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Dissertations / Theses on the topic 'Pharmaceutical cocrystals'

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Published: 4 June 2021
Last updated: 10 March 2023

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1

Mukherjee, Sreya. "Crystal Engineering of Pharmaceutical Cocrystals." Scholar Commons, 2011. http://scholarcommons.usf.edu/etd/3258.

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Pharmaceutical cocrystals use principles of crystal engineering for the design of crystalline forms of drugs and can improve their solubility, bioavailability, stability and other important properties without changing the efficacy of the drug. Herein reported are pharmaceutical cocrystals of two API's, caffeine and Pentoxifylline. Research has indicated that caffeine has the ability to reverse AB; plaque deposition in the brain (believed to be the primary cause of Alzheimer's pathogenesis) and thus revert memory and improve cognitive impairment. But owing to the fast absorption rate and short
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2

Karki, Shyam. "Pharmaceutical cocrystals : preparation and properties." Thesis, University of Cambridge, 2009. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.611636.

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3

Zu, Hui. "Mass transport of pharmaceutical cocrystals." Diss., University of Iowa, 2017. https://ir.uiowa.edu/etd/6023.

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Cocrystals have two or more neutral components (drug and cocrystal former) in the same crystal lattice which are held together via non-covalent bonds. Since the presence of the cocrystal former alters the energy of the drug molecules and their physicochemical properties, the drug dissolution characteristics can be manipulated by cocrystallization. A diffusion-convection-reaction (DCR) model has been developed to predict cocrystal intrinsic dissolution rates from the rotating disk system. In this work, the DCR model was used to further analyze the dissolution characteristics of 1:1 and 2:1 cocr
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4

CVETKOVSKI, Aleksandar. "Molecular cocrystals of pharmaceutical interest." Doctoral thesis, Università degli studi di Ferrara, 2015. http://hdl.handle.net/11392/2389116.

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Crystal form (cocrystals, polymorphs, salts, hydrates and solvates) assortment remains a scientific challenge that implicates practical issues in the pharmaceutical industry at the late stage of drug development of pharmaceutical formulations and in early stage of synthesis and isolation of an API in favorable defined crystalline form. Indeed, the selection of the optimal crystal form of an API that indisputably impacts the drug development program is directly related to the API’s aqueous solubility. Since the aqueous solubility of an API is the benchmark for its drug delivery and absorption
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5

Dabros, Marta. "Pharmaceutical Polymorphs, Cocrystals and Solid Solutions." Digital WPI, 2009. https://digitalcommons.wpi.edu/etd-dissertations/30.

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6

Trask, Andrew Vincent. "Pharmaceutical cocrystals : design, synthesis and analysis." Thesis, University of Cambridge, 2006. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.613783.

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7

Lange, Linda [Verfasser]. "Phase Behavior of Pharmaceutical Cocrystals / Linda Lange." München : Verlag Dr. Hut, 2017. http://d-nb.info/1126296147/34.

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8

Issa, N. "Towards more efficient screening of pharmaceutical cocrystals." Thesis, University College London (University of London), 2011. http://discovery.ucl.ac.uk/1333228/.

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Pharmaceutical cocrystals are formed between active pharmaceutical ingredients (APIs) and coformers that are biologically safe. Cocrystals are of considerable relevance to the pharmaceutical industry as they offer the ability of optimizing the physical properties of an API whilst retaining its biological function. However, producing cocrystals is experimentally challenging and often results in undesired forms. The objective of work presented herein is to investigate a more effective screening approach. Assuming that the formation of cocrystals is thermodynamically driven, we tested whether a c
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9

Patel, Bhavnita. "Pharmaceutical co-amorphous materials and cocrystals : preparation and analysis." Thesis, University of Cambridge, 2013. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.648098.

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10

Tomaszewska, Irena. "In vitro and physiologically based pharmacokinetic models for pharmaceutical cocrystals." Thesis, University of Bath, 2013. https://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.607145.

