8-(2-羟基苯甲酰胺基)辛酸钠

生物活性Salcaprozatesodium(SNAC)是一种口服吸收促进剂，有潜力作为口服形式的肝素和胰岛素的递送剂。Salcaprozatesodium可增加非共价大分子络合引起的亲脂性，从而增加小肠上皮细胞的被动跨细胞渗透。体外研究SNAC(12.5-400μg/mL;24h)hasnotoxicitytoCaco-2cells,andthesurvivalpercentageisabove90%whenSNACis200μg/mL.SNAC(50and200μg/mL)improvestheapparentpermeabilitycoeffcient(Papp)ofRAandSA-Bby2.14-foldand3.68-foldcomparedwiththePappofSAssolution.体内研究SNACimprovestheoralabsorptionofbothR1andSAsandenhancesbioavailabilityinrats.SNAC(2000mg/kg/d;oralgavagefor13weeks)relatedmortalityisevidentonlyatthe2000-mg/kg/dlevel,20%amongmalesand50%amongfemales;noclearcauseofdeathisevident.SNAC(100-1000mg/kg/d;oralgavagefor13weeks)inducesnomortalityintheWistarratstudyatdosesupto1000mg/kg/d.AnimalModel:Sprague-Dawleyrats(6-7weeks)Dosage:2000mg/kg/dAdministration:Oralgavagefor13weeksResult:Induced20%and50%mortalityinmalesandfemalesatthedoseof2000mg/kg/d.