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Objective Cryptotanshinone, derived from the roots of Salvia miltiorrhiza Bge and Salviaprzewalskii Maxim, is the major active component and possessed significant antibacterial, antidermatophytic, antioxidant, anti-inflammatory and anticancer activities.The objective of this study was to investigate the intestinal absorptive characteristics of cryptotanshinone as well as the absorptive behavior influenced by co-administration of diterpenoid tanshinones and danxingfang preparation using an in vitro everted rat gut sac model.Methods The everted rat gut sacs was prepared.All sample analysis was performed on an Agilent high performance liquid chromatography system.The uptake amount oferyptotanshinone in gut tissue and the recovery of cryptotanshinone at the concentration of 10, 50 and 100 μg/mL from the incubation medium in the serosal side, the medium in the mueosal side and gut sac tissue after 10-70 min incubation were examined.Results A good linear correlation between cr, ptotanshinone of absorption and the incubation time from 10 to 70 min.The concentration dependence showed that a non-linear correlation existed between the cryptotanshinone absorption and the concentration at 100 μg/mL.Coexisting diterpenoid tanshinones and danxingfang preparation could significantly enhance the absorption of cryptotanshinone.Coexisting diterpenoid tanshinones and danxingfang preparation, which influenced cryptotanshinones absorption, manifested as similar to that of the P-glycoprotein inhibitor.Conclusion The underlying mechanism of the improvement of oral bioavailability was proposed that coexisting diterpenoid tanshinones and danxingfang preparation could decrease the efflux transport of cryptotanshinone by P-glycoprotein.