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About 30% of commercial and developmental drugs exhibit poor solubility and thus poor bioavailability. Strategies that enhance solubility of such compounds have become more popular. Cocrystallisation is one of these strategies, so characterisation of in vitro performance of cocrystals is essential. Conventional dissolution systems (USP apparatus 1 and USP apparatus 2) are often not suitable for testing poorly soluble drugs due to failure in providing sink conditions and inability to change the media during the experiment. This project involves designing appropriate dissolution methods that wil
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11

Sander, John Roy George. "Expansions of supramolecular chemistry: nanocrystals, pharmaceutical cocrystals, imaging, and decorated olefins." Diss., University of Iowa, 2012. https://ir.uiowa.edu/etd/3527.

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Crystal engineering has matured into a design-driven field based on the exploitation of reliable interactions between the functional groups of molecules so as to achieve desired properties. The utility of crystal engineering has been realized in a breadth of fields and, as a microcosm of crystal engineering, this thesis will explore the application of crystal engineering in the pharmaceutical sciences, nanotechnology, synthetic chemistry, materials science, and biomedical imaging. As the trend in drug development continues to skew towards molecules with poor aqueous solubility the ability impr
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12

Odiase, Isaac Uhunomah. "An anti-solvent/solvent mixture approach for pharmaceutical cocrystals and salt at pilot-scale." Thesis, Durham University, 2014. http://etheses.dur.ac.uk/10566/.

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Cocrystals have generated a lot of interest due their ability to influence: physiochemical properties, optical properties etc. These properties are important in the pharmaceutical and food industry. In this thesis, the scale up of cocrystal synthesis is studied using a novel slurry cocrystallisation approach involving an anti-solvent and solvent mixture. The anti-solvent composition is typically > 97 %, with the solvent comprising the rest. This counter-intuitive approach resulted in > 95 % caffeine-oxalic acid cocrystal yield in less than 2 hrs. The mixed anti-solvent/solvent approach was app
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13

Singaraju, Aditya Bharadwaj. "Crystallographic and spectroscopic assessment of pharmaceutical material mechanics." Diss., University of Iowa, 2018. https://ir.uiowa.edu/etd/6643.

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Despite the advent of alternative dosage forms, solid dosage forms constitute a major proportion of dosage forms not only on the market, but also in many pharmaceutical companies’ pipelines. This is because of their superior stability and ease of manufacturing relative to other dosage forms. Although solid dosage forms have been the topic of discussion for decades, the process of compaction of these dosage forms is considered an art rather than science because of the empiricism that exists in this area. With the introduction of Quality by Design (QbD), it is imperative that the drug developmen
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14

Duncan, Andrew Jacob Edward. "Explorations in crystal engineering : supramolecular templates, helical assemblies, pharmaceutical reactivity, and applications to radio-imaging." Diss., University of Iowa, 2017. https://ir.uiowa.edu/etd/5931.

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Crystal engineering is a rapidly developing area of research with goals aimed at designing molecular solids with desired physical and chemical properties. By utilizing reliable intermolecular interactions, the principles of supramolecular chemistry are exploited in the solid state in order to achieve favorable arrangements of molecules in a crystal lattice. We have applied crystal engineering strategies to further develop the strategy of template-directed reactivity in the solid state. An evaluation of catechol, a regioisomer of the commonly used resorcinol template, was performed. Co-crystall
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15

Jadav, Niten B. "Novel Technology for Crystal Engineering of Pharmaceutical Solids." Thesis, University of Bradford, 2018. http://hdl.handle.net/10454/18177.

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The research work described in this thesis, the environmentally friendly novel "Microwave Assisted Sub-Critical water (MASCW)" technology for particle engineering of active pharmaceutical ingredients and excipients was developed. The present novel technology MASCW process is described as green technology as water is used as the solvent medium and microwave energy as external source of heat energy for generation of a particle with different morphological and chemical properties. In MASCW process supersaturated solution of APIs is prepared by dissolving solute in water at high tempe
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16

Qiao, Ning. "Investigation of carbamazepine-nicotinamide cocrystal solubility and dissolution by a UV imaging system." Thesis, De Montfort University, 2014. http://hdl.handle.net/2086/10201.

