material

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Publication Date
Thu Dec 01 2022
Journal Name
Baghdad Science Journal
Enhancement Ear-based Biometric System Using a Modified AdaBoost Method
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          The primary objective of this paper is to improve a biometric authentication and classification model using the ear as a distinct part of the face since it is unchanged with time and unaffected by facial expressions. The proposed model is a new scenario for enhancing ear recognition accuracy via modifying the AdaBoost algorithm to optimize adaptive learning. To overcome the limitation of image illumination, occlusion, and problems of image registration, the Scale-invariant feature transform technique was used to extract features. Various consecutive phases were used to improve classification accuracy. These phases are image acquisition, preprocessing, filtering, smoothing, and feature extraction. To assess the proposed

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Publication Date
Sun Jun 01 2014
Journal Name
Baghdad Science Journal
Computer aided photographic memory enhancement and speed reading (case study)
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This work aimed to design and testing of a computer program – based eyeQ improvement, photographic memory enhancement, and speed reading to match the reading speed 150 – 250 word per minute (WPM) with the mind ability of processing and eye snap shooting 5000WPM . The package designed based on Visual Basic 6. The efficiency of the designed program was tested on a 10 persons with different levels of education and ages and the results show an increase in their reading speed of approximately 25% in the first month of training with noticeable enhancement in the memory as well as an increase in the ability to read for longer time without feeling nerves or boring, a nonlinear continuously increase in reading speed is assured after the first mo

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Publication Date
Fri Jul 12 2024
Journal Name
Aaps Pharmscitech
Nanosuspension-Based Repaglinide Fast-Dissolving Buccal Film for Dissolution Enhancement
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Drug solubility and dissolution remain a significant challenge in pharmaceutical formulations. This study aimed to formulate and evaluate repanglinide (RPG) nanosuspension-based buccal fast-dissolving films (BDFs) for dissolution enhancement. RPG nanosuspension was prepared by the antisolvent-precipitation method using multiple hydrophilic polymers, including soluplus®, polyvinyl alcohol, polyvinyl pyrrolidine, poloxamers, and hydroxyl propyl methyl cellulose. The nanosuspension was then directly loaded into BDFs using the solvent casting technique. Twelve formulas were prepared with a particle size range of 81.6-1389 nm and PDI 0.002-1 for the different polymers. Nanosuspensions prepared with soluplus showed a favored mean particle size o

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Publication Date
Sun Jan 01 2017
Journal Name
Ieee Access
Low-Distortion MMSE Speech Enhancement Estimator Based on Laplacian Prior
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Publication Date
Sun Mar 01 2026
Journal Name
Journal Of Engineering
A Dual-Stage Perceptual-Harmonic Hybrid Estimator for Speech Enhancement
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This paper proposes a hybrid speech enhancement estimator that integrates the Perceptually-motivated Karhunen–Loève Transform (PKLT) with the Dual-Masking Harmonic-based (DMH) algorithm in a unified framework termed PKDMH. The main novelty lies in combining perceptual subspace projection with harmonic-residual suppression, enabling the system to jointly remove noise while preserving speech-relevant spectral cues. PKLT first performs perceptual subspace projection and suppresses inaudible components, after which DMH eliminates remaining broadband and harmonic residuals. The proposed PKDMH system was evaluated using the TIMIT dataset contaminated with five noise types: White, Pink, F16, Airport, and Car noise—across five SNR leve

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Publication Date
Wed Jan 01 2020
Journal Name
Ieee Access
Smart Routing Management Framework Exploiting Dynamic Data Resources of Cross-Layer Design and Machine Learning Approaches for Mobile Cognitive Radio Networks: A Survey
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Publication Date
Tue Mar 01 2022
Journal Name
Journal Of Osseointegration & Oral Rehablitation
Evaluation of marginal bone loss around SLActive implants by CBCT using different implant dimensions and surgical approaches: A clinical and radiological prospective study
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Aim: The reduction in the amount of marginal bone is the most important demand for the long term success of dental implants. This prospective clinical study was aimed to investigate the marginal bone loss of early loaded SLActive implants with different dimensions and surgical approaches. Materials and methods Fifteen patients aged from 18 to 60 years were divided into 2 groups (flapped and flapless approach) that underwent delayed implant placement protocol with SLActive implants. The marginal bone level was estimated by cone-beam computed tomography during three different periods: preoperatively, 8 weeks after surgery and 24 weeks after loading of the prosthesis. Results: The mean value of marginal bone level was not significantly chan

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