Abstract:
:ABSTRCT Felodipine has been widely used as a poorly water-soluble model drug for various studies to improve its oral bioavailability and in vivo efficacy. In this study, we developed amorphous solid dispersions (ASDs) via spray drying to enhance the bioavailability of felodipine through using natural zein protein as a novel polymeric excipient. The solid state characterization results demonstrated a single glass transition temperature (Tg ) around 128.6 °C and good physical stability post 3 months accelerated study under the condition of 40 °C and 75% relative humidity (RH), which is possibly accounted for the molecular immobilization and hydrogen bonding interactions between felodipine and zein. By combining the in vitro dissolution study with TIM-1 gastrointestinal simulation investigation, it is indicated that felodipine was rapidly released from the ASD in 30 mins, and the supersaturation of felodipine was well maintained over 6 h, which resulted in a significant enhancement of felodipine bioavailability during simulated digestive processes in the upper GI tract. This study suggests that spray drying combined with natural excipient zein is an efficient formulation strategy for the development of ASDs with enhanced aqueous solubility and bioavailability.
journal_name
Pharm Dev Technoljournal_title
Pharmaceutical development and technologyauthors
Zhang H,Liu X,Ma Xdoi
10.1080/10837450.2020.1809456subject
Has Abstractpub_date
2020-12-01 00:00:00pages
1226-1237issue
10eissn
1083-7450issn
1097-9867journal_volume
25pub_type
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journal_title:Pharmaceutical development and technology
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pub_type: 杂志文章,评审
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pub_type: 杂志文章,评审
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