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In this study, the ability of pharmaceutical cocrystals on improving solubility and dissolution behaviour of poorly water soluble drug has been studied by a novel technique SDI300 UV imaging surface dissolution system. Pharmaceutical cocrystals of poorly water soluble drug carbamazepine (CBZ) were synthesized, which are 1: 1 carbamazepine - nicotinamide (CBZ-NIC) cocrystal, and 2:1 carbamazepine - succinic acid (CBZ-SUC) cocrystal. Firstly, dissolution and solution mediated phase transformation behaviour (SMPT) of CBZ-NIC cocrystal was studied by in situ techniques of UV imaging and Raman spec
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17

Cheney, Miranda L. "The Role of Cocrystals in Solid-State Synthesis of Imides and the Development of Novel Crystalline Forms of Active Pharmaceutical Ingredients." Scholar Commons, 2009. http://scholarcommons.usf.edu/etd/3693.

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With a greater understanding of the fundamentals of crystal engineering lays the potential for the development of a vast array of novel materials for a plethora of applications. Addressed herein is the latent potential of the current knowledge base with an emphasis upon cocrystallization and the desire for scientific exploration that will lead to the development of a future generation of novel cocrystals. The focus of this dissertation is to expand the cocrystallization knowledge base in two directions with the utilization of cocrystals in the novel synthetic technique of cocrystal controlled
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18

BOTTI, Giada. "Cocrystals, prodrugs, microparticles, cyclodextrins and nasal administration of active pharmaceutical substances: innovative strategies to modulate their oral bioavailability or their action site targeting." Doctoral thesis, Università degli studi di Ferrara, 2023. https://hdl.handle.net/11392/2504895.

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The experimental work presented in this Thesis involves new strategies focused during my Ph.D. activity to improve drug oral bioavailability, avoid side effects or promote the targeting of therapeutic agents to their action site. The co-crystallization strategy was applied to increase the dissolution rate and the permeability across the intestinal barrier of nitrofurantoin (NITRO), an antibiotic characterized by low aqueous solubility and low oral bioavailability. In particular, NITRO dissolution rate and permeability were compared with those of its cocrystals containing isoniazid (ISO), bipyr
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19

Kavuru, Padmini. "Crystal engineering of flavonoids." [Tampa, Fla] : University of South Florida, 2008. http://purl.fcla.edu/usf/dc/et/SFE0002463.

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20

Robinson, Fiona. "Approaches to Understanding the Milling Outcomes of Pharmaceutical Polymorphs, Salts and Cocrystals. The Effect of Different Milling Techniques (Ball and Jet) on the Physical Nature and Surface Energetics of Different Forms of Indomethacin and Sulfathiazole to Include Computational Insights." Thesis, University of Bradford, 2011. http://hdl.handle.net/10454/5412.

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The process of milling drugs to obtain samples with a desirable particle size range has been widely used in the pharmaceutical industry, especially for the production of drugs for inhalation. However by subjecting materials to milling techniques surfaces may become thermodynamically activated which may in turn lead to formation of amorphous material. Polymorphic conversions have also been noted after milling of certain materials. Salt and cocrystal formation is a good way of enhancing the properties of an API but little or no work has been published which investigates the stability of these en
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21

Lee, Hong-Guann. "Mechanistic studies of cocrystal dissolution behavior." Diss., University of Iowa, 2015. https://ir.uiowa.edu/etd/5548.

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The objective of this study is to investigate cocrystal solubility and dissolution behavior to elucidate the factors affecting these processes in various media. Six cocrystals with xanthines (theophylline (THP), caffeine (CAF) and theobromine (THB)) were prepared and characterized by powder X-ray diffraction and thermal methods. Two cocrystals (CAFCA I and THBSA) are new solids and their crystal structures were determined by single crystal X-ray diffraction. Cocrystal solubility behavior depended on the dissolving complex solubility and its dissociation behavior in solution. Two THP cocrystals
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22

Forbes, Safiyyah. "Hydrogen-bond driven supramolecular chemistry for modulating physical properties of pharmaceutical compounds." Diss., Manhattan, Kan. : Kansas State University, 2010. http://hdl.handle.net/2097/3756.

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23

Weyna, David Rudy. "Crystal Engineering of Multiple Component Crystal Forms of Active Pharmaceutical Ingredients." Scholar Commons, 2011. http://scholarcommons.usf.edu/etd/3406.

