Estudo químico-farmacológico e desenvolvimento galênico de Spondias dulcis Forst
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Data
2017-09-21
Autores
Fernandes, Felipe Hugo Alencar [UNESP]
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Editor
Universidade Estadual Paulista (Unesp)
Resumo
Objetivou-se, neste trabalho, realizar um estudo químico-farmacológico, bem como o desenvolvimento de uma formulação galênica das folhas de Spondias dulcis Forst., conhecida popularmente como cajarana. Está planta apresenta uso popular como antiinflamatório e antisséptico. Inicialmente, foi feita uma avaliação farmacognóstica e microbiológica da droga. Em seguida, foram produzidos extratos hidroalcoólicos utilizando delineamento experimental e desenvolvido e validado um método para quantificação de polifenóis totais. O extrato hidroalcoólico foi avaliado em ensaios in vitro (atividade antimicrobiana e antioxidante) e in vivo (atividade laxante e toxicidade aguda). O componente majoritário foi identificado e isolado, utilizando técnicas de cromatografia em contracorrente e de espectroscopia. Por fim, foi desenvolvida e caracterizada uma dispersão sólida obtida com extrato e o polímero PVP K30 e avaliada sua estabilidade, utilizando cinética não isótermica. A droga vegetal foi caraterizada pela densidade aparente, tamanho de partícula, perda por dessecação, pH e teor de extrativos e controle microbiológico. A espectroscopia na região do infravermelho permitiu a identificação de grupamentos específicos provenientes de diversos metabólitos e a análise térmica identificou seis etapas de degradação. O extrato escolhido foi obtid por turboextração, utilizando a solução de 50% de etanol com 20% de droga vegetal. O método desenvolvido e validado para polifenóis totais apresentoi-se dentro das conformidades nas figuras de mérito (seletividade, linearidade, precisão, exatidão e robustez). A atividade farmacológica verificada foi o efeito laxante, resultado oposto ao descrito na literatura, porém reforçado pelo ensaio de toxicidade aguda. No ensaio de toxicidade, nenhum animal veio a óbito e todos os órgãos e enzimas hepáticas avaliadas não apresentaram diferença estatística significativa. O extrato hidroalcoólico das folhas de S. dulcis não apresentou atividade antimicrobiana frente aos microorganismos Staphylococcus aureus, S. epidermidis, Escherichia coli, Salmonella e Pseudomonas aeruginosa. Já a atividade antioxidante foi bastante relevante quando comparada ao ácido gálico e à quercetina. Através da cromatografia em contracorrente foi possível isolar a rutina como componente majoritário, a qual foi confirmada pelos espectros de RMN. Por fim, a dispersão sólida apresentou aspecto amorfo, caracterizada por MEV e DRX e análise térmica. Dessa forma, o extrato hidroalcoólico das folhas de S. dulcis, apresentou-se rico em polifenóis e com potencial farmacológico como antioxidante e laxativo e a formulação apresentou-se como uma boa alternativa para veiculação do extrato.
The objective of this work was to conduct a chemical-pharmacological study, as well as the development of a galenic formulation of the leaves of Spondias dulcis Forst., known as cajarana. This plant presents popular use as antiinflammatory and antiseptic. Initially, a pharmacological and microbiological evaluation of the herbal drug. Hydroalcoholic extracts were produced using experimental design and developed and validated a method for quantification of total polyphenols. The hydroalcoholic extract was evaluated in vitro tests (antimicrobial and antioxidant activity) and in vivo (laxative activity and acute toxicity). The main component, identified and isolated, countercurrent chromatography and spectroscopy techniques. Finally, a solid dispersion obtained with extract and the polymer PVP K30 was developed and characterized and its stability evaluated using non-isothermal kinetics. The herbal drug was characterized by apparent density, part size, desiccation loss, pH and extractive content and microbiological control. The infrared spectroscopy identified of specific data of several metabolites and a thermal analysis identified six stages of degradation. The extract were produced by turboextraction, use a solution of 50% ethanol with 20% plant drug. The method developed and validated for total polyphenols presented within the conformities in the figures of merit (selectivity, linearity, precision, accuracy and robustness). The pharmacological activity verified in the case of the effect, as opposed to literature in the literature, and reinforced by the acute toxicity test. No toxicity test, no animal died and all liver and liver enzymes evaluated did not present significant statistical difference. The hydroalcoholic extract of the leaves of S. dulcis did not present antimicrobial activity against the microorganisms Staphylococcus aureus, S. epidermidis, Escherichia coli, Salmonella sp. and Pseudomonas aeruginosa. The antioxidant activity was quite relevant when compared to gallic acid and quercetin. Countercorrent chromatography it was possible to isolate a rutine, as the major component. The data was confirmed by NMR spectra. Finally, a solid dispersion presented an amorphous appearance, characterized by SEM and XRD and thermal analysis. Thus, the hydroalcoholic extract of the leaves of S. dulcis, was rich in polyphenols and with pharmacological potential as antioxidant and laxative, and a formulation presented as a good alternative for the application of the extract.
The objective of this work was to conduct a chemical-pharmacological study, as well as the development of a galenic formulation of the leaves of Spondias dulcis Forst., known as cajarana. This plant presents popular use as antiinflammatory and antiseptic. Initially, a pharmacological and microbiological evaluation of the herbal drug. Hydroalcoholic extracts were produced using experimental design and developed and validated a method for quantification of total polyphenols. The hydroalcoholic extract was evaluated in vitro tests (antimicrobial and antioxidant activity) and in vivo (laxative activity and acute toxicity). The main component, identified and isolated, countercurrent chromatography and spectroscopy techniques. Finally, a solid dispersion obtained with extract and the polymer PVP K30 was developed and characterized and its stability evaluated using non-isothermal kinetics. The herbal drug was characterized by apparent density, part size, desiccation loss, pH and extractive content and microbiological control. The infrared spectroscopy identified of specific data of several metabolites and a thermal analysis identified six stages of degradation. The extract were produced by turboextraction, use a solution of 50% ethanol with 20% plant drug. The method developed and validated for total polyphenols presented within the conformities in the figures of merit (selectivity, linearity, precision, accuracy and robustness). The pharmacological activity verified in the case of the effect, as opposed to literature in the literature, and reinforced by the acute toxicity test. No toxicity test, no animal died and all liver and liver enzymes evaluated did not present significant statistical difference. The hydroalcoholic extract of the leaves of S. dulcis did not present antimicrobial activity against the microorganisms Staphylococcus aureus, S. epidermidis, Escherichia coli, Salmonella sp. and Pseudomonas aeruginosa. The antioxidant activity was quite relevant when compared to gallic acid and quercetin. Countercorrent chromatography it was possible to isolate a rutine, as the major component. The data was confirmed by NMR spectra. Finally, a solid dispersion presented an amorphous appearance, characterized by SEM and XRD and thermal analysis. Thus, the hydroalcoholic extract of the leaves of S. dulcis, was rich in polyphenols and with pharmacological potential as antioxidant and laxative, and a formulation presented as a good alternative for the application of the extract.
Descrição
Palavras-chave
Plantas medicinais, Spondias dulcis, Cajarana, Motilidade intestinal, Dispersão sólida, Estudo de estabilidade, Herbal drugs, Motility intestinal, Solid dispersion, Stability study