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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 Aug 01 2023
Journal Name
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A New Model Design for Combating COVID -19 Pandemic Based on SVM and CNN Approaches
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       In the current worldwide health crisis produced by coronavirus disease (COVID-19), researchers and medical specialists began looking for new ways to tackle the epidemic. According to recent studies, Machine Learning (ML) has been effectively deployed in the health sector. Medical imaging sources (radiography and computed tomography) have aided in the development of artificial intelligence(AI) strategies to tackle the coronavirus outbreak. As a result, a classical machine learning approach for coronavirus detection from      Computerized Tomography (CT) images was developed. In this study, the convolutional neural network (CNN) model for feature extraction and support vector machine (SVM) for the classification of axial

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Fri Jan 01 2016
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New Combined Technique for Fingerprint Image Enhancement
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This paper presents a combination of enhancement techniques for fingerprint images affected by different type of noise. These techniques were applied to improve image quality and come up with an acceptable image contrast. The proposed method included five different enhancement techniques: Normalization, Histogram Equalization, Binarization, Skeletonization and Fusion. The Normalization process standardized the pixel intensity which facilitated the processing of subsequent image enhancement stages. Subsequently, the Histogram Equalization technique increased the contrast of the images. Furthermore, the Binarization and Skeletonization techniques were implemented to differentiate between the ridge and valley structures and to obtain one

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Thu Jul 01 2021
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Forecasting enhancement using a hodrick-prescott filter
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Publication Date
Sun Feb 28 2021
Journal Name
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HEAT TRANSFER ENHANCEMENT USING PASSIVE TECHNIQUE: REVIEW
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Preserving and saving energy have never been more important, thus the requirement for more effective and efficient heat exchangers has never been more important. However, in order to pave the way for the proposal of a truly efficient technique, there is a need to understand the shortcomings and strengths of various aspects of heat transfer techniques. This review aims to systematically identify these characteristics two of the most popular passive heat transfer techniques: nanofluids and helically coiled tubes. The review indicated that nanoparticles improve thermal conductivity of base fluid and that the nanoparticle size, as well as the concentrations of the nanoparticles plays a major role in the effectiveness of the nanofluids.

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RC5 Performance Enhancement Based on Parallel Computing
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Enhancement of Uniformity of Solid Particles in Spouted Bed Using Stochastic Optimization
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Performance of gas-solid spouted bed benefit from solids uniformity structure (UI).Therefore, the focus of this work is to maximize UI across the bed based on process variables. Hence, UI is to be considered as the objective of the optimization process .Three selected process variables are affecting the objective function. These decision variables are: gas velocity, particle density and particle diameter. Steady-state solids concentration measurements were carried out in a narrow 3-inch cylindrical spouted bed made of Plexiglas that used 60° conical shape base. Radial concentration of particles (glass and steel beads) at various bed heights and different flow patterns were measured using sophisticated optical probes. Stochastic Genetic

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Publication Date
Mon Feb 18 2019
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Enhancement of gas response of annealed ZnO film for hydrogen gas detection
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Enhancement of surface properties of polyetheretherketone implant material by fractional laser texturing
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Background: Polyetheretherketone (PEEK) is a promising implant material due to its superior biomechanical strength. However, due to its hydrophobic nature and lack of cellular adhesion properties, it has poor integration with bone tissue. Methods: A fractional CO2 laser was used with various parameters for surface texturing of PEEK substrate to enhance its surface properties. An optical microscope and field-emission scanning electron microscope (FESEM) were used to examine the surface morphology of untextured and laser-textured samples. Energy dispersive X-ray spectroscopy (EDX) was performed to determine the effect of the laser on the microstructure of PEEK. Surface microroughness, atomic force microscopy (AFM), and wettability were invest

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Wed Jan 01 2020
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Data steganography is a technique used to hide data, secret message, within another data, cover carrier. It is considered as a part of information security. Audio steganography is a type of data steganography, where the secret message is hidden in audio carrier. This paper proposes an efficient audio steganography method that uses LSB technique. The proposed method enhances steganography performance by exploiting all carrier samples and balancing between hiding capacity and distortion ratio. It suggests an adaptive number of hiding bits for each audio sample depending on the secret message size, the cover carrier size, and the signal to noise ratio (SNR). Comparison results show that the proposed method outperforms state of the art methods

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