生物活性Salcaprozatesodium(SNAC)是一種口服吸收促進(jìn)劑，有潛力作為口服形式的肝素和胰島素的遞送劑。Salcaprozatesodium可增加非共價(jià)大分子絡(luò)合引起的親脂性，從而增加小腸上皮細(xì)胞的被動(dòng)跨細(xì)胞滲透。體外研究SNAC(12.5-400μg/mL;24h)hasnotoxicitytoCaco-2cells,andthesurvivalpercentageisabove90%whenSNACis200μg/mL.SNAC(50and200μg/mL)improvestheapparentpermeabilitycoeffcient(Papp)ofRAandSA-Bby2.14-foldand3.68-foldcomparedwiththePappofSAssolution.體內(nèi)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.