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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 Feb 28 2021
Journal Name
Jurnal Teknologi
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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Enhancement of Buckling Resistance of Aluminized Long Columns of Stainless Steel AISI 303
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This paper has investigated experimentally the dynamic buckling behavior of AISI 303 stainless steel Aluminized and as received long columns. These columns, hot-dip aluminized and as received, are tested under dynamic buckling, 22 specimens, without aluminizing (type 1), and 50 specimens, with hot-dip aluminizing at different aluminizing conditions of dipping temperature and dipping time (type 2), are tested under dynamic compression loading and under dynamic combined loading (compression and bending) by using a rotating buckling test machine. The experimental results are compared with Perry Robertson interaction formula that used for long columns. Greenhill formula is used to get a mathematical model that descripts the buckling behavior

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Enhancement efficiency of cadmium selenium solar cell by doping within silver
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We studied at the morphology, structural setup, and optical characteristics of thin cadmium (CdSe) films a thickness of 250 nm that were created by thermal evaporation over glass, The films exhibited a hexagonal shape were crystalline, and tended to form grains in the (111) crystallographic direction, according to the X-ray diffraction examinations. These characteristics were established using the investigation's findings. Through the use of thin films of CdSe doped with Ag at a concentration of 1.5%, the crystal structure orientations for pure CdSe (25.32, 41.84) and CdSe:Ag (25.39, 41.01) that were both pure as well as those that were doped with silver were both determined. The band gap of the optical spectrum decreased by 1.93–

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Publication Date
Wed Jan 01 2020
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Enhancement of lsb audio steganography based on carrier and message characteristics
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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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This work aimed PVA nanofibers in a range of concentrations were successfully manufactured via electrospinning. PVA NFs/Si was effectively prepared using the electrospinning process. The structural, morphological, optical and electrical properties of the prepared PVA were studied using XRD, FE-SEM, UV-Vis spectrophotometer and I-V characteristics, respectively. The amorphous structure of PVA nanofibers was observed. The optical energy gap from ultraviolet to visible was between (2.75 and 2.41) eV, making this compound highly sensitive to visible orange light at 610 nm, with a photosensitivity of 66%. The optical energy gap of PVA/Si heterojunction was utilized to modify this film from the UV to the visible spectrum. As show in the results,

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Tue Jan 08 2019
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Enhancement of vanadium oxide doped Eu+3 for gas sensor application
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Fabrication and Enhancement of Organic Photodetectors Based on Iron Phthalocyanine Films
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