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Enhancing the physicochemical properties of solid-state materials through crystal engineering enables optimization of these materials without covalent modification. Cocrystals have become a reliable means to generate novel crystalline forms with multiple components and they exhibit different physicochemical properties compared to the individual components. This dissertation exemplifies methodologies to generate cocrystals of active pharmaceutical ingredients (API's) based upon knowledge of supramolecular interactions (supramolecular synthons), while focusing on enhanced delivery through in vit
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24

Oburn, Shalisa M. "Applications in supramolecular chemistry and solid-state reactivity: template-mediated solid-state reactions, dynamic covalent chemistry, mechanochemistry, and pharmaceutical co-crystals." Diss., University of Iowa, 2019. https://ir.uiowa.edu/etd/7004.

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Supramolecular chemistry and crystal engineering seek to control molecular packing in the solid state to influence the physical and chemical properties of crystalline solid materials. A goal of supramolecular chemistry that seeks to control molecular packing in the solid state focuses on exploiting non-covalent interactions to assemble molecules into desirable arrangements. Strategies implemented to control molecular packing rely on strong, directional interactions such as hydrogen bonding, halogen bonding, and metal coordination to direct localized arrangement of molecules in solids. In this
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25

Clarke, Heather Dawn Marie. "Crystal Engineering of Multi-Component Crystal Forms: The Opportunities and Challenges in Design." Scholar Commons, 2012. http://scholarcommons.usf.edu/etd/4013.

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There is heightened interest to diversify the range of crystal forms exhibited by active pharmaceutical ingredients (APIs) in the pharmaceutical industry. The crystal form can be regarded as the Achilles' heel in the development of an API as it directly impacts the physicochemical properties, performance and safety of the API. This is of critical importance since the crystal form is the preferred method of oral drug delivery by industry and regulatory bodies. The ability to rationally design materials is a lucrative avenue towards the synthesis of functional molecular solids with customi
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26

Elbagerma, Mohamed A. "Analytical method development for structural studies of pharmaceutical and related materials in solution and solid state : an investigation of the solid forms and mechanisms of formation of cocrystal systems using vibrational spectroscopic and X-ray diffraction techniques." Thesis, University of Bradford, 2010. http://hdl.handle.net/10454/4467.

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Analysis of the molecular speciation of organic compounds in solution is essential for the understanding of ionic complexation. The Raman spectroscopic technique was chosen for this purpose because it allows the identification of compounds in different states and it can give information about the molecular geometry from the analysis of the vibrational spectra. In this research the ionisation steps of relevant pharmaceutical material have been studied by means of potentiometry coupled with Raman spectroscopy; the protonation and deprotonation behaviour of the molecules were studied in different
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27

Smith, Adam John. "Modulating the Pharmacokinetics of Bioflavonoids." Scholar Commons, 2012. http://scholarcommons.usf.edu/etd/4226.

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One of the largest obstacles in drug development is to overcome solubility and bioavailability problems. Preformulation strategies such as nanoparticle formation are often employed but sometimes create new issues and are limited in their effectiveness and applications. Since the majority of drugs are marketed and sold as solid forms, drug delivery systems are not always desirable. This is where solid-state chemistry becomes important. Traditional solid-state chemistry approaches are often successful but are sometimes too restrictive and cannot be applied to certain compounds. Cocrystals h
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28

Dasgupta, Archi. "Analysis Of Intermolecular Interactions In Pharmaceutical Salts And Cocrystals." Thesis, 2011. http://etd.iisc.ernet.in/handle/2005/2123.

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The studies on cocrystals and salts presented in the the chapters clearly bring out the influence of intermolecular interactions as the main evaluators of the cocrystal-salt regime. The observations made in Chapter 2 indicate that in case if the cocrystal formation is through hydrogen bonds the location of the proton decides the nature of the complex in the energy landscape. The observation that the coformer controls the topology of intermolecular space as demonstrated in Chapter 3 provides insights into the importance of directionality rather than strength of intermolecular interactions. Inde
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29

Aitipamula, S., and Venu R. Vangala. "X-ray crystallography and its role in understanding physicochemical properties of pharmaceutical cocrystals." 2017. http://hdl.handle.net/10454/11421.

