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http://www.repositorio.ufop.br/jspui/handle/123456789/11015
Título: | In silico and in vitro prediction of gastrointestinal absorption from potential drug eremantholide C. |
Autor(es): | Caldeira, Tamires Guedes Guimarães, Dênia Antunes Saúde Dezani, André Bersani Serra, Cristina Helena dos Reis Souza, Jacqueline de |
Palavras-chave: | Parallel artificial membrane permeability assay Solubility Permeability shake-flask |
Data do documento: | 2018 |
Referência: | CALDEIRA, T. G. et al. In silico and in vitro prediction of gastrointestinal absorption from potential drug eremantholide C. Journal of Pharmacy and Pharmacology, v. 69, p. 1468-1476, 2017. Disponível em: <https://onlinelibrary.wiley.com/doi/full/10.1111/jphp.12783>. Acesso em: 25 fev. 2019. |
Resumo: | Objectives Analysis of the biopharmaceutical properties of eremantholide C, sesquiterpene lactone with proven pharmacological activity and low toxicity, is required to evaluate its potential to become a drug. Methods Preliminary analysis of the physicochemical characteristics of eremantholide C was performed in silico. Equilibrium solubility was evaluated using the shake‐flask method, at 37.0 °C, 100 rpm during 72 h in biorelevant media. The permeability was analysed using parallel artificial membrane permeability assay, at 37.0 °C, 50 rpm for 5 h. The donor compartment was composed of an eremantholide C solution in intestinal fluid simulated without enzymes, while the acceptor compartment consisted of phosphate buffer. Key findings Physicochemical characteristics predicted in silico indicated that eremantholide C has a low solubility and high permeability. In‐vitro data of eremantholide C showed low solubility, with values for the dose/solubility ratio (ml): 9448.82, 10 389.61 e 15 000.00 for buffers acetate (pH 4.5), intestinal fluid simulated without enzymes (pH 6.8) and phosphate (pH 7.4), respectively. Also, it showed high permeability, with effective permeability of 30.4 × 10−6 cm/s, a higher result compared with propranolol hydrochloride (9.23 × 10−6 cm/s). Conclusions The high permeability combined with its solubility, pharmacological activity and low toxicity demonstrate the importance of eremantholide C as a potential drug candidate. |
URI: | http://www.repositorio.ufop.br/handle/123456789/11015 |
Link para o artigo: | https://onlinelibrary.wiley.com/doi/full/10.1111/jphp.12783 |
ISSN: | 20427158 |
Aparece nas coleções: | DEFAR - Artigos publicados em periódicos |
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ARTIGO_SilicoVitroPrediction.pdf Restricted Access | 275,51 kB | Adobe PDF | Visualizar/Abrir |
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