Desde as primeiras civilizações, o homem, de forma empírica, buscava o alívio e a cura para as enfermidades que os acometiam. Descobriram nas plantas atividades medicinais e terapêuticas, passando a utilizar esse recurso para tratar as mais diversas doenças de acordo com o conhecimento adquirido no decorrer dos tempos. O medicamento fitoterápico é aquele obtido com uso exclusivo de matérias-primas vegetais, ou seja, ativos extraídos de plantas, ou parte específica que contém a atividade terapêutica. O objetivo do presente estudo é expor e confrontar informações sobre interações medicamentosas dentro da fitoterapia, tendo em vista que ainda há, na população, uma certa crença de que medicamentos derivados de plantas não apresentam eventos adversos. Trata-se de um estudo de revisão de literatura, onde os dados obtidos reforçam a importância desse tipo de informação para a sociedade, que cada vez mais busca nos medicamentos naturais alternativas para melhoria da saúde e longevidade. A pesquisa envolveu artigos entre 2008 e 2021, onde foi observado que há relatos significativos de interações medicamentosas associadas ao uso de fitoterápicos. Os dados levantados são de extrema importância para quebrar tabus relacionados à segurança dos medicamentos de origem natural, contribuindo para seu uso racional.
Objective: To perform the solid-state characterization and the in vitro-in vivo correlation (IVIVC) of three batches of efavirenz (EFV) active pharmaceutical ingredients. Significance: EFV is an effective anti-HIV drug. Due to the poor aqueous solubility, the rate and extent of EFV absorption deeply depend on its dissolution characteristics. Methods: Thermal analyses, x-ray diffraction, and particle size distribution were performed. The saturation solubility and dissolution profiles were assessed in 0.5% (w/v) sodium lauryl sulfate (SLS), fasted-state simulated intestinal fluid (FaSSIF), and fed-state simulated intestinal fluid (FeSSIF) using a flow-through cell. Each batch was orally administered to Wistar rats and the pharmacokinetic parameters were correlated with those obtained from in vitro dissolution. Results: All batches of EFV consisted polymorph I. EFV-A presented the lowest particle size distribution [d(v,0.5) ¼ 197.8 mm; d(v,0.9) ¼ 444.6 mm] followed by EFV-B [d(v,0.5) ¼ 223.9 mm; d(v,0.9) ¼ 481.1 mm], and EFV-C [d(v,0.5) ¼ 240.8 mm; d(v,0.9) ¼ 497.3 mm]. The saturated solubility in FaSSIF was 36% and 40% of that in FeSSIF and SLS, respectively. EFV-A presented the fastest rate and largest extension of dissolution than EFV-B and C (79.15%, 69.93% and 54.22%, respectively, as well as the highest maximum plasma concentration. Levels B, C, and multiple-C of IVIVC models were achieved.
Conclusion:The FaSSIF medium discriminated the dissolution profiles of EFV APIs. Small differences in particle size distribution had a significant impact on the biopharmaceutical parameters of EFV, suggesting that strict control of such parameter is an important aspect during API development and drug formulation.
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