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Yes<br>Properties of a matter are intrinsically dependent upon the internal arrangement of molecules in the solid state. Therefore, knowledge of 3-dimensional structure of the matter is prerequisite for structure-property correlations and design of functional materials. Over the past century, X-ray crystallography has evolved as a method of choice for accurate determination of molecular structure at atomic resolution. The structural information obtained from crystallographic analysis paved the way for rapid development in electronic devices, mineralogy, geosciences, materials science, pharmace
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30

Baptista, Bárbara Violinha. "From synthesis to formulation of gliclazide and glibenclamide cocrystal pharmaceutical solid dosage forms." Master's thesis, 2017. http://hdl.handle.net/10451/34247.

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Tese de mestrado, Engenharia Farmacêutica, Universidade de Lisboa, Faculdade de Farmácia, 2017<br>Low solubility of pharmaceutical drugs is very often a limiting factor in the development of drug products. Cocrystals are known for a long time but still little explored as an alternative for drug solubility increase. Cocrystals are crystalline homogenous structures composed by two or more molecules in the same crystal lattice, all solid at room temperature. They are different from the precursors held together by noncovalent interactions (normally hydrogen bonds) with a well-defined stoichiometry
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31

Pêcego, Inês Gonçalves. "Synthesis of glibenclamide cocrystals through grinding methods." Master's thesis, 2018. http://hdl.handle.net/10451/40057.

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Tese de mestrado, Engenharia Farmacêutica, Universidade de Lisboa, Faculdade de Farmácia, 2018<br>The pharmaceutical industry has been struggling against problems related with drugs with low solubility as this is a very limiting factor in the development of drug products. Co-crystals are solid forms known for a very long time although they have not been fully explored in their potentialities. Co-crystals can be defined as crystalline homogenous structures composed of two or more compounds, held together by noncovalent bonds, usually hydrogen bonds, and solid at room temperature. These structur
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32

Korde, Sachin A., Sudhir K. Pagire, H. Pan, et al. "Continuous Manufacturing of Cocrystals Using Solid State Shear Milling Technology." 2018. http://hdl.handle.net/10454/15301.

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yes<br>Solid state shear milling (S3M) is reported as a scalable, continuous, polymer-assisted cocrystallization technique. A specially designed milling pan was employed to provide high levels of applied shear, and the addition of a polymeric processing aid enabled generation of high stress fields. Carbamazepine–salicylic acid cocrystals were produced with 5–25 wt % of poly(ethylene oxide) (PEO). A systematic study was carried out to understand the effect of process variables on properties and performance of the cocrystals. S3M offers an important new route for continuous manufacturing of phar
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33

Spong, Barbara Rodriguez. "Enhancing the pharmaceutical behavior of poorly soluble drugs through the formation of cocrystals and mesophases." 2005. http://books.google.com/books?id=KVVtAAAAMAAJ.

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34

Duarte, Íris Daniela Correia da Silva 1987. "Development of new screening methodologies and preparation methods with application in amorphous solid dispersions and pharmaceutical cocrystals." Doctoral thesis, 2016. http://hdl.handle.net/10451/25367.

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Tese de doutoramento, Farmácia (Tecnologia Farmacêutica), Universidade de Lisboa, Faculdade de Farmácia, 2016<br>The number of drugs with solubility limitations under development has been increasing. Limited aqueous solubility is a major challenge in the development of oral-dosage forms, as it may impact oral bioavailability. To circumvent this issue various solubilization strategies have been developed. Two of these strategies are the generation of amorphous solid dispersions and pharmaceutical cocrystals. Amorphous solid dispersions are today one of the most popular solubilization strategies
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35

Cordeiro, Catarina Isabel Costa. "Relatório de Estágio e Monografia intitulada "Cocristais iónicos: estratégia de desenvolvimento para ativos farmacêuticos sólidos"." Master's thesis, 2021. http://hdl.handle.net/10316/98990.

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Relatório de Estágio do Mestrado Integrado em Ciências Farmacêuticas apresentado à Faculdade de Farmácia<br>A cocristalização tem vindo a provar tratar-se de uma abordagem promissora no desenvolvimento de formas farmacêuticas sólidas, bem como na otimização de características como a solubilidade e a biodisponibilidade. Assim sendo, em virtude do aumento do interesse da indústria farmacêutica nesta área e até pela presença de alguns ativos na forma de cocristais farmacêuticos no mercado, verificou-se por parte das autoridades regulamentares a consequente criação de legislação específica. Dentro
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36

Shukla, A., E. Khan, M. H. D. Bashir Alsirawan, R. Mandal, P. Tandon, and Venu R. Vangala. "Spectroscopic (FT-IR, FT-Raman, and 13C SS-NMR) and quantum chemical investigations to provide structural insights into nitrofurantoin–4-hydroxybenzoic acid cocrystals." 2019. http://hdl.handle.net/10454/17019.

