Navegando por Palavras-chave "Efavirenz"

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    Avaliação Das Propriedades Físico-Químicas Das Amostras Cristalizadas De Efavirenz E Seu Impacto Na Formação De Comprimidos E Na Dissolução
    (Universidade Federal de São Paulo (UNIFESP), 2017-05-31) Oliveira, Maira Paladini De [UNIFESP]; Cuffini, Silvia Lucia [UNIFESP]; Universidade Federal de São Paulo (UNIFESP)
    HIV infection is a complex disease of slow and uncertain course that leads the individual to develop the acquired immunodeficiency syndrome (AIDS, or, more commonly, its acronym in English, AIDS). In view of the complexity of the disease and the need for a chronic treatment of it, the improvement in the properties of drugs for the treatment of patients is increasing. Efavirenz (EFV), a major antiretroviral therapy agent, is the most commonly used non-nucleoside reverse transcriptase inhibitor (NNRIT) in highly active antiretroviral therapy (HAART) for the treatment of adults And as part of efforts to simplify and optimize first-line treatment, the World Health Organization (WHO) has recommended EFV as the first choice. EFV is a Class II drug under the Biopharmaceutical Classification System , Which has a low solubility and high permeability, and is therefore interested in the development of strategies to increase solubility and / or dissolution, as well as to control manufacturing processes such as compression Which could modify critical parameters in the dissolution as the polymorphism, the morphology among others. Is one of the manufacturing processes that has the greatest impact on the dissolution of a drug. During this process, some physical-chemical parameters such as crystalline or polymorphic structure, morphology and particle size, microstructure, etc. are modified. In this work, the EFV solvent crystallization was carried out, varying solvents, temperatures and agitation. Thus, they obtained 27 crystallized samples and from them were made physical-chemical analyzes to evaluate the impact of these samples in relation to the polymorphism, particle size, Hausner factor, Carr index in the compression of the drug. Thus, it was found that the compression performed, given the axial force applied to the tabletting had better result for Polymorph I tablets, as well as the hardness was also higher for these tablets. And finally, it evaluated the dissolution efficiency of the tablets formed by the compressor, and having the highest rate of dissolution reached was by a tablet of Polimorph II.
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    Correlation between microstructure and bioequivalence in Anti-HIV Drug Efavirenz
    (Elsevier B.V., 2015-04-01) Fandaruff, Cinira; Segatto Silva, Marcos Antonio; Galindo Bedor, Danilo Cesar; Santana, Davi Pereira de; Antunes Rocha, Helvecio Vinicius; Rebuffi, Luca; Azanza Ricardo, Cristy Leonor; Scardi, Paolo; Cuffini, Silvia Lucia [UNIFESP]; Universidade Federal de Santa Catarina (UFSC); Universidade Federal de Pernambuco (UFPE); Inst Tecnol Farmacos Farmanguinhos FIOCRUZ; Univ Trento; Elettra Sincrotrone Trieste; Universidade Federal de São Paulo (UNIFESP)
    Polymorphism and particle size distribution can impact the dissolution behaviour and, as a consequence, bioavailability and bioequivalence of poorly soluble drugs, such as Efavirenz (EFV). Nevertheless, these characteristics do not explain some failures occurring in in vitro assays and in in vivo studies. EFV belongs to Class II and the High Activity Antiretroviral Therapy (HAART) is considered the best choice in the treatment of adults and children. EFV is a drug that needs bioequivalence studies for generic compounds. in this work, six raw materials were analyzed and two of them were utilized with human volunteers (in vivo assays or bioequivalence). All the routine pharmaceutical controls of raw materials were approved; however, the reasons for the failure of the bioequivalence assay could not be explained with current knowledge. the aim of this work was to study microstructure, a solid-state property of current interest in the pharmaceutical area, in order to find an explanation for the dissolution and bioequivalence behaviour. the microstructure of EFV raw materials was studied by Whole Powder Pattern Modelling (WPPM) of X-ray powder diffraction data. Results for different EFV batches showed the biorelevance of the crystalline domain size, and a clear correlation with in vitro (dissolution tests) and in vivo assays (bioequivalence). (C) 2015 Elsevier B.V. All rights reserved.
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    Impacto Das Condições De Cristalização Sobre Polimorfismo, Morfologia, Microestrutura Do Efavirenz
    (Universidade Federal de São Paulo (UNIFESP), 2017-02-21) Guimaraes, Renata [UNIFESP]; Cuffini, Silvia Lucia [UNIFESP]; Universidade Federal de São Paulo (UNIFESP)
    Efavirenz (EFV) is an antiretroviral used for the treatment of HIV infection, which causes Acquired Immunodeficiency Syndrome (AIDS). In 2013 in Brazil, it was estimated that approximately 800,000 people living with HIV (Human Immunodeficiency Virus). EFV shows proper characteristics that make it an antiretroviral most commonly used against the virus as high power viral suppression, proven long-term efficacy and low risk of adverse effects. However, its low solubility is a constraining factor in the pharmaceutical industry. There are different approaches to improve the properties of the solid crystalline forms of poorly soluble drugs. Crystallization is one of the strategies that impacts on these properties. However, there are no studies on the impact of crystallization conditions on the polymorphism, morphology and crystalline domain of EFV solid forms and their correlation with dissolution properties. This project prepared different EFV samples, controlling the polymorphism and morphology through the crystallization conditions (type of solvent, nucleation temperature and cooling rate). The samples obtained under different conditions were characterized for polymorphism, morphology, microstructure and dissolution. It was observed that the temperature has greater influence on the obtained polymorph. Polymorph I can only be obtained at high temperatures. Mixtures are favored at intermediate temperatures and agitation hinders the formation of pure polymorphs. The agitation also impacts the microstructure, but is more intrinsically bound to the type of polymorph, so that polymorph II is more crystalline than the I. Likewise, the type of polymorph also has great influence on the final morphology, with each polymorph has a characteristic morphology. However, high agitation also impacts the final external shape of the crystal.