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Improved oral bioavailability of Cajaninstilbene acid using metabolism-inhibitory self-miroemulsion

姬赐玉  FeiFei Yang  RuiLe Pan  Qi Chang  YuBin Ji  YongHong Liao  
【摘要】:Cajaninstilbene acid(CSA), a natural phenolic compound with extensive phar-macological activities, exhibits limited oral bioavailability due to intestinal udp-glucu-ronictransferase(UGT)-mediated metabolism. Therefore, we hypothesized that involving UGT inhibitors in formulation is an effective way to improve the oral bioavailability of CSA. The purpose of this study was to the bioavailability of CSA using UGT-enzyme inhibitors containing self-microemulsion(SME). we set out to prepare SME-1 with UGT inhibitory pharmaceutical excipients(SME prepared from excipients without inhibitory activities named SME-2), and compared pharmacokinetics of CSA and CSA-G(metabolite of CSA) after oral administration of SME-1, SME-2 and free drug. Higher CSA(Fig.A) level, reduced CSA-G(Fig.B) level and increased systemic bioavailability were observed post SME-1 administration compared with SME-2 and free drug. In vivo results demonstrated that the molar ratios of CSA-G/CSA were 133.18±21.74 and 87.52±4.56 for free drug and SME-2, respectively. It decreased to 45.31±8.42 in SME-1 group. Remarkably, production of CSA-G reduced 29.70% and 47.9% in SME-1 relative to SME-2 and free drug. Pharmacokinetic study confirmed the potential of UGT inhibitory excipients containing SME in increasing bioavailability of CSA through inhibiting glucuronidation. In conclusion, involving of UGT inhibitory excipients in SME formulation is an approach to improve oral bioavailability of those undergoing UGT-mediated intestinal metabolism.

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