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Yes<br>Cocrystallization is an attractive approach to improving the physicochemical properties of active pharmaceutical ingredients (APIs), which have great potential in drug development. Accordingly, there is a growing need to understand the physicochemical changes that occur upon co-crystallisation. This work focuses on the combined use of spectroscopy and density functional theory (DFT) calculations to understand the molecular structure, hydrogen bond interactions and physicochemical properties of a pharmaceutical cocrystal. Solid-state NMR (ssNMR) spectroscopy can provide detailed molecula
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37

Marques, Ana Margarida Almeida. "Investigação de Cocristais Farmacêuticos e Estudos de Compatibilidade cocristal-excipiente. Dois Casos de Estudo: diflunisal-isoniazida e lamotrigina-etossuximida." Master's thesis, 2021. http://hdl.handle.net/10316/97965.

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Dissertação de Mestrado em Química apresentada à Faculdade de Ciências e Tecnologia<br>Esta dissertação teve como objetivo o estudo de cocristais com potencial para utilização em terapia dual, tendo-se, para isso, investigado os sistemas binários constituídos por diflunisal, um anti-inflamatório não esteróide, e isoniazida, um tuberculostático; diflunisal e etossuximida, um anticonculsivante; assim como o sistema que junta dois anticonvulsivantes com mecanismos de ação distintos, a lamotrigina e a etossuximida. O trabalho teve, ainda, como objetivo contribuir para o conhecimento da estabilidad
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38

Santos, João Afonso Sêco Vieira. "Nanococristais Farmacêuticos: Síntese, Caracterização e Otimização de Processos." Master's thesis, 2020. http://hdl.handle.net/10316/92566.

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Dissertação de Mestrado em Química apresentada à Faculdade de Ciências e Tecnologia<br>Este trabalho tem por objetivo a investigação da síntese e caracterização de nanococristais farmacêuticos, formas sólidas que, combinando o aumento da solubilidade e da velocidade de dissolução que se associa à formação de cocristais e à redução do tamanho de partículas, têm potencial para promover o aumento da absorção gastrointestinal e, consequentemente, o aumento da biodisponibilidade oral dos APIs. Os cocristais de (S)-naproxeno e nicotinamida (2:1) e de (RS)-ibuprofeno com o mesmo coformador (1:1)
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39

Dhumal, Ravindra S., Adrian L. Kelly, Peter York, Philip D. Coates, and Anant R. Paradkar. "Cocrystalization and simultaneous agglomeration using hot melt extrusion." 2010. http://hdl.handle.net/10454/5955.

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No<br>PURPOSE: To explore hot melt extrusion (HME) as a scalable, solvent-free, continuous technology to design cocrystals in agglomerated form. METHODS: Cocrystal agglomerates of ibuprofen and nicotinamide in 1:1 ratio were produced using HME at different barrel temperature profiles, screw speeds, and screw configurations. Product was characterized for crystallinity by XRPD and DSC, while the morphology was determined by SEM. Dissolution rate and tabletting properties were compared with ibuprofen. RESULTS: Process parameters significantly affected the extent of cocrystallization which improve
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40

Chow, P. S., G. Lau, W. K. Ng, and Venu R. Vangala. "Stability of Pharmaceutical Cocrystal During Milling: A Case Study of 1:1 Caffeine-Glutaric Acid." 2017. http://hdl.handle.net/10454/12360.

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yes<br>Despite the rising interest in pharmaceutical cocrystals in the past decade, there is a lack of research in the solid processing of cocrystals downstream to crystallization. Mechanical stress induced by unit operations such as milling could affect the integrity of the material. The purpose of this study is to investigate the effect of milling on pharmaceutical cocrystal and compare the performance of ball mill and jet mill, using caffeine-glutaric acid (1:1) cocrystal as the model compound. Our results show that ball milling induced polymorphic transformation from the stable Form II
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