In vitro dissolution method fitted to in vivo absorption profile of rivaroxaban immediate-release tablets applying in silico data.
Drug Dev Ind Pharm
; 44(5): 723-728, 2018 May.
Article
em En
| MEDLINE
| ID: mdl-29192518
ABSTRACT
OBJECTIVE:
This study aimed to develop and validate an in vitro dissolution method based on in silico-in vivo data to determine whether an in vitro-in vivo relationship could be established for rivaroxaban in immediate-release tablets.SIGNIFICANCE:
Oral drugs with high permeability but poorly soluble in aqueous media, such as the anticoagulant rivaroxaban, have a major potential to reach a high level of in vitro-in vivo relationship. Currently, there is no study on scientific literature approaching the development of RIV dissolution profile based on its in vivo performance. METHODS ANDRESULTS:
Drug plasma concentration values were modeled using computer simulation with adjustment of pharmacokinetic properties. Those values were converted into drug fractions absorbed by the Wagner-Nelson deconvolution approach. Gradual and continuous dissolution of RIV tablets was obtained with a 30 rpm basket on 50 mM sodium acetate +0.2% SDS, pH 6.5 medium. Dissolution was conducted for up to 180 min. The fraction absorbed was plotted against the drug fraction dissolved, and a linear point-to-point regression (R2 = 0.9961) obtained.CONCLUSION:
The in vitro dissolution method designed promoted a more convenient dissolution profile of RIV tablets, whereas it suggests a better relationship with in vivo performance.Palavras-chave
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Solubilidade
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Comprimidos
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Rivaroxabana
Idioma:
En
Ano de publicação:
2018
Tipo de documento:
Article